Zhao, Jian published the artcileDiscovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist, Application In Synthesis of 1256345-79-5, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(21), 127496, database is CAplus and MEDLINE.
The discovery of a novel 3H-pyrido[2,3-d]pyrimidin-4-one series as potent and biased sst2 agonists is described. This class of mols. exhibits excellent sst2 potency and selectivity against sst1, sst3, and sst5 receptors, and they are significantly more potent at inhibiting cAMP production than inducing internalization. The orally bioavailable 6-(3-chloro-5-methylphenyl)-3-(3-fluoro-5-hydroxyphenyl)-5-({methyl[(2S)-pyrrolidin-2-ylmethyl]amino}methyl)-3H,4H-pyrido[2,3-d]pyrimidin-4-one (36) also suppresses GH secretion in GHRH-challenged rats in a dose-dependent manner.
Bioorganic & Medicinal Chemistry Letters published new progress about 1256345-79-5. 1256345-79-5 belongs to alcohols-buliding-blocks, auxiliary class Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic Acids,Boronic acid and ester, name is (3-Hydroxy-5-methylphenyl)boronic acid, and the molecular formula is C10H9NO4S, Application In Synthesis of 1256345-79-5.
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