Synthesis and structure-activity relationship of naphtho[1,2-b]furan-2-carboxamide derivatives as melanin concentrating hormone receptor 1 antagonists was written by Lim, Chae Jo;Choi, Jun Young;Lee, Byung Ho;Oh, Kwang-Seok;Yi, Kyu Yang. And the article was included in Chemical & Pharmaceutical Bulletin in 2013.Category: bromides-buliding-blocks This article mentions the following:
Synthesis and structure-activity relationship of naphtho[1,2-b]furan-2-carboxamides I (n = 2-5; R = H, Br, Ph, 4-MeC6H4, 3-ClC6H4, 2-pyridyl, 3-furyl, 3-thienyl, etc.) containing linked piperidinylphenylacetamide groups as melanin concentrating hormone receptor 1 (MCH-R1) antagonists are described. The structure activity relationship (SAR) study, probing members of this family that contain a variety of aryl and heteroaryl groups at C-5 of I skeleton and having different chain linker lengths, led to the identification of the 5-(4-pyridinyl)-substituted analog I (n = 2; R = pyridin-4-yl) as a highly potent MCH-R1 antagonist with an IC50 value of 3nM. This compound also displayed excellent metabolic stability and did not significantly inhibit cytochrome P 450 (CYP450) enzymes. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Category: bromides-buliding-blocks).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Category: bromides-buliding-blocks
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary