Organic Communications Articles

A series of new carboxamide derivatives of celecoxib, 4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide 1 were synthesized by the reaction of 3-(4-(3-(trifluoromethyl)-5-p-tolyl-1H-pyrazol-1-yl)phenylsulfonylamino)propanoic acid 2 with various bio-potent amines by using 1-methylimidazole as a base via. Schotten-Baumann reaction. The acid 2, which inturn prepared from 1 bytreatingwith3-bromopropanoic acid in the presence of sodium hydride. The newly synthesized compounds were characterized by IR, NMR and mass spectral analysis. The title molecules were evaluated for their efficacy as antimicrobial and antioxidant agents in vitro. Compounds 4(c-g) showed high growth inhibitory activity against both bacteria and fungi. The compounds 4c and 4f exhibited promising antioxidant activity .

Novel 2-(1,5-bis(aryl)penta-1,4-dien-2-yl)benzo[d]thiazol (5a,b) and 2-(((1S,2S,E)-2-(benzo[d]thiazol-2-yl)-1,5-di-arylpent-4-en-1-yl)thio)aniline (6a,b) derivatives were obtained by addition of 2-aminobenzothiol to bis-benzylidinecyclobutanones (3a,b). The structures of the obtained compounds were characterized using the spectroscopic methods (NMR, IR, Elemental Analysis). Compounds 5a,b showed cytotoxic activities against C6 (Rat Brain tumor cells) and HeLa (human uterus carcinoma) in vitro.