Showing papers in "Bioorganic & Medicinal Chemistry in 2008"

TL;DR: Significant developments in the isolation of tetramic acids and tetronic acids, in the elucidation of their biosyntheses and their biological activities and in laboratory syntheses are reviewed with a focus on those derivatives with medicinal and pharmacological relevance.

TL;DR: Eight new compounds were found to have significant anti-inflammatory activity in the carrageenan induced rat paw oedema model, with significant analgesic activity inThe acetic acid induced writhing model with no ulcerogenicity and showed promising results in histopathology studies.

TL;DR: The antibacterial activity of 31 chalcones was tested against bacterial strains, Bacillus cereus ATCC 11778, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, and Staphylococcus aureus AT CC 25923.

TL;DR: Three new chlorinated benzophenone derivatives have been isolated from cultures of an isolate of the plant endophytic fungus Pestalotiopsis adusta, and compounds 1 and 2 displayed significant antifungal activities against three plant pathogens.

TL;DR: It can be suggested that the potentially effective 6,6'-bieckol might be employed as a drug candidate for development of new generation therapeutic agents against HIV.

TL;DR: A series of 10 new 5-[2-(substituted sulfamoyl)-4,5-dimethoxy-benzyl]-4aryl-s-triazole-3-thiones synthesized and evaluated for in vitro antifungal and antibacterial activity found that Gram (-) bacteria seem to be more sensitive to these compounds than Gram (+) species.

TL;DR: The SAR analysis of flavonoids on influenza virus NAs revealed that for good inhibitory effect, the 4'-OH, 7-OH, C4O, and C2C3 functionalities were essential, and the presence of a glycosylation group greatly reduced NA inhibition.

TL;DR: The antiviral evaluation of some selected new products showed that they have promising antiviral activity against hepatitis-A virus (HAV) and herpes simplex virus type-1 (HSV-1).

TL;DR: A general strategy for the synthesis of 3'-prenylated chalcones was established and a series of prenylated hydroxychalcones, including the hop secondary metabolites xanthohumol, revealed interesting synthetic possibilities for the development of more potent compounds.

TL;DR: The 'one pot' condensation reaction for the synthesis of phthalic imide derivative (benzothiazole containing phthalimide), exhibiting in vitro cytotoxic potential on human cancer cell lines and induced apoptosis on cancer cells is described.

TL;DR: The synthesis of pharmaceutically active compounds bearing a disubstituted piperidine framework is reviewed and the activity and/or usage of the same is briefly covered.

TL;DR: Some novel 1-methyl-4-(2-substitutedphenyl-1H-benzimidazol-1-yl)acetyl)thiosemicarbazides synthesized and tested for antioxidant properties by using various in vitro systems found to be a good scavenger of DPPH radical when compared to BHT.

TL;DR: Novel thiosemicarbazone derivatives clearly display stronger antiproliferative activity on five tumor cell lines than the reference compounds 3 and 4, which supports their further investigation as potential antitumor agents.

TL;DR: Molecular modeling experiments involving 12f and the colchicine binding site of alpha,beta-tubulin showed that the triazole moiety interacts with beta- Tubulin via hydrogen bonding with several amino acids.

TL;DR: The development of an mt-QSAR for more than 500 drugs tested in the literature against different parasites and the outputs of the QSAR are used to construct, by the first time, a multi-species Complex Networks of antiparasite drugs.

TL;DR: Some salicylic acid derivatives investigated here showed effective hCA I and II inhibitory activity, and might be used as leads for generating enzyme inhibitors eventually targeting other isoforms which have not been assayed yet for their interactions with such agents.

TL;DR: The bioassay results showed that title compound 10a possess high antifungal activities with EC(50) values ranging from 19.91 to 63.97 microg/mL, and the mechanism of action of 10a against Sclerotinia sclerotiorum was studied.

TL;DR: It is suggested that reactive oxygen species generation plays a critical role in dihydroxycoumarin-induced apoptosis in U-937 cells and may have a potential therapeutic role in the treatment of hematological malignancies.

TL;DR: It is indicated that UK-1 and analogs may exert their cytotoxic effects by interaction with Cu2+ or other transition metal ions, rather than Mg2+, and that metal ion-mediated DNA binding,rather than metal ion binding affinity, is important for the cytotoxicity effect of these compounds.

TL;DR: The structure and bioactivity of mucilage components are validated by further fractionation and this is the first study that provides clear evidence for the structure and activity relationship of the polysaccharide in D. huoshanense.

TL;DR: Several classes of flavonoids [flavanoids (1-10), flavonol (11, isoflavones (12-18), isoflavanones (19-22), chalcones (27-30), auronol (31), pterocarpans (32-37), 2-arylbenzofuran (38), and neoflavonoid (39)] and lignans (40-42) isolated from the MeOH extract of Brazilian red propolis were investigated for their cytotoxic activity against a panel of six

TL;DR: The MeOH soluble extract of Brazilian red propolis was found to kill 100% PANC-1 cells preferentially in the nutrient-deprived condition and study on the mode of cell death induced by DMPC indicated that killing process was not accompanied by DNA fragmentation, rather through a nonapoptotic pathway accompanied by necrotic-type morphological changes.

TL;DR: It is worth noting that the replacement of the thiazole nucleus for the benzo[d]thiazole bicyclic system in the parent 2-(benzylidene-2-ylimino)thiazolidin-4-one leads to significant antifungal properties against both yeasts and moulds, properties not shown by the analogous 2-thiazolyl- and 2-benzo[ d]isothiazoly l-imino-5-

TL;DR: Seven TGS-aptamers, designated as T7, T15, T19, T20, T22, T23, and T24, showed high affinity to the basic TET backbone, which is predicted to be essential for high affinity and group specificity.

TL;DR: A series of novel, fluorescent ligands designed to bind with high affinity and specificity to the asialoglycoprotein receptor (ASGP-R) has been synthesized and tested on human liver cells and showed the process to be receptor-mediated and selective.

TL;DR: A series of competitive inhibitors were optimized from oleanolic acid, a natural triterpenoid identified against PTP1B by screening libraries of traditional Chinese medicinal herbs, which exhibited good selectivity between other phosphatases involved in insulin pathway except T-cell protein tyrosine phosphatase.

TL;DR: Curcumin analogues described here represent a novel class of highly selective P. falciparum inhibitors and promising candidates for the design of novel anti-malarial agents.

TL;DR: No clear correlation was observed between the antiepileptic activity and molecular lipophilicity descriptors of the tested compounds, and some selected compounds were assayed against seizures induced by pentylenetetrazole and strychnine in mice.

TL;DR: Two series of pyrazole derivatives were synthesized by parallel solution-phase synthesis and were assayed as inhibitors of Mycobacterium tuberculosis and showed high activity against MTB.

TL;DR: The results indicated that the aptamers No. 4, 5, and 20 with variable 40-base oligonucleotides can be good candidates for selectively binding to OTC with high molecular discrimination over its analogs such as tetracycline and doxycycline.