HIV-1 non-nucleoside reverse transcriptase inhibitors: incorporation of benzylphosphonate moiety for solubility improvement

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• 作者：Elena S. Matyugina^a ; Vladimir T. Valuev-Elliston^a ; Alexander O. Chizhov^b ; Sergei N. Kochetkov^a ; Anastasia L. Khandazhinskaya^a ; ^{khandazhinskaya@bk.ru" class="auth_mail" title="E-mail the corresponding author}
• 刊名：Mendeleev Communications
• 出版年：2016
• 出版时间：March-April 2016
• 年：2016
• 卷：26
• 期：2
• 页码：114-116
• 全文大小：159 K

文摘

Benzylphosphonates of 5’-norcarbocyclic analogue of 2’,3’-dideoxy-2’,3’-didehydrouridine and its N³-benzyl derivatives with different substituents at the phosphorus atom were designed and synthesized in attempt to improve solubility of potential non-nucleoside reverse transcriptase inhibitor. Solubility of the most hydrophilic representative was 400 mg in 100 ml of 1% DMSO solution in water. The target phosphonates were examined against HIV-1 reverse transcriptase with K_I for all compounds being higher than 100 μM.