CCK1-antagonists: Design, Synthesis and Evaluation of N-Substituted Isobuyl-5-Hydroxy-5-Phenyl-Pyrrol-2-Ones as Adjunct to Opiates

Eric Lattmann, Jintana Sattayasai, Ramesh Narayanan, Julian Benyamen, Balaram Pn and Pornthip Lattmann
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Eric Lattmann: School of Life and Health Sciences, Aston University, England
Jintana Sattayasai: Department of Pharmacology, Faculty of Medicine, Khon Kaen University, Thailand
Ramesh Narayanan: Department of Medicine, University of Tennessee Health Science Center, USA
Pornthip Lattmann: PNB Vesper Life Science PVT, India

Organic & Medicinal Chemistry International Journal, 2018, vol. 5, issue 5, 138-147

Abstract: Arylated 5-hydroxy–pyrrol-2-ones were prepared in 2 synthetic steps from muco- chloric acid and were optimised as CCK selective ligands using radiolabelled binding assays. A potent CCK1 selective ligand was identified ( PNB-081: CCK1= 20 nM) as part of systematic SAR optimisation. The antagonism was confirmed for the ligands by using isolated tissue preparations with CCK8S. The cholecystokinin antagonist PNB-081 potentiated the analgesic effect of morphine and reversed opiate tolerance in mice from doses >1 mg/kg by oral administration.

Keywords: juniper publishers:Medicinal Chemistry; Biochemistry Journal; Pharmacology Journal; biochemical pharmacology; molecular pharmacology; biochemistry; open access journals; peer reviewed journals; Open Access; Journal of Molecular Biochemistry; International Research Journal of Pure and Applied Chemistry; World Journal of Biological Chemistry; Biochemistry and Analytical Biochemistry; Biochemistry & Physiology: Open Access; Molecular Biology International; Plant Biochemistry & Physiology; International Journal of Molecular Sciences; Journal of Clinical and Medical Genomics; Environmental Analytical Chemistry; Medicinal Chemistry; Juniper publishers reivews (search for similar items in EconPapers)
Date: 2018
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Persistent link: https://EconPapers.repec.org/RePEc:adp:jomcij:v:5:y:2018:i:5:p:138-147

DOI: 10.19080/OMCIJ.2018.05.555672

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