Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1

D Dhanak; L T Christmann; M G Darcy; A J Jurewicz; R M Keenan; J Lee; H M Sarau; K L Widdowson; J R White

doi:10.1016/s0960-894x(01)00248-7

Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1441-4. doi: 10.1016/s0960-894x(01)00248-7.

Authors

D Dhanak¹, L T Christmann, M G Darcy, A J Jurewicz, R M Keenan, J Lee, H M Sarau, K L Widdowson, J R White

Affiliation

¹ SmithKline Beecham Pharmaceuticals, 1250 South Collegeville Road, PO Box 5089, Collegeville, PA 19426-0989, USA. dash_dhanak-1@sbphrd.com

PMID: 11378373
DOI: 10.1016/s0960-894x(01)00248-7

Abstract

The discovery of a series of phenylalanine derived CCR3 antagonists is reported. Parallel, solution-phase library synthesis has been utilized to delineate the structure-activity relationship leading to the synthesis of highly potent, CCR3-selective antagonists.

MeSH terms

Humans
Phenylalanine / chemistry*
Phenylalanine / pharmacology*
Receptors, CCR3
Receptors, Chemokine / antagonists & inhibitors*
Receptors, Chemokine / metabolism
Structure-Activity Relationship

Substances

CCR3 protein, human
Receptors, CCR3
Receptors, Chemokine
Phenylalanine