Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors

[Display omitted] Integration of viral DNA into the host cell genome is an obligatory process for successful replication of HIV-1. Integrase catalyzes the insertion of viral DNA into the target DNA and is a validated target for drug discovery. Herein, we report the synthesis, antiviral activity and...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-02, Vol.25 (3), p.717-720
Hauptverfasser:	Naidu, B. Narasimhulu, Sorenson, Margaret E., Patel, Manoj, Ueda, Yasutsugu, Banville, Jacques, Beaulieu, Francis, Bollini, Sagarika, Dicker, Ira B., Higley, Helen, Lin, Zeyu, Pajor, Lori, Parker, Dawn D., Terry, Brian J., Zheng, Ming, Martel, Alain, Meanwell, Nicholas A., Krystal, Mark, Walker, Michael A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - chemistry Amides - pharmacokinetics Animals Half-Life Heterocyclic Compounds - chemistry HIV Integrase - chemistry HIV Integrase - metabolism HIV Integrase Inhibitors - chemical synthesis HIV Integrase Inhibitors - chemistry HIV Integrase Inhibitors - pharmacokinetics HIV-1 HIV-1 - drug effects HIV-1 - enzymology Human immunodeficiency virus 1 Humans Inhibitor Integrase Male Pyrimidine-4-carboxamide Pyrimidines - chemistry Rats Rats, Sprague-Dawley Strand transfer Structure-Activity Relationship
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Zusammenfassung:	[Display omitted] Integration of viral DNA into the host cell genome is an obligatory process for successful replication of HIV-1. Integrase catalyzes the insertion of viral DNA into the target DNA and is a validated target for drug discovery. Herein, we report the synthesis, antiviral activity and pharmacokinetic profiles of several C2-carbon-linked heterocyclic pyrimidinone-4-carboxamides that inhibit the strand transfer step of the integration process.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.11.060