So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Qiao, Chang-Jiang; Ali, Hamed I.; Ahn, Kwang H.; Kolluru, Srikanth; Kendall, Debra A.; Lu, Dai researched the compound: Ethyl 5-chloro-3-formyl-1H-indole-2-carboxylate( cas:43142-76-3 ).Application of 43142-76-3.They published the article 《Synthesis and biological evaluation of indole-2-carboxamides bearing photoactivatable functionalities as novel allosteric modulators for the cannabinoid CB1 receptor》 about this compound( cas:43142-76-3 ) in European Journal of Medicinal Chemistry. Keywords: indole carboxamide preparation allosteric modulator; Allosteric modulator; Cannabinoid receptor; Photoactivatable ligands; Photoaffinity labeling. We’ll tell you more about this compound (cas:43142-76-3).
The compound 5-chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (ORG27569) is a prototypical allosteric modulator for the cannabinoid CB1 receptor. Based on this indole-2-carboxamide scaffold, a novel CB1 allosteric modulators that possess photoactivatable functionalities I (R = N3, N(CH3)2, piperidin-1-yl, etc.; R1 = N3CH2, C2H5, C5H11, etc.) has been designed and synthesized. To assess their allosteric effects, the dissociation constant (KB) and allosteric binding cooperativity factor (α) are determined and compared to their parent compds I (R = piperidin-1-yl, N(CH3)2; R1 = C2H5, n-C5H11, n-C6H13). With in this series, benzophenone-containing compounds I (R = (CO)C6H5; R1 = C2H5, n-C5H11, CH2N3), phenylazide-containing compound I (R = N3; R1 = n-C6H13), and the aliphatic azide containing compound I showed allosteric binding parameters (KB and α) comparable to their parent compound I (R = piperidin-1-yl, N(CH3)2; R1 = C2H5, n-C5H11, n-C6H13), resp. These modulators for their impact on G-protein coupling activity has been further assessed. Interestingly, these compounds exhibited neg. allosteric modulator properties in a manner similar to their parent compounds I, which antagonize agonist-induced G-protein coupling. These novel CB1 allosteric modulators, possessing photoactivatable functionalities, provide valuable tools for future photo-affinity labeling and mapping the CB1 allosteric binding site(s).
As far as I know, this compound(43142-76-3)Application of 43142-76-3 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.