Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead

Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery of nanomolar BRS-3 agonists. Starting from a weak omeprazole screening hit, repla...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-10, Vol.18 (20), p.5451-5455
Main Authors: Carlton, David L., Collin-Smith, Lissa J., Daniels, Alejandro J., Deaton, David N., Goetz, Aaron S., Laudeman, Christopher P., Littleton, Thomas R., Musso, David L., Morgan, Ronda J. Ott, Szewczyk, Jerzy R., Zhang, Cunyu
Format: Article
Language:English
Subjects:
Baculoviridae - metabolism
BB 3
Benzimidazoles - chemistry
Biological and medical sciences
Bombesin
Bombesin receptor subtype 3 agonist
Brain - metabolism
BRS-3
Chemistry, Pharmaceutical - methods
Chlorofluorocarbons, Methane - chemistry
Drug Design
Drug Evaluation, Preclinical
G-Protein coupled seven transmembrane receptor modulation
Humans
Kinetics
Medical sciences
Models, Chemical
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Omeprazole
Omeprazole - chemistry
Orphan seven transmembrane receptor
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Pyridines - chemistry
Receptors, Bombesin - agonists
Receptors, Bombesin - chemistry
Sulfides - chemistry
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Summary:Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery of nanomolar BRS-3 agonists. Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery of nanomolar BRS-3 agonists.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.09.033