Song, Kwang-Seop; Kim, Min Ju; Seo, Hee Jeong; Lee, Sung-Han; Jung, Myung Eun; Kim, Soo-Un; Kim, Jeongmin; Lee, Jinhwa published the artcile< Synthesis and structure-activity relationship of novel diarylpyrazole imide analogues as CB1 cannabinoid receptor ligands>, Category: amides-buliding-blocks, the main research area is diarylpyrazole imide derivative preparation CB1 cannabinoid receptor antagonist.
A myriad of research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant, I), a CB1 receptor antagonist, was discovered for an obesity treatment. In this research, extended series, based on the 1,5-diarylpyrazole template of rimonabant, was synthesized and tested for CB1 receptor binding affinity. In the present study, N-piperidinylcarboxamide group of rimonabant was replaced with the corresponding sulfonamide, imide, N-Me imide and methylenediamide, resp. The SAR studies to optimize the CB1 binding affinity led to the potent imide derivatives The in vivo efficacy test of a derivative II gave a promising result for this novel scaffold. In order to explore physicochem. properties (hydrophobic, steric and electronic) of the representative imide derivatives responsible for their CB1 receptor binding affinity, quant. structure activity relationship (QSAR) studies were performed. Hansch QSAR models, which were moderate in the explanation for SAR, were generated with hydrophobic, steric and electronic properties of substituents. Especially, the Taft Es-based parabolic model was obtained with the best correlation result (r 2 = 0.846).
Bioorganic & Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Category: amides-buliding-blocks.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics