A search for a suitable replacement for the central norbornyl scaffold presented in the recently disclosed novel FLAP inhibitors is herein described, as well as the SAR study performed on the endo and exo-aryl groups.
Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.
Sulfonamide analogues of the potent CB1R inverse agonist taranabant were prepared and optimized for potency and selectivity for CB1R. They were variably more potent than the corresponding amide analogues. The most potent representative 22 had good pharmacokinetic and brain levels, but was modestly active in blocking CB1R agonist-mediated hypothermia.
linda l chang合作论文数3Mark T. Goulet合作论文数3J. J. BRONSON合作论文数2Amy Takvorian合作论文数2Tricia L. Johnson合作论文数2Sherry Xu合作论文数2Ge Zhang合作论文数2Junying Wang合作论文数2Dasgupta Bireshwar合作论文数2Kasireddy-Polam Padmaja合作论文数2Tong Xinchun S合作论文数2Lanza Thomas J合作论文数2Jing Chen合作论文数2George L. Trainor合作论文数2William K. Hagmann合作论文数2Thaddeus F. Molski合作论文数2Argyrios G. Arvanitis合作论文数2John E. Macor合作论文数2Tung M. Fong合作论文数2Linus S. Lin合作论文数2Thais M. Sielecki合作论文数2D. Sloan Stribling合作论文数2Lauren P. Shearman合作论文数2Carolyn D. Dzierba合作论文数2James P. Jewell合作论文数2Shrenik K. Shah合作论文数2Andrew P. Combs合作论文数2
Alison Strack合作论文数2Paul J. Gilligan合作论文数2Quang Truong合作论文数2Kimberly Rosko合作论文数2Robert Zaczek合作论文数2Julie Lao合作论文数2Chun-Pyn Shen合作论文数2Grace Quaker合作论文数2Maria Rafalski合作论文数2Shikha Vig合作论文数2hyun o ok合作论文数1Feroze Ujjainwalla合作论文数1Helen M. Armstrong合作论文数1Jilly Evans合作论文数1Jane Lo合作论文数1Koppara Samuel合作论文数1Sookhee N Ha合作论文数1Heather L Sings合作论文数1John Menke合作论文数1Lex Van Der Ploeg合作论文数1Jonathan M Wilson合作论文数1Yue Feng合作论文数1
