SYNTHESIS, MOLECULAR CONFORMATION AND ACTIVITY AGAINST HERPES SIMPLEX VIRUS OF (E)-5-(2-BROMOVINYL)-2′-DEOXYCYTIDINE ANALOGS

被引:0
|
作者
Zoghaib, Wajdi Michel [1 ]
Mannala, Shajan [3 ]
Gupta, V. Sagar [3 ]
Tourigny, Guy [2 ]
机构
[1] Sultan Qaboos Univ, Dept Chem, Al Khoud 123, Oman
[2] Univ Saskatchewan, Dept Chem, Saskatoon, SK S7N 0W0, Canada
[3] Univ Saskatchewan, Dept Biomed Sci, Saskatoon, SK S7N 0W0, Canada
来源
基金
英国医学研究理事会;
关键词
Herpes simplex virus; (E)-5-(2-bromovinyl)-2 '-deoxycytidine; conformational analysis; CRYSTAL-STRUCTURES; THYMIDINE KINASE; 5-METHOXYMETHYL-2'-DEOXYCYTIDINE; NUCLEOSIDES; DNA;
D O I
10.1080/15257770.2012.661214
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Analogs of (E)-5-(2-bromovinyl)-2'-deoxycytidine (BrVdCyd) (1) by substitution at N-4 were synthesized to impart resistance against deamination. The anti-HSV-1 activity and solution conformation of these analogs were determined. N-4-Acetyl-BrVdCyd (2) was a potent inhibitor of HSV-1 replication whereas N-4-propanoyl-BrVdCyd (3) had good activity and N-4-Butanoyl-BrVdCyd (4) had only low activity against HSV-1 replication. N-4-Methyl-BrVdCyd (5) was devoid of activity against HSV-1.
引用
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页码:364 / 376
页数:13
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