Showing papers in "Molecules in 2006"
TL;DR: A series of novel 1-anilino-4-(arylsulfanylmethyl)phthalazines showed higher activity than a cisplatin control when tested in vitro against two different cancer cell lines using the microculture tetrazolium method (MTT) method.
Abstract: A series of novel 1-anilino-4-(arylsulfanylmethyl)phthalazines were designed and synthesized. The structures of all the compounds were confirmed by IR, 1H-NMR, elemental analysis and MS. The analogues 1-(3-chloro-4-fluoroanilino)-4-(3,4- difluorophenylthio-methyl)phthalazine (12) and 1-(4-fluoro-3-trifluoromethylanilino)-4- (3,4-difluorophenyl-thiomethyl)phthalazine (13) showed higher activity than a cisplatin control when tested in vitro against two different cancer cell lines using the microculture tetrazolium method (MTT) method.
126 citations
TL;DR: Five novel Schiff bases have been prepared from o-formylphenoxyacetic acid and a series of aminothiazoles to form a number of potentially biologically active compounds.
Abstract: Five novel Schiff bases have been prepared from o -formylphenoxyacetic acid and a series of aminothiazoles to form a number of potentially biologically active compounds. The structures of these Schiff bases have been characterized using IR and 1 H- and 13 C-NMR spectroscopy. Keywords: aminothiazoles, o -formylphenoxyacetic acid, Schiff bases, biological activity Introduction Schiff bases are used as substrates in the preparation of a number of industrial and biologically active compounds via ring closure, cycloaddition, and replacement reactions [1]. Moreover, Schiff bases are also known to have biological activities such as antimicrobial [2-5], antifungal [4-6], antitumor [7-9], and as herbicides [10]. Schiff bases have also been employed as ligands for complexation of metal ions [11]. On the industrial scale, they have wide range of applications such as dyes and pigments [12]. Keeping in view the facts mentioned, we decided to synthesize new Schiff bases which were predicted to have useful biological activity. The synthesis of other similar Schiff bases, their biological activity, and complex formation are under study.
88 citations
TL;DR: Compound 2, is the key intermediate for the synthesis of several series of new compounds such as Schiff's bases 3a-l, formic acid N'-[2-(7-hydroxy-2-oxo-2H-chromen-4-yl)acetyl] hydrazide and acetic acid N'(4-trifluoromethylphenylimino)methyl].
Abstract: (7-Hydroxy-2-oxo-2 H -chromen-4-yl)-acetic acid hydrazide ( 2 ) was prepared from (7-hydroxy-2-oxo-2 H -chromen-4-yl)-acetic acid ethyl ester ( 1 ) and 100% hydrazine hydrate. Compound 2 , is the key intermediate for the synthesis of several series of new compounds such as Schiff’s bases 3a-l , formic acid N'-[2-(7-hydroxy-2-oxo-2 H -chromen-4-yl)acetyl] hydrazide ( 4 ), acetic acid N'-[2-(7-hydroxy-2-oxo-2 H -chromen-4-yl)-acetyl] hydrazide ( 5 ), (7-hydroxy-2-oxo-2 H -chromen-4-yl)-acetic acid N'-[2-(4-hydroxy-2-oxo-2 H -chromen-3-yl)-2-oxoethyl] hydrazide ( 6 ), 4-phenyl-1-(7-hydroxy-2-oxo-2 H -chromen- 4-acetyl) thiosemicarbazide ( 7 ), ethyl 3-{2-[2-(7-hydroxy-2-oxo-2 H -chromen-4-yl)-acetyl]hydrazono}butanoate ( 8 ), (7-hydroxy-2-oxo-2 H -chromen-4-yl)-acetic acid N'-[(4-trifluoromethylphenylimino)methyl] hydrazide ( 9 ) and (7-hydroxy-2-oxo-2 H -chromen-4-yl)acetic acid N'-[(2,3,4-trifluorophenylimino)-methyl] hydrazide ( 10 ). Cyclo- condensation of compound
88 citations
TL;DR: The synthesis of three substituted 6,7-dihydroxy-4-quinazolineamines: tandutinib, erlotinib and gefitinib in improved yields is reported.
Abstract: The synthesis of three substituted 6,7-dihydroxy-4-quinazolineamines: tandutinib (1), erlotinib (2) and gefitinib (3) in improved yields is reported. The intermediates were characterized by NMR and the purities determined by HPLC.
86 citations
TL;DR: Several specific synthetic protocols were developed for the preparation from cyanuric chloride of a range of symmetric and non-symmetric di- and tri-substituted 1,3,5-triazines containing alkyl, aromatic, hindered, chiral and achiral hydroxyalkyl, ester and imidazole groups via sequential nucleophilic substitution of the C-Cl bond by C-O, C-N and C-S bonds.
Abstract: Several specific synthetic protocols were developed for the preparation from cyanuric chloride of a range of symmetric and non-symmetric di- and tri-substituted 1,3,5-triazines containing alkyl, aromatic, hindered, chiral and achiral hydroxyalkyl, ester and imidazole groups via sequential nucleophilic substitution of the C-Cl bond by C-O, C-N and C-S bonds.
79 citations
TL;DR: The qualitative and quantitative antimicrobial activity test results proved that all the prepared complexes are very active, especially against samples of Ps.
Abstract: The synthesis of Cu(II) complexes derived from Schiff base ligands obtainedby the condensation of 2-hydroxybenzaldehyde or terephtalic aldehyde with 4-amino-antipyrine (4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one) is presented. The newlyprepared compounds were characterized by 1H-NMR, UV-VIS, IR and ESRspectroscopy. The determination of the antimicrobial activity of the ligands and of thecomplexes was carried out on samples of Escherichia coli, Klebsiella pneumoniae,Acinetobacter boumanii, Pseudomonas aeruginosa, Staphylococcus aureus and Candidasp. The qualitative and quantitative antimicrobial activity test results proved that all theprepared complexes are very active, especially against samples of Ps. aeruginosa, A.Boumanii, E. coli and S. aureus.
77 citations
TL;DR: The content and distribution of stilbenes and resin acids in Scots pine and spruce sampled in central Norway, have been examined and significant amounts of lignans were present in the sapwood.
Abstract: The content and distribution of stilbenes and resin acids in Scots pine (Pinus sylvestris) and spruce (Picea abies), sampled in central Norway, have been examined. The contents of pinosylvin stilbenes in pine heartwood/living knots were 0.2-2/2-8 % (w/w). No stilbenes could be detected in spruce (Picea abies). The resin acid contents of pine sapwood/heartwood and knots were 1-4 and 5-10 % (w/w), respectively. Minor amounts of resin acids (<0.2/<0.04 %w/w) were identified in spruce wood/knots. The lignan content in knots of Norwegian spruce was 6.5 % (w/w). Diastereomerically pure hydroxymatairesinol (HMR, 84 % of total lignans) was readily isolated from this source since only minor quantities (2.6 % of total lignans) of the allo-HMR diastereomer was detected. Insignificant amounts of lignans were present in the sapwood. Lignans could not be detected in the sapwood or knots of Norwegian sallow (Salix caprea), birch (Betula pendula) or juniper (Juniperus communis).
76 citations
TL;DR: A simple, efficient, and general method for the synthesis of various alpha-aminophosphonate derivatives 4a-4l by treatment of substituted benzaldehydes and aniline with bis( 2-methoxyethyl)- or bis(2-ethoxy methyl) phosphite under microwave irradiation without solvents and catalysts is developed.
Abstract: A simple, efficient, and general method has been developed for the synthesis of various alpha-aminophosphonate derivatives 4a-4l by treatment of substituted benzaldehydes and aniline with bis(2-methoxyethyl)- or bis(2-ethoxyethyl) phosphite under microwave irradiation without solvents and catalysts. The products were characterized by elemental analysis, IR, 1H-NMR, 13C- and 31P-NMR spectra. The X-ray crystallographic data of the representative compound 4l was determined. The new alpha-aminophosphonate derivatives were found to possess moderate to good antiviral activity.
72 citations
TL;DR: A series of new 1,2/1,3-bis[o-(N-methylidenamino-3-aryl-5-phenyl-4H-1,2,4-triazole-4-yl)phenoxy]ethane/propane derivatives 4 were prepared in good yields by treatment of 4-amino.
Abstract: A series of new 1,2/1,3-bis[o-(N-methylidenamino-3-aryl-5-phenyl-4H-1,2,4-triazole-4-yl)phenoxy]ethane/propane derivatives 4 were prepared in good yields bytreatment of 4-amino-3-aryl-5-phenyl-4H-1,2,4-triazoles 2 with certain bis-aldehydes 1.Compounds 4 were reduced with NaBH4 to afford the corresponding 1,2/1,3-bis[o-(N-methylamino-3-aryl-5-phenyl-4H-1,2,4-triazole-4-yl)phenoxy]ethane/propane derivatives5. All new compounds were characterized by IR, 1H-NMR, 13C-NMR and mass spectraldata.
70 citations
TL;DR: This review covers all the literature related to the ring contraction of cyclic ketones and olefins promoted by iodine(III) species.
Abstract: Hypervalent iodine reagents constitute a powerful tool in modern synthetic organic chemistry, promoting several important reactions. One such reaction is the ring contraction of cycloalkenes and cycloalkanones promoted by iodine(III) compounds, such as iodobenzene diacetate, iodosylbenzene, iodotoluene difluoride, and [hydroxy(tosyloxy)- iodo]benzene (Koser s reagent). This review covers all the literature related to the ring contraction of cyclic ketones and olefins promoted by iodine(III) species.
65 citations
TL;DR: 2-Thiohydantoin derivatives are produced by heating a mixture of thiourea and an alpha-amino acid and the method described offers the advantages of simplicity, low cost, easy work-up and scalability.
Abstract: 2-Thiohydantoin derivatives are produced by heating a mixture of thiourea and an α-amino acid. The method described offers the advantages of simplicity, low cost, easy work-up and scalability. Keywords: Amino acids, Antiviral agents, Cyclization, Heterocycles, 2-Thiohydantoin Introduction Thiohydantoins are sulfur analogs of hydantoins with one or both carbonyl groups replaced by thiocarbonyl groups [1]. Among the known thiohydantoins, 2-thiohydantoins are most notably known due of their wide applications as hypolipidemic [2], anticarcinogenic [3], antimutagenic [4], antithyroidal [5] antiviral (e.g., against herpes simplex virus, HSV) [6], human immunodeficiency virus (HIV) [7] and tuberculosis [8]), antimicrobial (antifungal and antibacterial) [9], anti-ulcer and anti-inflammatory agents [10], as well as pesticides [11]. Additionally, 2-thiohydantoins have been used as reference standards for the development of C-terminal protein sequencing [12], as reagents for the development of dyes [13] and in textile printing, metal cation complexation and polymerization catalysis [14]. It is therefore not surprising that various different synthetic methods have been developed to prepare 2-thiohydantoin and its derivatives. Some of the most commonly used methods are the treatment of α-amino acids with acetic anhydride followed by ammonium thiocyanate [15] and the coupling reaction between α-amino acid derivatives and isothiocyanate [4a,12b,16]. Other preparative methods for 2-thiohydantoins include the reactions between thiourea and benzil [17],
TL;DR: A review of results of bioactivity and reactivity examinations of marine sesquiterpene (hydro)quinones is presented, focused mostly on friedo- rearranged drimane structural types isolated from sponges of the order Dictyoceratida.
Abstract: A review of results of bioactivity and reactivity examinations of marine sesquiterpene (hydro)quinones is presented. The article is focused mostly on friedo- rearranged drimane structural types, isolated from sponges of the order Dictyoceratida. Examples of structural correlations are outlined. Available results on the mechanism of redox processes and examinations of chemo- and regioselectivity in addition reactions are presented and, where possible, analyzed in relation to established bioactivities. Most of the bioactivity examinations are concerned with antitumor activities and the mechanism thereof, such as DNA damage, arylation of nucleophiles, tubulin assembly inhibition, protein kinase inhibition, inhibition of the arachidonic cascade, etc. Perspectives on marine drug development are discussed with respect to biotechnological methods and synthesis. Examples of the recognition of validated core structures and synthesis of structurally simplified compounds retaining modes of activity are analyzed.
TL;DR: 3,5-Bromo-4-hydroxyphenyl derivatives of substituted pyrazinecarboxylic acid have shown the highest activity against Mycobacterium tuberculosis H(37)Rv (54-72% inhibition).
Abstract: Condensation of the corresponding chlorides of some substituted pyrazine-2-carboxylic acids (pyrazine-2-carboxylic acid, 6-chloropyrazine-2-carboxylic acid, 5- tert- butylpyrazine-2-carboxylic acid or 5- tert -butyl-6-chloropyrazine-2-carboxylic acid) with various ring-substituted aminothiazoles or anilines yielded a series of amides. The syntheses, analytical and spectroscopic data of thirty newly prepared compounds are presented. Structure-activity relationships between the chemical structures and the anti-mycobacterial, antifungal and photosynthesis-inhibiting activity of the evaluated compounds are discussed. 3,5-Bromo-4-hydroxyphenyl derivatives of substituted pyrazinecarboxylic acid, 16-18 , have shown the highest activity against Mycobacterium tuberculosis H 37 Rv (54-72% inhibition). The highest antifungal effect against Trichophyton mentagrophytes , the most susceptible fungal strain tested, was found for 5- tert- butyl-6-chloro- N -(4-methyl-1,3-thiazol-2-yl)pyrazine-2-carboxamide (
TL;DR: L-proline catalyzed additions of 13 different thiols to 11 different alpha-enone Michael acceptors in [bmim] PF(6 ) are reported.
Abstract: L-proline catalyzed additions of 13 different thiols to 11 different alpha-enone Michael acceptors in [bmim] PF(6 )are reported. Reasonable to high yields of the reaction products were isolated in most cases.
TL;DR: New cis monocyclic beta-lactams were synthesized by [2+2] Staudinger cycloaddition reactions of the imine (3,4-dimethoxybenzylidene)-(4-methoxyphenyl)-amine and ketenes derived from different acyl chlorides and Et3N.
Abstract: — New cis monocyclic β-lactams were synthesized by [2+2] Staudinger cycloaddition reactions of the imine (3,4-dimethoxybenzylidene)-(4-methoxyphenyl)- amine and ketenes derived from different acyl chlorides and Et 3 N. These monocyclic β-lactams were then cleaved by ceric ammonium nitrate (CAN) to give NH-monocyclic β-lactams, which in turn were converted to N -sulfonyl monocyclic β-lactams by treatment with four different sulfonyl chlorides in the presence of Et 3 N and 4,4-dimethyl-aminopyridine (DMAP). Keywords: 2-Azetidinones, N-Sulfonyl β-lactams, Ketene, Imine, CAN, DMAP Introduction Even more than 70 years after the discovery of penicillin, β-lactam antibiotics remain as one of the most important contributions of science to Humanity [1]. The β-lactam skeleton is the common structural element of the widely used penicillins, cephalosporins, thienamycine, nocardicins, aztreonam and carumonam [2]. The first member of this class of compounds was synthesized by Staudinger in 1907 [3], but until the discovery of penicillin by Fleming in 1929, the importance of β-lactams as antibiotics was not recognized [4]. Widespread use of β-lactam antibiotics exerts selective pressure on bacteria and permits the proliferation of resistant organisms [5]. A comparison of current antibiograms with those from previous decades shows an alarming increase in bacterial resistance to
TL;DR: 3,5-Disubstituted hydantoin (1,3-imidazolidinedione) derivatives 5a-h were prepared by base induced cyclization of the corresponding N-(1-benzotriazolecarbonyl)-L- and D-amino acid amides 4 a-h to evaluate their cytostatic and antiviral activities.
Abstract: 3,5-Disubstituted hydantoin (1,3-imidazolidinedione) derivatives 5a-h wereprepared by base induced cyclization of the corresponding N-(1-benzotriazolecarbonyl)-L-and D-amino acid amides 4a-h. Compounds 5a-h were evaluated for their cytostatic andantiviral activities. Among all the compounds evaluated, 3-benzhydryl-5-isopropylhydantoin (5a) showed a weak but selective inhibitory effect against vaccinia virus (EC50 =16 μg/mL; selectivity index: 25). 3-Cyclohexyl-5-phenyl hydantoin (5g) showed inhibitoryactivity against cervical carcinoma (HeLa, IC50 = 5.4 μM) and breast carcinoma (MCF-7,IC50 = 2 μM), but also cytotoxic effects towards human normal fibroblasts (WI 38). On thecontrary, the 3-benzhydryl-5-phenyl substituted hydantoin derivative 5h showed moderateinhibitory activity towards HeLa, MCF-7, pancreatic carcinoma (MiaPaCa-2), lungcarcinoma (H 460) and colon carcinoma (SW 620) (IC50 = 20−23 μM), but no effect on WI38.
TL;DR: Morphological observations and cell cycle analysis suggest that these compounds inhibit the proliferation of hepatoma by inducing apoptosis and consequently kalopanaxsaponins A and I may be potential therapeutic agents for the treatment of parental and drug resistant hepatoma.
Abstract: During an investigation of antitumor substances from Nigella glandulifera Freyn et Sint. (Ranunculaceae) the cytotoxicity of two oleanane triterpene saponins isolated from the seeds of this species, kalopanaxsaponins A and I, was evaluated against HepG2, drug resistant HepG2 (R-HepG2) (two hepatocyte cell lines) and primary cultured normal mouse hepatocytes. Evident cytotoxic activities were observed. Morphological observations and cell cycle analysis suggest that these compounds inhibit the proliferation of hepatoma by inducing apoptosis and consequently kalopanaxsaponins A and I may be potential therapeutic agents for the treatment of parental and drug resistant hepatoma.
TL;DR: If the esterification was performed in toluene under azeotropic reflux conditions to remove water, both the catalytic activity of ZrOCl x 8H(2)O and the rate of esters could be increased greatly and in the present catalytic system, the esterscould be easily separated from the reaction mixtures and the catalyst could be easily recovered and reused.
Abstract: Esterifications of carboxylic acids with equimolar amount of alcohols could beefficiently catalyzed by ZrOCl2·8H2O. Acrylate esters were obtained in good yields undersolvent-free conditions at ambient temperature. The esterification of other carboxylicacids with alcohols also proceeded at ambient temperature or at 50 oC to afford esters inhigh yields. If the esterification was performed in toluene under azeotropic refluxconditions to remove water, both the catalytic activity of ZrOCl2·8H2O and the rate ofesterification could be increased greatly. Furthermore, in the present catalytic system, theesters could be easily separated from the reaction mixtures and the catalyst could beeasily recovered and reused.
TL;DR: Title compound 6-bromo-3-propylquinazolin-4-one (3h) was found to possess good antifungal activity.
Abstract: : A simple, efficient, and general method has been developed for the synthesis of various 3-alkylquinazolin-4-one derivatives from quinazolin-4-one treated with alkyl bromides under phase transfer catalysis condition. The structures of the compounds were characterized by elemental analysis, IR, 1 H-NMR and 13 C-NMR spectra. Title compound 6-bromo-3-propylquinazolin-4-one ( 3h ) was found to possess good antifungal activity. Keywords: Quinazolinone, Phase Transfer Catalyst, synthesis, antifungal activity Introduction A variety of the reports regarding synthetic studies of quinazolinone derivatives have been presented due to the chemical and biological interests to the quinazoline [1, 2]. Quinazoline compounds are widely used in agrochemicals as plant virucides [3], antifungal agents [4] and herbicides [5]. According to recent data, quinazoline nucleus has attracted the attention of medicinal chemists due to its well known anticancer activity, and many substituted quinazoline derivatives have recently earned great interest in chemotherapy as antitumor drugs [6, 7]. In order to find potential new plant fungicides and anticancer agents, we had designed and synthesized a series of
TL;DR: Cerium(III) nitrate hexahydrate efficiently catalyzes the three-component Biginelli reaction under solvent-free conditions of an aldehyde, a beta-keto ester or beta-diketone and urea or thiourea to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones or -thiones in excellent yields.
Abstract: Cerium(III) nitrate hexahydrate efficiently catalyzes the three-component Biginelli reaction under solvent-free conditions of an aldehyde, a beta-keto ester or beta-diketone and urea or thiourea to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones or -thiones in excellent yields.
TL;DR: A. trifida essential oil demonstrated bactericidal and fungicidal activity against six bacterial strains and two fungal strains, using the agar diffusion method.
Abstract: The essential oil obtained by steam distillation of dried aerial parts of Ambrosia trifida L. from Northeast China was analyzed by GC and GC–MS. The essential oil yield based on dried plant material was 0.12% and thirty-five compounds (corresponding to 86.7% of the total weight) were identified. The main components were: bornyl acetate (15.5%), borneol (8.5%), caryophyllene oxide (8.3%), α-pinene (8.0%), germacrene D (6.3%), β-caryophyllene (4.6%), trans-carveol (2.9%), β-myrcene (2.6%), camphor (2.4%) and limonene (3.2%). A. trifida essential oil demonstrated bactericidal and fungicidal activity against six bacterial strains and two fungal strains, using the agar diffusion method.
TL;DR: Ten new 2-(3-aryl-1-phenyl-4-pyrazolyl)benzoxazoles have been synthesized by oxidative intramolecular cyclization of the corresponding Schiff's bases using iodobenzene diacetate in methanol as an oxidant.
Abstract: Ten new 2-(3-aryl-1-phenyl-4-pyrazolyl)benzoxazoles have been synthesized by oxidative intramolecular cyclization of the corresponding Schiff's bases using iodobenzene diacetate in methanol as an oxidant.
TL;DR: A rapid and easy solvent free one-pot synthesis of 5-arylidene-2-imino-4-thiazolidinones by condensation of the thioureas with chloroacetic acid and an aldehyde under microwave-irradiation is described.
Abstract: A rapid and easy solvent free one-pot synthesis of 5-arylidene-2-imino-4- thiazolidinones by condensation of the thioureas with chloroacetic acid and an aldehyde under microwave-irradiation is described.
TL;DR: The reactivity of compound 3 towards dimethylformamide dimethyl acetal (DMF-DMA), carbon disulfide, urea, thiourea, formamide, formic acid, acetyl chloride and isothiocyanate were studied and the antimicrobial activity of some selected derivatives is reported.
Abstract: 2–Amino–4-phenyl–5,6,7,8–tetrahydroquinoline–3–carbonitrile ( 3 ) was synthesized by treating cyclohexanone ( 1 ) with 2–benzylidenemalononitrile ( 2 ) in the presence of ammonium acetate. The reactivity of compound 3 towards dimethylformamide dimethyl acetal (DMF-DMA), carbon disulfide, urea, thiourea, formamide, formic acid, acetyl chloride and isothiocyanate were studied. In addition, the antimicrobial activity of some selected derivatives is reported. Keywords : Tetrahydroquinoline; pyrimidine; thioureide; pyrimidoquinoline; X-ray crystal structure. Introduction Pyrimidoquinolines are important compounds because of their biological properties, which are known to depend mainly on the nature and position of substituents, and include antimalarial [1], anticancer [2], antimicrobial [3, 4], and anti-inflammatory activities [5, 6]. Recently there has also been considerable interest in the synthesis and chemistry of tetrahydroquinolines and their fused derivatives [7-11]. Our aim in the work presented herein was to synthesize pyrimido[4,5-b]quinolines using tetrahydroqinolinecarbonitriles as building blocks. Such a synthesis of condensed azines is of biological interest due to the formal isoelectronic relationship that exists between the pyrimidine ring and tetrahydroquinoline [12-23].
TL;DR: Criteria for classification of systematic names in terms of quality/correctness are discussed and applied to a sample set of several hundred names extracted from the literature.
Abstract: This work deals with the use of organic systematic nomenclature in scientific literature, its quality, and computerized methods for its improvement. Criteria for classification of systematic names in terms of quality/correctness are discussed and applied to a sample set of several hundred names extracted from the literature. The same structures are named with three popular state-of-the-art nomenclature programs - AutoNom 2000, ChemDraw 10.0, and ACD/Name 9.0. When comparing the results, all nomenclature tools show a significantly better performance than 'average chemists'. One program allows the generation not only of IUPAC names but also of CAS-like index names that are compared with the officially registered names. The scope and limitations of nomenclature software are discussed and a comparison of the programs' actual capabilities is given.
TL;DR: Thioxothienopyrimidinones, alkylthio- and arylalkylthiothienOPyrimid inones, thienop Skyrimidine, a thienotriazolo-pyrimidInones and aThienopyridines prepared from 2-amino-3-carboethoxy-4,5-disubstituted thiophenes via reactions with different reagents.
Abstract: Thioxothienopyrimidinones, alkylthio- and arylalkylthiothienopyrimidinones, thienopyrimidinones, thienopyrimidines a thienopyrimidinedione and a thienotriazolo- pyrimidinone were prepared from 2-amino-3-carboethoxy-4,5-disubstituted thiophenes and 2-amino-3-cyano-4,5-disubstituted thiophenes via reactions with different reagents.
TL;DR: Oxidation reactions of aliphatic and aromatic hydrocarbons were carried out in the presence of molecular oxygen at atmospheric pressure and epoxides or ketones were obtained as the main products with high selectivity.
Abstract: Polymer-supported heterogeneous catalysts in a form of complexes of 8-hydroxy- quinoline with cobalt acetate were synthesized. Conjugated polymers - polyaniline (PANI), poly-o-toluidine (POT), poly-o-anisidine (POA) - were used as supports. Oxidation reactions of aliphatic and aromatic hydrocarbons were carried out in the presence of molecular oxygen at atmospheric pressure and epoxides or ketones were obtained as the main products with high selectivity.
TL;DR: Volatile component profiles of the oils obtained by normal soil and semi-hydroponic cultivation were similar, whereas a quantitative difference was noted in some major volatiles when the cultivation system containing microbes was utilized.
Abstract: Roots of Vetiveria zizanioides Nash (Mae Hae; Thai ecotype) planted in three different cultivation systems (normal soil, normal soil with added microbes and semi- hydroponically) were extracted using a simultaneous steam distillation and solvent extraction (SDE) apparatus. Yields of the essential oils obtained were 0.27, 0.18 and 0.06%, respectively. The separation profiles obtained by comprehensive two-dimensional gas chromatography (GC×GC) and solid phase microextraction (SPME)-GC×GC analyses of the crude essential oils showed a total of 156 and 48 well-resolved components, respectively. The highly volatile fractions isolated from the three essential oils by SPME were subjected to analysis by GC-MS and 42 compounds were identified in total. Volatile component profiles of the oils obtained by normal soil and semi-hydroponic cultivation were similar, whereas a quantitative difference was noted in some major volatiles when the cultivation system containing microbes was utilized.
TL;DR: Water soluble hydrochloride salts of 6-amino-2-(substituted-phenyl)benzothiazole (13-19) were found to exert cytostatic activities against malignant human cell lines and normal human fibroblast cell lines.
Abstract: Novel derivatives of 6-amino-2-phenylbenzothiazole bearing different substituents (amino, dimethylamino or fluoro) on the phenyl ring were prepared as the corresponding hydrochloride salts. 6-Nitro-2-(substituted-phenyl)benzothiazoles (1-6) were synthesized by condensation reactions of substituted benzaldehydes with 2-amino-5-nitrothiophenol. Nitro derivatives were reduced to the amino derivatives with SnCl(2)/HCl. Water soluble hydrochloride salts of 6-amino-2-(substituted-phenyl)benzothiazole (13-19)were prepared using concentrated or gaseous HCl. Compounds 13-19 were found to exert cytostatic activities against malignant human cell lines: cervical (HeLa), breast (MCF-7),colon (CaCo-2), laryngeal carcinoma (Hep-2), and normal human fibroblast cell lines (WI-38).
TL;DR: Nine known and one new ent-kaurene diterpenoid were isolated from the acetone Extract of Sideritis stricta Boiss & Heldr and the whole crude acetone extract were evaluated against E. coli, S. aureus, K. pneumeonia and C. albicans.
Abstract: Nine known and one new ent-kaurene diterpenoid were isolated from the acetone extract of Sideritis stricta Boiss & Heldr. The new compound, identified as ent-1β-hydroxy-7α-acetyl-15β,16β-epoxykaurane (1) by IR, 1D and 2D NMR techniques and mass spectra, was isolated along with sideroxol (2), 7-acetyl sideroxol (3), 7-epicandicandiol (4), linearol (5), ent-7α,15β,18-trihydroxy-kaur-16-ene (6), ent-7α-acetyl,15,18-dihydroxy-kaur-16-ene (7), foliol (8), sideridiol (9) and siderol (10). The antibacterial and antifungal activities of these compounds and the whole crude acetone extract were evaluated against E. coli, S. aureus, K. pneumeonia and C. albicans.