Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Benzyl derivatives with broad potency against resistant mutant viruses

An analysis of the binding motifs of known HIV-1 non-nucleoside reverse transcriptase inhibitors has led to discovery of novel piperidine-linked aminopyrimidine derivatives with broad activity against wild-type as well as drug-resistant mutant viruses. Notably, the series retains potency against the...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (14), p.4215-4218
Hauptverfasser:	Kertesz, Denis J., Brotherton-Pleiss, Christine, Yang, Minmin, Wang, Zhanguo, Lin, Xianfeng, Qiu, Zongxing, Hirschfeld, Donald R., Gleason, Shelley, Mirzadegan, Taraneh, Dunten, Pete W., Harris, Seth F., Villaseñor, Armando G., Hang, Julie Qi, Heilek, Gabrielle M., Klumpp, Klaus
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminopyrimidine Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral Antiviral agents Biological and medical sciences Crystal structure Drug Discovery Drug Resistance, Viral - genetics HIV HIV Reverse Transcriptase - antagonists & inhibitors HIV-1 - drug effects HIV-1 - genetics Human immunodeficiency virus 1 Inhibitor Medical sciences Models, Molecular Mutation NNRTI Pharmacology. Drug treatments Pyrimidines - chemistry Pyrimidines - pharmacology Reverse transcriptase Reverse Transcriptase Inhibitors - pharmacology Structure-Activity Relationship Viral mutants
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