Kormos, Chad M. published the artcileDiscovery of N-{4-[(3-Hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide Analogues as Selective Kappa Opioid Receptor Antagonists, Computed Properties of 33697-81-3, the publication is Journal of Medicinal Chemistry (2013), 56(11), 4551-4567, database is CAplus and MEDLINE.
There is continuing interest in the discovery and development of new κ opioid receptor antagonists. We recently reported that N-substituted 3-methyl-4-(3-hydroxyphenyl)piperazines were a new class of opioid receptor antagonists. In this study, we report the syntheses of two piperazine JDTic-like analogs. Evaluation of the two compounds in an in vitro [35S]GTPγS binding assay showed that neither compound showed the high potency and κ opioid receptor selectivity of JDTic. A library of compounds was synthesized by amidation of compound I with com. available arylcarboxylic acids and tested for their ability to inhibit [35S]GTPγS binding stimulated by the selective κ opioid agonist U69,593. These studies led to N-[(1S)-1-{[(3S)-4-(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl}-2-methylpropyl]-4-phenoxybenzamide (II), a compound that showed good κ opioid receptor antagonist properties. An SAR study based on II provided 28 novel analogs. Evaluation of these 28 compounds in the [35S]GTPγS binding assay showed that several of the analogs were potent and selective κ opioid receptor antagonists.
Journal of Medicinal Chemistry published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Computed Properties of 33697-81-3.
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