Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.

Debnath Bhuniya,Rajendra K Kharul,Atul Hajare,Nadim Shaikh,Sandeep Bhosale,Sandip Balwe, Fouzia Begum,Siddhartha De, Sonalee Athavankar, Dhananjay Joshi,Vamsi Madgula, Kaushal Joshi,Amol A Raje,Ashwinkumar V Meru, Amol Magdum,Kasim A Mookhtiar, Rashmi Barbhaiya

Bioorganic & Medicinal Chemistry Letters（2019）

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摘要

•Novel scaffold as FAAH inhibitor with reversible mechanism of action.•Proof of MoA by recovery of active enzyme upon preincubation with inhibitor.•Synthesis via diastereomeric resolution of novel chiral dissymmetric intermediate.•Drug-like DMPK properties of Opt. Leads (−)-12l-m suitable for preclinical development.•Antihyperalgesic effects, in rat CIPN model at 3–30 mg/kg po dose.

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关键词

Fatty acid amide hydrolase (FAAH) inhibitors,Chemotherapy-induced peripheral neuropathy,Reversible mechanism of action,Diastereomeric resolution

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