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 derivative...
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https://www.riss.kr/link?id=O118980121
Zi‐Li Ren ; Hao Liu ; Di Jiao ; Hao‐Tian Hu ; Wei Wang ; Jie‐Xiu Gong ; Ai‐Li Wang ; Hai‐Qun Cao ; Xian‐Hai Lv
2018년
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0272-4391
1098-2299
SCI;SCIE;SCOPUS
학술저널
307-312 [※수록면이 p5 이하이면, Review, Columns, Editor's Note, Abstract 등일 경우가 있습니다.]
0
상세조회0
다운로드다국어 초록 (Multilingual 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 derivative...
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 IC50 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.
Cover image, volume 79, issue 6