Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists

Autor:	André deRosier, David G. Loughhead, David Mark Rotstein, Shelley K. Gleason, Eun Kyung Lee, Fernando Padilla, Lina Setti, Dick Cournoyer, Remy Lemoine, Cheng-I. Mau, Paul Weller, Andreas Jekle, Jutta Wanner, Pamela Berry, Chris Richard Melville, Marianna Dioszegi, Ann C. Petersen, Surya Sankuratri, Jason Manka, Changhua Ji, Lin Xiao-Fa, Lijing Chen, Gabrielle Heilek, Lubov Filonova
Rok vydání:	2010
Předmět:	Anti hiv 1 Receptors CCR5 medicine.drug_class Stereochemistry Anti-HIV Agents Clinical Biochemistry Human immunodeficiency virus (HIV) Pharmaceutical Science Carboxamide CCR5 receptor antagonist medicine.disease_cause Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship HIV Fusion Inhibitors Drug Discovery medicine Animals Humans Pyrroles skin and connective tissue diseases Molecular Biology Pyrrole Anti hiv fungi Organic Chemistry Combinatorial chemistry Rats body regions chemistry Benzamides CCR5 Receptor Antagonists Microsomes Liver Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 20(10)
ISSN:	1464-3405
Popis:	Starting with a high-throughput screening lead, a novel series of CCR5 antagonists was developed utilizing an information-based approach. Improvement of pharmacokinetic properties for the series was pursued by SAR exploration of the lead template. The synthesis, SAR and biological profiles of the series are described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::757bbb465169e0977e2a95f17e17d1e6 https://pubmed.ncbi.nlm.nih.gov/20417098 Zobrazit plný text záznamu Full Text from ScienceDirect