136539-67-8Relevant articles and documents
Syntheses of 3-arylphenols from (3-aryl-3-oxopropyl)dialkylammonium chlorides and 1-(2-Oxopropyl)pyridinium chloride
Eichinger,Nussbaumer
, p. 663 - 664 (1991)
The reactions of (3-aryl-3-oxopropyl)dialkylammonium chlorides 1a-f with 1-(2-oxopropyl)pyridinium chloride (2) and triethylamine gave the 3-arylphenols 3a-f with yields from 43 to 83%.
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution
Nguyen, Thuy,German, Nadezhda,Decker, Ann M.,Langston, Tiffany L.,Gamage, Thomas F.,Farquhar, Charlotte E.,Li, Jun-Xu,Wiley, Jenny L.,Thomas, Brian F.,Zhang, Yanan
, p. 7410 - 7424 (2017/09/22)
Allosteric modulators of the cannabinoid CB1 receptor have recently been reported as an alternative approach to modulate the CB1 receptor for therapeutic benefits. In this study, we report the design and synthesis of a series of diarylureas derived from PSNCBAM-1 (2). Similar to 2, these diarylureas dose-dependently inhibited CP55,940-induced intracellular calcium mobilization and [35S]GTP-γ-S binding while enhancing [3H]CP55,940 binding to the CB1 receptor. Structure-activity relationship studies revealed that the pyridinyl ring of 2 could be replaced by other aromatic rings and the pyrrolidinyl ring is not required for CB1 allosteric modulation. 34 (RTICBM-74) had similar potencies as 2 in all in vitro assays but showed significantly improved metabolic stability to rat liver microsomes. More importantly, 34 was more effective than 2 in attenuating the reinstatement of extinguished cocaine-seeking behavior in rats, demonstrating the potential of this diarylurea series as promising candidates for the development of relapse treatment of cocaine addiction.
Cyclohexylcarbamic acid 3′- or 4′-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: Synthesis, quantitative structure-activity relationships, and molecular modeling studies
Mor, Marco,Rivara, Silvia,Lodola, Alessio,Plazzi, Pier Vincenzo,Tarzia, Giorgio,Duranti, Andrea,Tontini, Andrea,Piersanti, Giovanni,Kathuria, Satish,Piomelli, Daniele
, p. 4998 - 5008 (2007/10/03)
Fatty acid amide hydrolase (FAAH) is a promising target for modulating endocannabinoid and fatty acid ethanolamide signaling, which may have important therapeutic potential. We recently described a new class of O-arylcarbamate inhibitors of FAAH, includin