신규 피리미딘 티오에피오 뉴크레오사이드의 합성 및 항바이러스 약효검색

• 영문명: Synthesis and Antiviral Evaluation of Novel Pyrimidine Thioapionucleosides
• 발행기관: 대한약학회
• 저자명: 이내상(Rae Sang Lee) 홍준희(Joon Hee Hong) 고옥현(Ok Hyun Ko)
• 간행물 정보: 『약학회지』제50권 제2호 (2006년), 65~69쪽, 전체 5쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2006.04.30

영문 초록

Novel 4'-hydroxymethyl blanched thioapiosyl nucleosides were synthesized in this study. The introduction of hydroxymethyl group in the 4'-position was accomplished by a 〔3,3〕-sigmatropic rearrangement. Thisoapiosyl sugar moiety was comstructed by sequential ozonolysis, reduction and cyclization. The pyrimidine nucleosidic bases (uracil, 5-fluorouracil, 5-iodouracil, 5-cchlorouracil, 5-bromouracil) were efficiently coupled by Vorbruggen glycosyl condensation procedure (per- silyated base and TMSOTf). The antiviral activities of the synthesized compounds were evaluated against the HIV-1, HSV-1, HSV-2 and EMCV. 5-lodouracil 18 showed weak antiviral activity against HSZ-1 (EC50=30.7 ㎛).

키워드

antiviral agent thioapionucleoside Vorbruggen reaction