Application In Synthesis of 1H-1,2,4-Triazol-5-amine. Recently I am researching about DRUG; 5-ENE-4-THIAZOLIDINONES; INHIBITORS; DESIGN; AGENTS; ASSAY, Saw an article supported by the . Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Holota, S; Kryshchyshyn, A; Derkach, H; Trufin, Y; Demchuk, I; Gzella, A; Grellier, P; Lesyk, R. The CAS is 61-82-5. Through research, I have a further understanding and discovery of 1H-1,2,4-Triazol-5-amine
A series of novel 2-(5-aminomethylene-4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropionic acid ethyl esters has been synthesized. Target compounds were evaluated for their trypanocidal activity towards Trypanosoma brucei brucei and Trypanosoma brucei gambiense. Several hit-compounds (8, 10, 12) inhibited growth of the parasites at sub-micromolar concentrations (IC50 0.027-1.936 mu M) and showed significant selectivity indices (SI= 108-1396.2) being non-toxic towards the human primary fibroblasts. The screening of anticancer activity in vitro within NCI DTP protocol allowed to identify active 2-(5-{[5-(2,4-dichlorobenzyl)-thiazol-2-ylamino]methylene}- 4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropionic acid ethyl ester 14 that demonstrated inhibition against all 59 human tumor cell lines with the average GI(50) value of 2.57 mu M. It was established that the activity type (antitrypanosomal or anticancer) as well as its level depends on the character of enamine fragment in the C5 position of thiazolidinone core.
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics