A few series of indole derivatives were screened for antimicrobial, antifungal and anti-HBV activities. The compounds were tested for their in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and for their antifungal activity against Candida albicans using a disc diffusion method, which measures the diameter of the inhibition zone around a paper di...

Pyridobenzimidazoles 6a-iwere synthesized in very good to excellent yields (81-96%) by the condensation of substituted N-phenyl-o-phenylenediamines 4a-d with indole/benzo[b]thiophene-3-aldehydes 5a-t inmethoxyethanol under reflux conditions. The diamines 4a-d were prepared byfirst treating 2-chloro-3-nitropyridine (1)with suitably substituted anilines 2a-d then reducing the resulting3-nitro-N-p...

The synthesis of new meridianin derivatives substituted at the C-5 position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. These compounds were tested for their kinase inhibitory potencies toward five kinases (CDK5/p25, CK1delta/epsilon, GSK-3alpha/beta, Dyrk1A and Erk2) as well as their in vitro antiproliferati...

Present work describes the Synthesis of 3-(3-substituted-1H-indon-1-yl)-2-phenylquinoline-4carboxylic acid derivatives by Pfitzinger reaction of isatin with 2(1H-indol-1-yl)-1-phenyl ethanone and 1-phenyl-2-[-3-(substituted)-1-H-indole-1-yl] ethanone. The structures of all the compounds are established by elemental analysis, IR, H NMR and Mass spectral data. These compounds possess excellent an...

1,2,3,4-Tetrahydro-β-carbolines (THβCs) are a pharmacologically important group of compounds belonging to the indole alkaloids. C1-Substituted optically active THβCs have been the target of extensive synthetic efforts due to the presence of the scaffold in numerous natural products and synthetic targets. This review briefly summarizes the methods to obtain the C1 stereocenter and concentrates o...

Purpose: The article is aimed to synthesize,characterize and screening the biological activity of a series of Synthesis of 1-(2-(3-(3-chloro-1-(4-substituted phenyl)-4-tetrazole-2-yl)-1H-indol-1-yl)acetyl)-4-(2-(4substituted phenyl)hydrazono)-3-(trifluoromethyl)-1H-pyrazol-5(4H)-one 4(a-f). Indole-3-carbaldehyde and chloro ethyl acetate were dissolved in DMF. To this reaction mixture anhydrous ...

Indole is a benzopyrrole in which the benzene and pyrrole rings are fused through the 2-and 3-positions of the pyrrole nucleus. The indole derivatives are very much used as anticonvulsant agents. In the same context, several indole derivatives were prepared by the reaction between indole-3carboxaldehyde and various p-substituted phenylsemicarbazides, in the presence of glacial acetic acid. The ...

A straightforward and atom-economical method is described for the synthesis of 2,3-disubstituted indoles. Anilines and 1,2-diols are condensed under neat conditions with catalytic amounts of either [Cp*IrCl(2)](2)/MsOH or RuCl(3)·xH(2)O/phosphine (phosphine = PPh(3) or xantphos). The reaction does not require any stoichiometric additives and only produces water and dihydrogen as byproducts. Ani...

An efficient and economical method was developed for the synthesis of 3-substituted indoles by one-pot three-component coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or N-methylindole using Yb(OTf)(3)-SiO(2) as a catalyst. All the synthesized compounds were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovari...

An efficient strategy for the synthesis of asymmetrically substituted enediynes fused to benzothiophene, benzofuran, and indole was developed. The proposed approach is based on the electrophilic cyclization of diacetylenes and Sonogashira coupling. Thus, iodocyclization of readily available ortho-functionalized (buta-1,3-diynyl)arenes was used as a direct way for the synthesis of 2-ethynyl-3-io...