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  • 03월 04일 13시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

Discovery of (4-Cyanobenzo[b]thiophene-2-carbonyl)guanidine methanesulfonate (KR-33028) , a Novel Na+/H+ Exchanger isoform 1 (NHE-1) Inhibitor as a Putative Cardioprotective Agent

등록일
2005년 2월 17일 15시 53분 01초
접수번호
0998
발표코드
토25I5구 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
토 10시 : 30분
발표형식
구두발표
발표분야
의약화학
저자 및
공동저자
이현숙, 이선경, 이규양
한국화학연구원 심장순환계 연구팀,
From our efforts to find a novel NHE-1 inhibitor based on bicyclic template, we found that (benzo[b]thiophene-2-carbonyl)guanidines with 4-substituent including halogen, nitrile, nitro, alkyl, and aryl groups showed good NHE-1 inhibitiory activity which was well translated into the cardioprotective efficacy. Especially the 4-cyano compound (KR-33028) excellently improved cardiac function in isolated rat heart ischemia model, and markedly reduced infarct size in the in vivo rat myocardial infarction model as well as strong inhibition on NHE-1. The nitrile function was introduced by microwave-promoted nucleophilic substitution using CuCN in DMF from 4-bromobenzothiophene-2-carboxylic ester in 20 minutes. The final acylguanidine was prepared by treating the ester with excess guanidine in DMF, purified by crystallization as a methanesulfonic acid salt.

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