Delving into the Latest Updates on SB-568849 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

SB 568849

Target

MCHR1

Action

inhibitors

Mechanism

MCHR1 inhibitors(Melanin-concentrating hormone receptor 1 inhibitors)

Therapeutic Areas

Endocrinology and Metabolic DiseaseOther Diseases

Active Indication-

Inactive Indication

Anxiety DisordersObesity

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK Plc

License Organization-

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques were utilised to allow rapid exploration of the structure-activity relationship around this template, leading to compound SB-568849 which possessed good receptor affinity and selectivity. This compound proved to be an antagonist with stability in vivo, an acceptable brain-blood ratio and oral bioavailability.

01 Sep 2006·Bioorganic & medicinal chemistry lettersQ4 · MEDICINE

Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849

Q4 · MEDICINE

Article

Author: Jeffrey, Phillip ; O'Hanlon, Peter J. ; Muir, Alison I. ; Stemp, Geoffrey ; Johnson, Christopher N. ; Winborn, Kim Y. ; Stevens, Alex J. ; Al-Barazanji, Kamal ; Witty, David R. ; Haynes, Andrea ; Thewlis, Kevin ; Hervieu, Guillaume J. ; Hamprecht, Dieter ; Bateson, John

A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.

100 Deals associated with SB-568849

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