Structural Optimization of the Diarylurea PSNCBAM-1, an Allosteric Modulator of Cannabinoid Receptor 1

ConclusionsIn contrast to PSNCBAM-1, the synthesized compounds are analogs with fewer rings. The compounds LDK1317 (12a) and LDK1321 (6a) contained only 2 or 3 rings, respectively, and showed the binding parameters (KB = 110 nM, α = 2.3, and KB = 85 nM, α = 5.9). Further, the computationally predicted drug-like properties and solubility suggest these compounds are acceptable new lead compounds for further development of CB1 allosteric modulators.

Source: Current Therapeutic Research - December 25, 2019 Category: Drugs & Pharmacology Source Type: research