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Autor:
Kia Sepassi, Xiahou Deng, Brad M. Savall, Wall Jessica L, Nicholas I. Carruthers, Hong Ao, Anindya Bhattacharya, Brian Lord, Michael A. Letavic, Tatiana Koudriakova, Kevin J. Coe, Anita Everson, Freddy Schoetens, Devin M. Swanson, Meri De Angelis, Brian Scott, Timothy W. Lovenberg, Jason C. Rech, Judith Skaptason, Qi Wang
Publikováno v:
Journal of Medicinal Chemistry. 59:8535-8548
The synthesis and SAR of a series of 4,5,6,7-tetrahydro-imidazo[4,5-c]pyridine P2X7 antagonists are described. Addressing P2X7 affinity and liver microsomal stability issues encountered with this template afforded methyl substituted 4,5,6,7-tetrahydr