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Structure-activity Relationship Studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a Potent Inhibitor of Leukotriene A(4) (LTA(4)) Hydrolase

Structure-activity Relationship Studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a Potent Inhibitor of Leukotriene A(4) (LTA(4)) Hydrolase

T D Penning, N S Chandrakumar, B B Chen, H Y Chen, B N Desai, S W Djuric, S H Docter, A F Gasiecki, R A Haack, J M Miyashiro, M A Russell, S S Yu, D G Corley, R C Durley, B F Kilpatrick, B L Parnas, L J Askonas, etc.

J Med Chem. 2000 Feb 24;43(4):721-35.

PMID: 10691697

Abstract:

Leukotriene B(4) (LTB(4)) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA(4) hydrolase is the rate-limiting step for LTB(4) production, this enzyme represents an attractive pharmacological target for the suppression of LTB(4) production. From an in-house screening program, SC-22716 (1, 1-[2-(4-phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA(4) hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA(4) hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP262451898	SC 22716		262451-89-8	Price

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