参考标题:Synthesis Of 1,2,3,Triazole Modified Analogues Of Hydrochlorothiazide Via Click Chemistry Approach And In-Vitro α-Glucosidase Enzyme Inhibition Studies 作者:Hina Siddiqui,M. A. A. Baheej,Saeed Ullah,Fazila Rizvi,Shazia Iqbal,Haroon M. Haniffa,Atia-Tul Wahab,M. Iqbal Choudhary |发布日期:2022.8 摘要:The Current Study Was Aimed To Discover Potent Inhibitors Of α-Glucosidase Enzyme. A 25 Membered Library Of New 1,2,3-Triazole Derivatives Of Hydrochlorothiazide (1) (Hctz, A Diuretic Drug Also Being Used For The Treatment Of High Blood Pressure) Was Synthesized Through Click Chemistry Approach. The Structures Of All Derivatives 2-26 Were Deduced By Ms, Ir, 1H-Nmr, And 13C-Nmr Spectroscopic Techniques. All The Compounds Were Found To Be New. Compounds 1-26 Were Evaluated For α-Glucosidase Enzyme Inhibition Activity. Among Them, 18 Compounds Showed Potent Inhibitory Activity Against α-Glucosidase With Ic50 Values Between 24 And 379 µm. α-Glucosidase Inhibitor Drug Acarbose (Ic50 = 875.75 +/- 2.08 μm) Was Used As The Standard. Kinetics Studies Of Compounds 6, 9, 11, 12, 15, 20, 23, And 24 Revealed That Only Compound 15 As A Mixed-Type Of Inhibitor, While Others Were Non-Competitive Inhibitors Of α-Glucosidase Enzyme. All The Compounds Were Found To Be Non-Cytotoxic When Checked Against Mouse Fibroblast 3T3 Cell Line.
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