Literature DB >> 15177466

BMS-201620: a selective beta 3 agonist.

W N Washburn1, C-Q Sun, G Bisacchi, G Wu, P T Cheng, P M Sher, D Ryono, A V Gavai, K Poss, R N Girotra, P J McCann, A B Mikkilineni, T C Dejneka, T C Wang, Z Merchant, M Morella, C M Arbeeny, T W Harper, D A Slusarchyk, S Skwish, A D Russell, G T Allen, B Tesfamariam, B H Frohlich, B E Abboa-Offei, M Cap, T L Waldron, R J George, D Young, K E Dickinson, A A Seymour.   

Abstract

A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human beta3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation.

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Year:  2004        PMID: 15177466     DOI: 10.1016/j.bmcl.2004.04.074

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.

Authors:  P Senthil Kumar; Prasad V Bharatam
Journal:  Med Chem Res       Date:  2009-10-31       Impact factor: 1.965

2.  Asymmetric synthesis of α-allyl-α-aryl α-amino acids by tandem alkylation/π-allylation of α-iminoesters.

Authors:  John M Curto; Joshua S Dickstein; Simon Berritt; Marisa C Kozlowski
Journal:  Org Lett       Date:  2014-03-25       Impact factor: 6.005

3.  α-Allyl-α-aryl α-amino esters in the asymmetric synthesis of acyclic and cyclic amino acid derivatives by alkene metathesis.

Authors:  John M Curto; Marisa C Kozlowski
Journal:  J Org Chem       Date:  2014-05-14       Impact factor: 4.354

  3 in total

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