4',5'-측쇄를 가진 새로운 피리미딘 뉴크레오사이드의 합성 및 항바이러스 약효검색

• 영문명: Synthesis and Activity of Novel 4',5'-Branched Pyrimidine Nucleosides
• 발행기관: 대한약학회
• 저자명: 김애홍(Aihong Kim) 구대호(Dae-Ho Ko) 고옥현(Ok Hyun Ko) 홍준희(Joon Hee Hong)
• 간행물 정보: 『약학회지』제49권 제1호 (2005년), 20~24쪽, 전체 5쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2005.02.28

영문 초록

The synthesis of 4',5'-doubly branched carbocyclic nucleosides was accomplished in this study. The selective methylation in the 5'-position was made by Felkin-Anh controlled Grignard addition. The construction of the required 4'-quaternary carbon was carried out by using a [3,3]-sigmatropic rearrangement. Bis-vinyl 6 was successfully cyclized using a Grubbs' catalyst ll. The natural pyrimidine bases (cytosine, uracil, thymine) were efficiently coupled using a Pd(0) catalyst. When the synthesized compounds were examined for their activity against several viruses such as the HIV-1, HSV-1, HSV-2 and HCMV, the cytosine analogue 13 exhibited weak antiviral activity against the HCMV.

키워드

doubly branched nucleoside antiviral agents grignard addition felkin-anh model