Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.

Shankaran Kothandaraman,Karla L. Donnely,Gabor Butora,Richard Jiao,Alexander Pasternak,Gregori J. Morriello,Stephen D. Goble,Changyou Zhou,Sander G. Mills,Malcolm Maccoss,Pasquale P. Vicario,Julia M. Ayala,Julie A. DeMartino,Mary Struthers,Margaret A. Cascieri,Lihu Yang

Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.

2009

Shankaran Kothandaraman
Karla L. Donnely
Gabor Butora
Richard Jiao
Alexander Pasternak
Gregori J. Morriello
Stephen D. Goble
Changyou Zhou
Sander G. Mills
Malcolm Maccoss
Pasquale P. Vicario
Julia M. Ayala
Julie A. DeMartino
Mary Struthers
Margaret A. Cascieri
Lihu Yang

A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity.

Keywords:

CCR2
Organic chemistry
Stereochemistry
Structure–activity relationship
Receptor
Tetrahydropyran
Biochemistry
Chemistry
Carboxamide
Chemical synthesis
design synthesis
Amination

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