96155-89-4Relevant academic research and scientific papers
BMS-201620: A selective beta 3 agonist
Washburn,Sun,Bisacchi,Wu,Cheng,Sher,Ryono,Gavai,Poss,Girotra,McCann,Mikkilineni,Dejneka,Wang,Merchant,Morella,Arbeeny,Harper,Slusarchyk,Skwish,Russell,Allen,Tesfamariam,Frohlich,Abboa-Offei,Cap,Waldron,George,Young,Dickinson,Seymour
, p. 3525 - 3529 (2007/10/03)
A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human β3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent β3 full agonist (Ki=93nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation.
Quantitative Approaches to Optical Resolution. Part 1. Resolution of DL-Phenylglycine Derivatives with (+)-Tartaric Acid
Lopata, Antal,Faigl, Ferenc,Fogassy, Elemer,Darvas, Ferenc
, p. 2930 - 2952 (2007/10/02)
The results of 23 cases of resolution of DL-phenyldlycine derivatives (I) with (+)-tartaric acid in various solvents are investigated, using correlation analysis, as a function of the introduced racemic compounds and the solvent used.A procedure, combining three quantitative structure-activity relationship methods, i.e.Golender and Rozenblit's logico-structural approach with the Free-Wilson and Hansch analyses, resulted in statistically significant relationships.It is suggested that the solvent may exert two kinds of influence: (1) the higher the solvent polarity, the more likely the L-(I) salt to crystallise; (2) alcoholic mixtures, although being highly polar, favour the precipitation of the D-(I) salt rather than that of the L-(I) salt, probably due to a selective interaction with the diastereomers.As to the racemic compound, the relationships obtained are in accord with literature statements that resolution proceeds by a multiple interaction mechanism.
A QUANTITATIVE APPROACH TO OPTICAL RESOLUTION
Fogassy, Elemer,Lopata, Antal,Faigl, Ferenc,Darvas, Ferenc,Acs, Maria,Toke, Laszlo
, p. 647 - 650 (2007/10/02)
Significant statistical relationships have been found between the parameters characterizing the results and circumstances of the resolutions of seventeen phenylglycine derivatives.The successful predictions given for the results of six indefendent resolutions prove the utility of these relationships.
