دورية
Allosteric Inhibitors against HIV-1 Reverse Transcriptase: Design and Synthesis of MKC-442 Analogues Having an Ω-Functionalized Acyclic Structure
| العنوان: | Allosteric Inhibitors against HIV-1 Reverse Transcriptase: Design and Synthesis of MKC-442 Analogues Having an Ω-Functionalized Acyclic Structure |
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| المؤلفون: | Tanaka, H, Walker, RT, Hopkins, AL, Ren, J, Jones, EY, Fujimoto, K, Hayashi, M, Miyasaka, T, Baba, M, Stammers, DK, Stuart, DI |
| المصدر: | Antiviral Chemistry & Chemotherapy; August 1998, Vol. 9 Issue: 4 p41-48, 8p |
| مستخلص: | Based on X-ray crystallographic analysis of MKC-442/human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) complex, analogues in which the N1-substituent is replaced with ω-functionalized alkyl groups were designed to improve the affinity for the enzyme. Synthesis of these compounds was carried out starting from MKC-442 by a sequence of reactions (N3-protection, removal of N1-ethoxymethyl group, alkylation, and N3-deprotection). The compounds were evaluated for anti-HIV activity. Structure–activity relationships are discussed in terms of the possible interaction with the enzyme. |
| قاعدة البيانات: | Supplemental Index |
Full Text Finder | تدمد: | 09563202 20402066 |
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| DOI: | 10.1177/095632029800900404 |