B-973, a Novel ?7 nAChR Ago-PAM: Racemic and Asymmetric Synthesis, Electrophysiological Studies, and in Vivo Evaluation.
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ABSTRACT:
SUBMITTER: Garai S
PROVIDER: S-EPMC6231182 | biostudies-literature | 2018 Nov
REPOSITORIES: biostudies-literature
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B-973, a Novel α7 nAChR Ago-PAM: Racemic and Asymmetric Synthesis, Electrophysiological Studies, and <i>in Vivo</i> Evaluation.
Garai Sumanta S Raja Krishnamohan S KS Papke Roger L RL Deschamps Jeffrey R JR Damaj M Imad MI Thakur Ganesh A GA
ACS medicinal chemistry letters 20181011 11
We report here the total synthesis of B-973 (five steps), a recently identified α7 nAChR ago-PAM, its enantiomeric resolution, and its electrophysiological characterization in <i>Xenopus</i> oocytes to identify (-)-B-973B as the bioactive enantiomer. The asymmetric synthesis of B-973B was accomplished in 99% ee, and X-ray crystallography studies revealed its absolute "<i>S</i>" stereochemistry. B-973B was effective in attenuating pain behavior and decreasing paw edema (formalin test), and its an ...[more]
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