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Synthesis and Biological Evaluation of (2-Aryl-4-methylimidazol-5-ylcarbonyl)guanidine Analogs as Potential Na+/H+ Exchanger Isoform 1(NHE-1) Inhibitors

등록일
2005년 2월 17일 15시 42분 34초
접수번호
0985
발표코드
25P260포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
토 <발표Ⅲ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
유현지, 이선경, 이규양, 서지희
한국화학연구원 심장순환계연구팀,
A series of (2-aryl-4-methylimidazol-5-ylcarbonyl)guanidines were synthesized as the potential NHE-1 inhibitors. Bromination of ethyl 4-methylimidazole-5-carboxylate using NBS regioselectively gave the 2-bromoimidazole compound, where the various aryl groups were introduced by the Suzuki-coupling reaction. The acylguanidines were obtained by treating with excess guanidine from the carboxylic esters. Both the Suzuki coupling and the reaction with guanidine were facilitated through the protection of imidazole amine with ethylvinyl ether. Finally the deprotection of ethylvinyl ether group using methanesufonic acid, following purification by crystallization yielded the methanesulfonic acid salt of acylguanidine. The NHE-1 inhibitory activity of synthesized compounds was determined using NHE-1 overexpressed PS120 variant cells.

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