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An efficient single-pot strategy for 2-amino nicotinonitrile derivatives 5 has been developed by multi-component reaction of arylaldehydes 1, methylketones 2, malononitrile 3, and ammonium acetate 4 using tetrabutyl ammonium bromide as catalyst in aqueous medium. [ABSTRACT FROM AUTHOR]

A series of novel substituted 4-trifluoromethyl-pyridin-2-yl hydrazide derivatives 5 and 7-trifluoromethyl-1,2,4-triazolo[4,3-a]pyridine derivatives 6 were synthesized through a facile method in single step from 2-hydrazino-pyridine derivatives 4 and their reaction with aliphatic/aromatic acids in the presence of POCl3 and PCl5. In each reaction, an 5 and product 6 were formed in definite proportion except in 5a, 5d, and 6e and were independent of reaction time and temperature. [ABSTRACT FROM AUTHOR]

The 3-amino-6-(trifluoromethyl)furo[2,3- b]pyridine-2-carbohydrazide ( 5) was prepared from 3-cyano-6-trifluoromethyl-2(1 H)pyridone ( 2) in series of steps via selective , followed by reaction with hydrazine hydrate. The 2-carbohydrazide ( 5) was further reacted with aliphatic acids under different reaction temperatures to form a series of novel N-acylfuro[2,3- b]pyridine-2-carbohydrazide ( 6) and pyrido[3′,2′:4,5]furo[3,2- d]pyrimidine derivatives ( 7). All the compounds 6 and 7 were screened for cytotoxic activity against breast carcinoma MD Anderson-Metastatic Breast (MDA-MB) 231 (aggressive) cell lines at 10 µM concentration. Compounds 6a, 6b, and 6c showed promising activity. [ABSTRACT FROM AUTHOR]

A facile and an efficient protocol has been developed for the synthesis of novel 1,2,3-triazole substituted 4 H-chromene derivatives 4 in single pot by of 1,3-cyclohexanedione, malononitrile and 1-substituted 1,2,3-triazole-5-aldehyde using potassium carbonate as catalyst. [ABSTRACT FROM AUTHOR]

A series of novel pyrido[3,2-e]tetrazolo[1,5-c]pyrimidine derivative 4 were synthesized starting from 2-amino-4-trifluoromethyl-6-phenyl nicotinonitrile 1 via construction of tetrazole followed by fusion of pyrimidine ring. All final products were screened for antibacterial and antifungal activities. [ABSTRACT FROM AUTHOR]

The article offers information on the multi component reactions for the synthesis of pyranopyrazole derivatives. It discusses several facts which include their applications as pharmaceutical ingredients and bio-degradable agrochemicals, their properties as analgesics, anti-cancer, anti-microbial and anti-inflammatory activity and initial formation of the pyrazolinone ring followed by condensation with benzylidenemalononitrile.

A series of novel 1,2,3-thiadiazolo-5-carboxylic acid hydrazide Schiff's bases 4a- 4r were prepared starting from ethyl-4,4,4-trifluoroacetoacetate and ethyl carbazate in four steps. All the compounds were screened for antibacterial activity against various bacterial strains at 150 μg/ml concentration and found no activity. Similarly, all the compounds were screened for antifungal activity against various fungal strains at 100 and 150 μg/ml concentrations. Compounds 4a, 4m, and 4q found to show moderate activity against Candida albicans. Further, compounds were evaluated for cytotoxic activity against breast carcinoma cells MDA-MB 231 (aggressive), MCF-7 (non-aggressive) using doxorubicin as standard. Compound 4n was found to show 25.39 % cell viability against MDA-MB 231 and 63.60 % cell viability against MCF-7 cells. [ABSTRACT FROM AUTHOR]

The three component Grieco condensation of indazoles, aliphatic/aromatic aldehydes, and electron rich olefins in the presence of GdCl resulted in a novel pyrimidine fused indazoles in single pot under mild conditions. Representative examples were screened for in vitro anti-cancer activity and some of the compounds exhibited promising cytotoxic activity against U937 cell lines in comparable with standard drug etoposide. The data were further compared with structure-based investigations using docking studies with the crystal structure of Rho-kinase (2F2U) protein. The fitness values estimated by genetic algorithm were found to have a good correlation with the experimental inhibitory potencies. [ABSTRACT FROM AUTHOR]

A series of novel naphthyridine derivatives 3 and 4 was prepared from substituted pyridine 2 and ketones using ZnCl as catalyst under microwave irradiation conditions. All the compounds were evaluated for AChE inhibitory activity and promising compounds 3d, 3e, 4b, and 4g was identified. Representative compounds 3d and 3e were found to show insignificant THLE-2 liver cell viability/toxicity. The binding mode between X-ray crystal structure of human AChE and compounds was studied using molecular docking method and fitness scores were found to be in good correlation with the activity data. [ABSTRACT FROM AUTHOR]

A simple and facile strategy for the synthesis of highly substituted imidazoles has been developed by multi-component condensation of 1,2-diketone, aldehyde, amine, and ammonium acetate in presence of tetrabutyl ammonium bromide as catalyst. [ABSTRACT FROM AUTHOR]