Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. SDS of cas: 761446-44-0.
Remya, Chandran;Dileep, K. V.;Koti Reddy, Eeda;Mantosh, Kumar;Lakshmi, Kesavan;Sarah Jacob, Reena;Sajith, Ayyiliyath M.;Jayadevi Variyar, E.;Anwar, Shaik;Zhang, Kam Y. J.;Sadasivan, C.;Omkumar, R. V. research published 《 Neuroprotective derivatives of tacrine that target NMDA receptor and acetyl cholinesterase – Design, synthesis and biological evaluation》, the research content is summarized as follows. An novel high affinity multi-target directed ligands (MTDLs) against AChE and NMDAR, with reduced hepatotoxicity, performed in-silico structure-based modifications on tacrine, chem. synthesis of the derivatives and in-vitro validation of their activities. Nineteen such derivatives I [R = H, methylcarbamoyl, hydrazinecarbonyl, ethoxycarbonyl; R1 = 2-furanyl, 1-methylpyrazol-4-yl, 2-FC6H4, etc.] showed inhibition with IC50 values in the range of 18.53 ± 2.09 – 184.09 ± 19.23 nM against AChE and 0.27 ± 0.05 – 38.84 ± 9.64μM against NMDAR. Some of the selected compounds protected rat primary cortical neurons from glutamate induced excitotoxicity. Two of the tacrine derived MTDLs, I [R = H, R1 = 1-methylpyrazol-4-yl; R = H, R1 = 2-FC6H4] exhibited in-vivo efficacy in rats by protecting against behavioral impairment induced by administration of the excitotoxic agent, monosodium glutamate. Addnl., several of these synthesized compounds also exhibited promising inhibitory activitiy against butyrylcholinesterase. MTDL-201 I [R = H, R1 = 1-methylpyrazol-4-yl] was also devoid of hepatotoxicity in-vivo. Given the therapeutic potential of MTDLs in disease-modifying therapy, studies revealed several promising MTDLs among which I [R = H, R1 = 1-methylpyrazol-4-yl] appeared to be a potential candidate for immediate preclin. evaluations.
SDS of cas: 761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics