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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 omega-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.


Journal article


Antiviral chemistry & chemotherapy

Publication Date





325 - 332


School of Pharmaceutical Sciences, Showa University, Tokyo, Japan.


Cell Line, HIV-1, Uracil, Reverse Transcriptase Inhibitors, Antiviral Agents, Anti-HIV Agents, Virus Replication, Allosteric Site, Molecular Structure, Hydrogen Bonding, Models, Molecular, Mass Spectrometry, HIV Reverse Transcriptase