Yadav, Veena D.; Kumar, Lalan; Kumari, Poonam; Kumar, Sakesh; Singh, Maninder; Siddiqi, Mohammad I.; Yadav, Prem N.; Batra, Sanjay published the artcile< Synthesis and Assessment of Fused β-Carboline Derivatives as Kappa Opioid Receptor Agonists>, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde, the main research area is embryonic kidney cell kappa opioid receptor agonist cAMP; beta-carboline; kappa opioid receptor agonist; molecular modeling; nitrogen heterocycle; pain.
The synthesis of 5-formyl-6-aryl-6H-indolo[3,2,1-de][1,5] naphthyridine-2-carboxylates by reaction between 1-formyl-9H-β-carbolines and cinnamaldehydes in the presence of pyrrolidine in water with microwave irradiation is described. Pharmacophoric modification of the formyl group offered several new fused β-carboline derivatives, which were investigated for their κ-opioid receptor (KOR) agonistic activity. Two compounds 4 a and 4 c produced appreciable agonist activity on KOR with EC50 values of 46±19 and 134±9 nM, resp. Moreover, compound-induced KOR signaling studies suggested both compounds to be extremely G-protein-biased agonists. The analgesic effect of 4 a was validated by the increase in tail flick latency in mice in a time-dependent manner, which was completely blocked by the KOR-selective antagonist norBNI. Moreover, unlike U50488, an unbiased full KOR agonist, 4 a did not induce sedation. The docking of 4 a with the human KOR was studied to rationalize the result.
ChemMedChem published new progress about Alkenes Role: BUU (Biological Use, Unclassified), BIOL (Biological Study), USES (Uses). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary