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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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 20; no. 14; pp. 4215 - 4218
Main Authors:	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:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 15-07-2010 Elsevier
Subjects:	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 Aminopyrimidine Reverse transcriptase HIV NNRTI Antiviral Inhibitor Viral mutants Nitrile RNA-directed DNA polymerase Sulfone HIV-1 virus Non nucleoside compound Structure activity relation Chlorine Organic compounds Reverse transcriptase inhibitor Piperidine derivatives Bromine Organic compounds Enzyme Transferases Benzene derivatives Retroviridae Enzyme inhibitor Lentivirus In vitro Virus Resistance Nucleotidyltransferases Pyrimidine derivatives Human immunodeficiency virus Mutation
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