Recently I am researching about PARKINSONS-DISEASE; DERIVATIVES; SAFINAMIDE; TARGETS; OPTIMIZATION; SEMBRAGILINE; PHARMACOLOGY; MODELS; POTENT, Saw an article supported by the KIST Institutional Programs from Korea Institute of Science and Technology [2E30240]; Creative Fusion Research Program through the Creative Allied Project – National Research Council of Science Technology [CAP-12-1-KIST]; National Research Foundation of Korea (NRF) – Korea Government (MSIT) [NRF-2018R1A5A2023127, NRF-2018M3A9C8016849]; Korea Institute of Science and Technology (KIST)Korea Institute of Science & Technology (KIST). Application In Synthesis of Pyrazine-2-carboxylic acid. Published in TAYLOR & FRANCIS LTD in ABINGDON ,Authors: Elkamhawy, A; Paik, S; Kim, HJ; Park, JH; Londhe, AM; Lee, K; Pae, AN; Park, KD; Roh, EJ. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid
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.
Application In Synthesis of Pyrazine-2-carboxylic acid. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.
Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem