{"id":12185,"date":"2023-02-07T02:27:13","date_gmt":"2023-02-06T18:27:13","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=12185"},"modified":"2023-02-07T02:27:13","modified_gmt":"2023-02-06T18:27:13","slug":"meng-wei-et-al-published-their-research-in-journal-of-medicinal-chemistry-in-2010-cas-3528-58-3","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=12185","title":{"rendered":"Meng, Wei et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 3528-58-3"},"content":{"rendered":"

Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors was written by Meng, Wei;Brigance, Robert P.;Chao, Hannguang J.;Fura, Aberra;Harrity, Thomas;Marcinkeviciene, Jovita;O’Connor, Stephen P.;Tamura, James K.;Xie, Dianlin;Zhang, Yaqun;Klei, Herbert E.;Kish, Kevin;Weigelt, Carolyn A.;Turdi, Huji;Wang, Aiying;Zahler, Robert;Kirby, Mark S.;Hamann, Lawrence G.. And the article was included in Journal of Medicinal Chemistry in 2010.Related Products of 3528-58-3<\/a> This article mentions the following:<\/p>\n

Continued structure-activity relation (SAR) exploration within our previously disclosed azolopyrimidine containing dipeptidyl peptidase-4 (DPP4) inhibitors led us to focus on an imidazolopyrimidine series in particular. Further study revealed that by replacing the aryl substitution on the imidazole ring with a more polar carboxylic ester or amide, these compounds displayed not only increased DPP4 binding activity but also significantly reduced human ether-a-go-go related gene (hERG) and sodium channel inhibitory activities. Addnl. incremental adjustment of polarity led to permeable mols. which exhibited favorable pharmacokinetic (PK) profiles in preclin. animal species. The active site binding mode of these compounds was determined by x-ray crystallog. as exemplified by amide 24c. A subsequent lead mol. from this series, (+)-6-(aminomethyl)-5-(2,4-dichlorophenyl)-N-(1-ethyl-1H-pyrazol-5-yl)-7-me3 thylimidazo[1,2-a]pyrimidine-2-carboxamide (24s), emerged as a potent, selective DPP4 inhibitor that displayed excellent PK profiles and in vivo efficacy in ob\/ob mice. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3Related Products of 3528-58-3<\/a>).<\/p>\n

1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. The pyrazole ring is resistant to oxidation and reduction but the groups, such as alkyl and formyl attached to the ring, are oxidized to respective acids. Only electrolytic oxidation, ozonolysis, and a strong base cause ring opening.Related Products of 3528-58-3<\/a><\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. The pyrazole ring is resistant to oxidation and reduction but the groups, such as alkyl and formyl attached to the ring, are oxidized to respective acids. Only electrolytic oxidation, ozonolysis, and a strong base cause ring opening.Related Products of 3528-58-3<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[830,131],"tags":[128],"class_list":["post-12185","post","type-post","status-publish","format-standard","hentry","category-3528-58-3","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"\nMeng, Wei et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 3528-58-3 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors was written by Meng, Wei;Brigance, Robert P.;Chao, Hannguang J.;Fura, Aberra;Harrity, Thomas;Marcinkeviciene, Jovita;O'Connor, Stephen P.;Tamura, James K.;Xie, Dianlin;Zhang, Yaqun;Klei, Herbert E.;Kish, Kevin;Weigelt, Carolyn A.;Turdi, Huji;Wang, Aiying;Zahler, Robert;Kirby, Mark S.;Hamann, Lawrence G.. 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