Nilay Shah, P. N. Patel, Denish C. Karia
2018
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Influential Citations
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Journal
Asian Journal of Chemistry
Abstract
Amino pyrazole and their derivatives for their biological activities. Present work describes the synthesis of novel amino pyrazole derivatives and evaluation of their medicinal value. The reaction of 3,5- bis (trifluoromethyl) aniline with cyano acetic acid in presence of ethylene dichloride-hydrochloride produced N-[3,5- bis (trifluoromethyl)phenyl]-2-cyanoacetamide (1) ; this intermediate, upon further reaction with dimethyl sulfide in presence of K 2 CO 3 followed by reaction with methyl iodide was converted to N-[3,5- bis (trifluoromethyl)phenyl]-2-cyano-3,3- bis (methylthio)acrylamide (2) . The cyclization of 2 with hydrazine in isopropyl alcohol resulted in 3-amino-N-[3,5-bis (trifluoromethyl)phenyl]-5-(methylthio)-1 H -pyrazole-4-carboxamide (3) as main scaffold. This isolated scaffold finally reacted with various derivatives of aldehyde followed by reduction with sodium borohydride to isolate target compounds AP-1 to AP-17 . The structures of the synthesized compounds were confirmed by mass, FT-IR and 1 H NMR analysis. All the compounds were tested for potential antifungal and antimicrobial activity. Out of 17 compounds AP-1, 3, 4, 7, 9, 10 and 11 compounds having good activity in antimicrobial agent.