Mannich bases are generally formed by the reaction between formaldehyde, a secondary amine and a compound containing reactive hydrogen atoms. They display varied biological activities such as antimicrobial [1], cytotoxic [2,3], anticancer [2], analgesic [4], anti-inflammatory [5] and anticonvulsant [6] and DNA topoisomerase I inhibiting activities [3]. In this study, it was planned to synthesiz...

A valuable pharmacophore, the 2-aminoimidazole moiety, can be accessed with a variety of substitution patterns through an addition-hydroamination-isomerization sequence (see scheme; R(1),R(4),R(5)=alkyl; R(3)=alkyl, aryl; R(2)=H, alkyl, aryl). The synthesis of the propargyl cyanamide precursors through a three-component coupling enables the preparation of this important heterocyclic core struct...

The addition of heteroaryllithium to various ketones followed by dehydration gave 1-(2-heteroaryl)cycloalkenes and (2-hetero- aryl)alkenes. When alkenes were treated with 10 mol% NIS, calix[4]thiophenes and calix[4]furans were obtained in good yields.

A new series of 6-(aryl/heteryl)-3-(5-methyl-1-phenyl-1H-4-pyrazolyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (7a-j) has been synthesized by the reaction of 4-amino-5-(5-methyl-1-phenyl-1H-4-pyrazolyl)-4H-1,2,4-triazol-3-yl-hydrosulfide (6) with POCl(3) and the corresponding aryl/heteryl carboxylic acid, in ethanol at reflux temperature for 12 h. All the synthesized compounds were tested for i...

A series of novel pyrazoline derivatives 5-(substituted aryl)-3-(3,4-dimethoxyphenyl)-1-(2,4dinitrophenyl)-4,5-dihydro-1H-pyrazole (5a-l) were synthesized by heating 2,4-dinitrophenyl hydrazine (4) with (E)-3-(3,4-dimethoxyphenyl)-1-substituted aryl prop-2-en-1-one (3) in presence of catalytic amount of concentrated H2SO4. The structures of the novel derivatives were confirmed by various spectr...

Preliminary examination for the structure-activity relationship of quinone monooxime derivatives on cytotoxicity against HeLa S3 cell and further trials using eight different cell lines suggested that 2-aryl-6,7-methylenedioxy-1,4-naphthoquinone-1-oxime methyl ethers, carrying 2-methoxy-4,5-methylenedioxyphenyl, 7-methoxy-2-methylbenzofuran-4-yl, and 2-methoxycarbonyl-3,4-dimethoxyphenyl as the...