An article Discovery ofN-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide: a novel, selective, and competitive indole-based lead inhibitor for human monoamine oxidase B WOS:000555606100001 published article about PARKINSONS-DISEASE; DERIVATIVES; SAFINAMIDE; TARGETS; OPTIMIZATION; SEMBRAGILINE; PHARMACOLOGY; MODELS; POTENT in [Elkamhawy, Ahmed; Lee, Kyeong; Pae, Ae Nim; Park, Ki Duk] Dongguk Univ Seoul, Coll Pharm, Goyang 10326, South Korea; [Elkamhawy, Ahmed] Mansoura Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Mansoura, Egypt; [Paik, Sora; Roh, Eun Joo] Korea Inst Sci & Technol KIST, Chem Kin Res Ctr, Seoul 02792, South Korea; [Kim, Hyeon Jeong; Park, Jong-Hyun; Londhe, Ashwini M.] Korea Inst Sci & Technol KIST, Convergence Res Ctr Diag Treatment & Care Syst De, Seoul, South Korea; [Kim, Hyeon Jeong] Yonsei Univ, Dept Biotechnol, Seoul, South Korea; [Londhe, Ashwini M.; Pae, Ae Nim; Park, Ki Duk; Roh, Eun Joo] Korea Univ Sci & Technol, KIST Sch, Div Biomed Sci & Technol, Seoul, South Korea; [Park, Ki Duk] Kyung Hee Univ, KHU KIST Dept Converging Sci & Technol, Seoul, South Korea in 2020, Cited 52. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. COA of Formula: C5H4N2O2
Herein, two new series ofN-substituted indole-based analogues were rationally designed, synthesizedviamicrowave heating technology, and evaluated as noteworthy MAO-B potential inhibitors. Compared to the reported indazole-based hitsVIandVII, compounds4band4eexhibited higher inhibitory activities over MAO-B with IC(50)values of 1.65 and 0.78 mu M, respectively. When compared to the modest selectivity index of rasagiline (II, a well-known MAO-B inhibitor, SI > 50), both4band4ealso showed better selectivity indices (SI > 60 and 120, respectively). A further kinetic evaluation of the most potent derivative (4e) displayed a competitive mode of inhibition (inhibition constant (K-i)/MAO-B = 94.52 nM). Reasonable explanations of the elicited biological activities were presentedviaSAR study and molecular docking simulation. Accordingly, the remarkable MAO-B inhibitory activity of4e(N-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide), with its selectivity and competitive inhibition, advocates its potential role as a promising lead worthy of further optimization.
About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Elkamhawy, A; Paik, S; Kim, HJ; Park, JH; Londhe, AM; Lee, K; Pae, AN; Park, KD; Roh, EJ or concate me.. COA of Formula: C5H4N2O2
Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem