7-엑소메칠렌 세팔로스포라네이트 유도체의 합성과 beta-락타메이즈 억제작용

• 영문명: Synthesis and beta-Lactamase Inhibitory Activity of 7-Exomethylene Cephalosporanates
• 발행기관: 대한약학회
• 저자명: 이종민(Jong Min Lee) 최수항(Su Hang Choi) 이현수(Hyun Soo Lee) 임채욱(Chae Uk Im) 임철부(Chul Bu Yim)
• 간행물 정보: 『약학회지』제43권 제6호 (1999년), 782~788쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1999.12.28

영문 초록

7-Oxocephalosporanate 1 was treated with phosphonium salts 2~4 by Wittig reaction to afford 7-exomethylene cephalosporanates 5-7. They were oxidized to sulfones 8-10 with mCPBA. Deprotection of benzhydryl 7-exomethylene cephalosporanate with AlCl3 and NaHC03 gave sodium salts of 7-exomethylene cephalosporanates 11-16. The beta-lactamase inhibitory activity of synthesized compounds 11~16 were compared with sulbactam, tazobactam and clavulanic acid against Type I, II, III, IV and TEM-2 beta-lactamase in vitro. Compound 15 showed more potent activity than sulbactam and clavulanic acid against Type III, IV beta-lactamase enzyme.

키워드

7-Exomethylene cephalosporanates β-lactamase inhibitors.