Synthesis, characterization, pharmacological and computational studies of 4, 5, 6, 7-tetrahydro-1, 3-benzothiazole incorporated azo dyes

This article presents the results of spectroscopic studies of two compounds from the 1,3,4-thiadiazole group, that is, 4-(5-methyl-1,3,4-thiadiazole-2-yl)benzene-1,3-diol (C1) and 4-(5-heptyl-1,3,4-thiadiazole-2-yl)benzene-1,3-diol (C7), present at different molar concentrations in 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) liposome systems In the case of both investigated compounds, fluorescence measurements revealed the presence of several emission bands, whose appearance is related to the molecular organization induced by changes in the phase transition in DPPC On the basis of the interpretation of Fourier transform infrared spectra, we determined the molecular organization of the analyzed compounds in multilayers formed from DPPC and the 1,3,4-thiadiazoles It was found that the compound with a longer alkyl substituent both occupied the lipid polar head region in the lipid multilayer and interacted with lipid hydrocarbon chains In turn, the compound with a shorter alkyl substituent int

Molecular Organization of Dipalmitoylphosphatidylcholine Bilayers Containing Bioactive Compounds 4-(5-Heptyl-1,3,4-thiadiazol-2-yl) Benzene-1,3-diol and 4-(5-Methyl-1,3,4-thiadiazol-2-yl) Benzene-1,3-diols

Schiff Bases of 5 - (2 - phenoxypyridin - 3 - yl) - 1, 3, 4 - thiadiazol - 2 - amine derivatives 6 (a - h ) have been synthesized with different aromatic aldehyde and tested for in vitro anticancer activity; th e 1, 3, 4 - thiadiazole derivatives were prepared by the reaction of thiosemicarbazide, phosphorousoxy chloride and aromatic acids. The synthesized final Schiff base compounds were purified by column - chromatography and t he structures of the titled Schiff bases were elucidated by IR, 1 H NMR and LCMS spectral measurements. Three different cell lines namely Hela, Hep - G2 and MCF7 are used for the present study. The compounds tested were, in m ost of cases shows cytotoxic effect but, only one compound showed good act ivity on breast carcinoma cell line having IC 50 = 2 .28 μg/ mL.

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Synthesis, characterisation and anticancer activity of schiff base derivatives of 5 - (2 - phenoxypyridin - 3 - yl) - 1, 3, 4 - thiadiazol - 2 - amine

The search for new antimicrobials is imperative due to the emergent resistance of new microorganism strains. In this context, revisiting known classes like 8-hydroxyquinolines could be an interesting strategy to discover new agents. The 8-hydroxyquinoline derivatives nitroxoline and clioquinol are used to treat microbial infections; however, these drugs are underused, being available in few countries or limited to topical use. After years of few advances, in the last two decades, the potent activity of clioquinol and nitroxoline against several targets and the privileged structure of 8-hydroxyquinoline nucleus have prompted an increased interest in the design of novel antimicrobial, anticancer, and anti-Alzheimer agents based on this class. Herein, we discuss the current development and antimicrobial structure-activity relationships of this class in the perspective of using the 8-hydroxyquinoline nucleus for the search for novel antimicrobial agents. Furthermore, the most investigated molecular targets concerning 8-hydroxyquinoline derivatives are explored in the final section.

Novel Antimicrobial 8-Hydroxyquinoline-Based Agents: Current Development, Structure-Activity Relationships, and Perspectives.

Oxidative stress may link to psychiatric disorders, and is being regarded as a plausible mechanism that can affect the regulation of these illnesses. The present study was undertaken to investigate the antidepressant and anxiolytic potential of A. hydaspica R. parkers. Brain oxidative stress enzyme levels were analyzed to correlate depression and stress with brain antioxidant status. Antidepressant and anxiolytic effect of methanol extract of A. hydaspica and its derived soluble fractions [n-hexane (AHH), ethyl-acetate (AHE), chloroform (AHC), n-butanol (AHB) and remaining aqueous fraction (AHA)] was investigated by using three behavioral models; the Forced swimming test, Tail suspension test and Elevated plus-maze test (EPM). Chronic unpredictable mild stress (CMS) was employed to induce stress in rats. AHM and AHE (200 mg/kg, p.o), fluoxetine (5 mg/kg, i.p) and diazepam (DZM) (1 mg/kg, p.o) were administered during the 7 day stress exposure period, and rats were assessed for antidepressant and anxiolytic behavioral despair paradigms. Antioxidant enzymes and oxidative stress markers were measured in brain tissue of depressed rats. Phytochemical analysis was done by GCMS experimentation. AHM and AHE (acute dose) significantly (p < 0.0001) reduced the immobility time and ameliorated climbing behavior as compared to the control in FST and TST, and similar to fluoxetine. AHM and AHE showed significant (p < 0.0001) anxiolytic potential in EPM, and comparable to DZM (1 mg/kg b.w., i.p). Significant decrease in antioxidant enzyme levels and increase in MDA, H2O2 and NO level were observed in stressed rats. AHM and AHE (for 7 days/CMS) significantly improved behavior in FST, TST and EPMT. Treatment also improved antioxidant enzyme level and controlled the oxidative stress markers in brain tissues. GCMS analysis indicated the presence of 10 different chemical constituents in A. hydaspica. The present study revealed that A. hydaspica exerts an antidepressant and anxiolytic effect by improving brain antioxidant status. The observed activities might be due to the presence of diverse phytochemicals.

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Anti-depressant and anxiolytic potential of Acacia hydaspica R. Parker aerial parts extract: Modulation of brain antioxidant enzyme status

5-Phenyl-1,3,4-thiadiazole-2-amine has been synthesized by single step reaction. A series of heterocyclic azodyes were synthesized by diazotisation of 5-phenyl-1,3,4-thiadiazole-2-amine by nitrosyl sulphuric acid followed by coupling with different coupling compounds such as 8-hydroxyquinoline, 2,6-diaminopyridine, 2-naphthol, N,N-dimethyl aniline, resorcinol, and 4,6-dihydroxypyrimidine. The dyes were characterized by UV-Vis, IR, 1H-NMR, 13C NMR, and elemental analysis. The synthesized compounds were also screened for biological activity.

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Chinnagiri T. Keerthi Kumar

Papers

Synthesis, Characterization, and Biological Activity of 5-Phenyl-1,3,4-thiadiazole-2-amine Incorporated Azo Dye Derivatives