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二氧化苯并噻二嗪的抗HIV-1活性。

Anti-HIV-1 activity of benzothiadiazine dioxide.

作者信息

Martinez A, Gil C, Castro A, Perez C, Witvrouw M, Pannecouque C, Balzarini J, De Clercq E

机构信息

Instituto de Química Médica (CSIC), Madrid, Spain.

出版信息

Antivir Chem Chemother. 2001 Nov;12(6):347-51. doi: 10.1177/095632020101200604.

Abstract

Antiviral assays carried out on the potent benzothiadiazine dioxide (BTD) human cytomegalovirus (HCMV) inhibitors have led us to find marginal but selective anti-HIV-1 activity. Specific pharmacological studies, such as time of addition experiments and assays on specific viral strains with mutations on its reverse transcriptase, have indicated that BTD compounds act as non-nucleoside reverse transcriptase inhibitors. Theoretical calculations showed a butterfly conformation for the active derivatives that are compatible with their mechanism of action. Therefore, BTD derivatives can be considered as potential lead compounds for the treatment of opportunistic HCMV infections in immunocompromised individuals such as AIDS patients.

摘要

对强效苯并噻二嗪二氧化物(BTD)人巨细胞病毒(HCMV)抑制剂进行的抗病毒试验,使我们发现了微弱但具有选择性的抗HIV-1活性。具体的药理学研究,如添加时间实验以及对逆转录酶有突变的特定病毒株的检测,表明BTD化合物可作为非核苷类逆转录酶抑制剂。理论计算显示,活性衍生物呈蝴蝶构象,这与其作用机制相符。因此,BTD衍生物可被视为治疗免疫功能低下个体(如艾滋病患者)机会性HCMV感染的潜在先导化合物。

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