Application In Synthesis of 1H-1,2,4-Triazol-5-amine. In 2019.0 EUR J MED CHEM published article about ACETYLCHOLINESTERASE; INHIBITORS; PROTOCOL; NEURODEGENERATION; DISCOVERY; PEPTIDES; AGENTS; DRUGS; SITE in [Umar, Tarana; Hoda, Nasimul] Jamia Millia Islamia, Dept Chem, New Delhi 110025, India; [Shalini, Shruti; Gusain, Siddharth; Seth, Prerna; Tiwari, Manisha] Univ Delhi, Dr BR Ambedkar Ctr Biomed Res, New Delhi 110007, India; [Raza, Md Kausar] Indian Inst Sci, Dept Inorgan & Phys Chem, Bangalore 560012, Karnataka, India; [Kumar, Jitendra] Sardar Vallabhbhai Patel Coll, Dept Chem, Bhabua 821101, Kaimur, India; [Kumar, Jitendra] VKSU, Ara 802301, Bihar, India in 2019.0, Cited 65.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.
2-(piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides are described as a new class of selective and potent acetylcholinesterase (AChE) inhibitors and amyloid beta aggregation inhibitors. Formation of synthesized compounds (P1-P9) was justified via H-1 NMR, C-13 NMR, mass spectra and single crystal X-Ray diffraction study. All compounds were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity, inhibition of self-mediated A beta aggregation and Cu(II)-mediated A beta aggregation. Also, docking study carried out was in concordance with in vitro results. The most potent molecule amongst the derivatives exhibited excellent anti-AChE activity (IC50=4.8 nM). Kinetic study of P3 suggested it to be a mixed type inhibitor. In vitro study revealed that all the compounds are capable of inhibiting self-induced beta-amyloid (A beta) aggregation with the highest inhibition percentage to be 81.65%. Potency of P1 and P3 to inhibit self-induced A beta(1-)(42) aggregation was ascertained by TEM analysis. Compounds were also evaluated for their A beta disaggregation, antioxidation, metal-chelation activity. (C) 2019 Elsevier Masson SAS. All rights reserved.
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
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