{"id":11070,"date":"2022-11-21T04:54:55","date_gmt":"2022-11-20T20:54:55","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11070"},"modified":"2022-11-21T04:54:55","modified_gmt":"2022-11-20T20:54:55","slug":"procopiou-panayiotis-a-s-team-published-research-in-journal-of-medicinal-chemistry-in-61-cas-1025735-46-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11070","title":{"rendered":"Procopiou, Panayiotis A.’s team published research in Journal of Medicinal Chemistry in 61 | CAS: 1025735-46-9"},"content":{"rendered":"

Procopiou, Panayiotis A. published the artcileDiscovery of (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic \u03b1v<\/sub>\u03b26<\/sub> Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis<\/i><\/b>, Quality Control of 1025735-46-9<\/a>, the publication is Journal of Medicinal Chemistry (2018), 61(18), 8417-8443, database is CAplus and MEDLINE.<\/p>\n

A series of 3-aryl-(pyrrolidin-1-yl)butanoic acids were synthesized using a diastereoselective route, which involved rhodium catalyzed asym. 1,4-addition of arylboronic acids in the presence of (R)-BINAP to a crotonate ester to provide the (S) absolute configuration for the major product. A variety of aryl substituents including morpholine, pyrazole, triazole, imidazole and cyclic ether were screened in cell adhesion assays for affinity against \u03b1v\u03b21, \u03b1v\u03b23, \u03b1v\u03b25, \u03b1v\u03b26 and \u03b1v\u03b28 integrins. Several analogs with high affinity and selectivity for the \u03b1v\u03b26 integrin were identified. The analog I<\/strong>\u00b7HCl was found to have high affinity for \u03b1v\u03b26 integrin in a radioligand binding assay (pKi = 11), a long dissociation half-life (7 h) , high solubility in saline at pH 7 (>71 mg\/mL) and pharmacokinetic properties commensurate with inhaled dosing by nebulization. It was selected for further investigation as a potential therapeutic agent for the treatment of idiopathic pulmonary fibrosis.<\/p>\n

Journal of Medicinal Chemistry published new progress about 1025735-46-9. 1025735-46-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Benzene,Boronic Acids, name is 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid, and the molecular formula is C11H13BN2O2, Quality Control of 1025735-46-9<\/a>.<\/p>\n

Referemce:
https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

Journal of Medicinal Chemistry published new progress about 1025735-46-9. 1025735-46-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Benzene,Boronic Acids, name is 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid, and the molecular formula is C11H13BN2O2, Quality Control of 1025735-46-9<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[131],"tags":[716],"class_list":["post-11070","post","type-post","status-publish","format-standard","hentry","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nProcopiou, Panayiotis A.'s team published research in Journal of Medicinal Chemistry in 61 | CAS: 1025735-46-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Procopiou, Panayiotis A. published the artcileDiscovery of 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