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HERO ID
9087681
Reference Type
Journal Article
Title
Synthesis characterization and biological evaluation of some novel amino pyrazole derivatives
Author(s)
Shah, N; Patel, PN; Karia, DC
Year
2018
Is Peer Reviewed?
Yes
Journal
Asian Journal of Chemistry
ISSN:
0970-7077
EISSN:
0975-427X
Volume
30
Issue
12
Page Numbers
2647-2651
Language
English
DOI
10.14233/ajchem.2018.21499
URL
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85055995326&doi=10.14233%2fajchem.2018.21499&partnerID=40&md5=ee5253dce9ba164243fa0102f75e0c33
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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 K2CO3 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)-1H-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 1H 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. © 2018 Chemical Publishing Co. All rights reserved.
Keywords
Amine derivatives; Antifungal activity.; Antimicrobial; Carboxamide derivatives; Pyrazole
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