Structure-activity relationship on our recently reported triaryl bis-sulfone class of cannabinoid-2 (CB2) receptor selective inverse agonists was explored. Modifications to the methane sulfonamide, substitutions to B and C phenyl rings, and replacements of the C-ring were investigated. A compound with excellent CB2 activity, selectivity for CB2 over CB1, and in vivo plasma levels was identified.
Die Synthese der im Titel genannten Verbindungen (III) durch Kondensation der 8‐Aminopurine (I) mit den Malonsäureestern (II) bzw. durch spezifische 7‐Alky ie‐ rung der Tricyclen (IV) wird beschrieben.
Shing-Chun Wong合作论文数2Martin S. Domalski合作论文数1J. M. Hilbert合作论文数1David J. Conn合作论文数1Bb Shankar合作论文数1Joseph A Kozlowski合作论文数1L. Lehman Verbiar合作论文数1Jj Kaminski合作论文数1Stuart W. Mccombie合作论文数1
Andrew T. Mcphail合作论文数Duke University;Trinity College of Arts & Sciences1D. M. Solomon合作论文数1Marvin I. Siegel合作论文数1Brian J. Lavey合作论文数1
Charles Lunn合作论文数1David J. Blythin合作论文数1P. J. S. Chiu合作论文数1Jie Wu合作论文数1Guowei Zhou合作论文数1Michael K.C. Wong合作论文数1Razia Rizvi合作论文数1De-Yi Yang合作论文数1Arthur S. Watnick合作论文数1Loretta A. Bober合作论文数1Ronald L. Wolin合作论文数1Neng-Yang Shih合作论文数WuXi AppTec1
