Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 22, 2010, Pages 6802-6807

  Wanner, Jutta ^a,b   Chen, Lijing ^a   Lemoine, Rémy C ^a   Kondru, Rama ^a,b   Jekle, Andreas ^a,c   Heilek, Gabrielle ^a   Derosier, André ^a   Ji, Changhua ^a   Berry, Pamela W ^a,b   Rotstein, David M ^a  

^a Roche Palo Alto ^*  (United States)

^b HOFFMANN LA ROCHE INC   (United States)

^c NovaBay Pharmaceuticals Inc   (United States)

Author keywords

CCR5 antagonist; HIV entry inhibition; Permeability

Indexed keywords

AMIDE; AZETIDINE; CHEMOKINE RECEPTOR CCR5 ANTAGONIST; PIPERIDINE; RANTES; SULFONAMIDE;

ANTIVIRAL ACTIVITY; ARTICLE; CELL FUSION; DRUG PENETRATION; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; GRIGNARD REACTION; HYDROGENATION; IC 50; STRUCTURE ACTIVITY RELATION;

AMIDES; AZA COMPOUNDS; RECEPTORS, CCR5; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77958043300     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.08.118     Document Type: Article

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