《Design, microwave-assisted synthesis, biological evaluation and molecular modeling studies of 4-phenylthiazoles as potent fatty acid amide hydrolase inhibitors》 was written by Wilt, Stephanie R.; Rodriguez, Mark; Le, Thanh N. H.; Baltodano, Emily V.; Salas, Adrian; Pecic, Stevan. Application of 16629-19-9 And the article was included in Chemical Biology & Drug Design in 2020. The article conveys some information:
Endocannabinoids, anandamide (AEA) and 2-arachidonoylglycerol (2-AG), are endogenous lipids that activate cannabinoid receptors. Activation of these receptors produces anti-inflammatory and analgesic effects. Fatty acid amide hydrolase (FAAH) is a membrane enzyme that hydrolases endocannabinoids; thus, inhibition of FAAH represents an attractive approach to develop new therapeutics for treating inflammation and pain. Previously, potent rat FAAH inhibitors containing 2-naphthyl- and 4-phenylthiazole scaffolds were identified, but up to the present time, very little structure-activity relationship studies have been performed on these moieties. We designed and synthesized several analogs containing these structural motifs and evaluated their inhibition potencies against human FAAH enzyme. In addition, we built and validated a homol. model of human FAAH enzyme and performed docking experiments We identified several inhibitors in the low nanomolar range and calculated their ADME predicted values. These FAAH inhibitors represent promising drug candidates for future preclin. in vivo studies. In the experimental materials used by the author, we found Thiophene-2-sulfonyl chloride(cas: 16629-19-9Application of 16629-19-9)
Thiophene-2-sulfonyl chloride(cas: 16629-19-9) is a member of sulfonyl chlorides. Sulfonyl chlorides are reactive sulfonic acid derivatives similar in properties and reactivity to acid chlorides of carboxylates. The sulfonic acid group, however, is a highly hindered molecule, containing a tetrahedral configuration of substituents. Application of 16629-19-9
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics