Delving into the Latest Updates on L-674636 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

L 674636

Target

FLAP

Action

inhibitors

Mechanism

FLAP inhibitors(5-lipoxygenase activating protein inhibitors)

Therapeutic Areas

Respiratory Diseases

Active Indication-

Inactive Indication

Respiratory Diseases

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization-

Inactive Organization

Merck Sharp & Dohme Corp.

License Organization-

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC28H26ClNO3S

InChIKeyQEJSGEVFYKLAOJ-UHFFFAOYSA-N

CAS Registry127481-38-3

The authors describe the development of a second class of a highly potent LT synthesis inhibitor, based on a quinoline structure.These compounds, like MK 886, are inhibitors of cellular LT synthesis and are inactive inhibitors of soluble 5-lipoxygenase (5-LO).Such agents also act on the 18 kDa FLAP protein and inhibit 5-LO translocation in a manner analogous to MK 886.A member of this class of compounds, ((4- (4-Chlorophenyl)-1-(4-2-quinolinylmethoxy)phenyl)butyl)-thio)acetic acid, L-674,636, showed excellent bioavailability and demonstrated functional and biochem. efficacy in animal models.

Journal of lipid mediators

A new class of leukotriene biosynthesis inhibitor: the development of MK-0591.

Article

Author: Brideau, C ; Evans, J F ; Frenette, R ; Belley, M ; Chan, C ; Blouin, M ; Guay, J ; Gauthier, J Y ; Charleson, S ; Prasit, P

The evolution of MK-0591 (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-ylmethoxy+ ++)indol-2-yl]- 2,2-dimethylpropanoic acid), 12, a potent, orally active leukotriene biosynthesis inhibitor is described. MK-0591 is currently undergoing clinical evaluation as a potential agent for the treatment of asthma and inflammatory bowel disease. It acts through a novel mechanism by a specific interaction with a membrane protein, 5-lipoxygenase activating protein (FLAP), which has been shown to be essential for LT synthesis in inflammatory cells. A brief comparison of its biological activity with that of its progenitors MK-886 and L-674,636 is described.

100 Deals associated with L-674636

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