In:
Drug Development Research, Wiley, Vol. 79, No. 6 ( 2018-09), p. 307-312
Abstract:
Hit, Lead & Candidate Discovery To discover succinate dehydrogenase inhibitors with a novel structure, we introduced cinnamic acid structure to optimize the lead structure 1 and synthesized four series of cinnamon–pyrazole carboxamide derivatives. The bioassay data showed that compounds (E)‐N‐(1‐[4‐chlorophenyl]‐4‐cyano‐1H‐pyrazol‐5‐yl)‐3‐(2‐fluorophenyl) acrylamide ( 5III‐d) and (E)‐3‐(2‐chlorophenyl)‐N‐(1‐[4‐chlorophenyl]‐4‐cyano‐1H‐pyrazol‐5‐yl) acrylamide ( 5III‐f) showed the significant antifungal activity against three fungi. In addition, 5III‐d and 5III‐f exhibited the excellent inhibitory effect against succinate dehydrogenase (SDH) enzymes with IC 50 values ranging from 19.4 to 28.7 μM. The study demonstrates that the chlorine substituent group is present on both the phenyl and pyrazole rings that have a very good effect on the antifungal effect, and the compounds 5III‐d and 5III‐f can act as potential SDH inhibitors (SDHI) and throw a sprat for a new generation of SDHI.
Type of Medium:
Online Resource
ISSN:
0272-4391
,
1098-2299
Language:
English
Publisher:
Wiley
Publication Date:
2018
detail.hit.zdb_id:
1500191-X
SSG:
15,3
