The Front Cover shows new macrocyclic plasmin inhibitors containing a C-terminal P1 benzylamine group. Their N-terminal substitution provided analogues with sub-nanomolar K i values. Additional inhibitors containing an as...
Hydrazone‐Tethered 5‐(Pyridin‐4‐yl)‐4H‐1,2,4‐triazole‐3‐thiol Hybrids: Synthesis, Characterisation, in silico ADME Studies, and in vitro Antimycobacterial Evaluation and Cytotoxicity
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A small set of hydrazone-linked arylpyrrole-1,2,4-triazole compounds was synthesised and evaluated against Mycobacterium tuberculosis. The most promising compound, the derivative without the benzene ring appended to the pyrrole unit, displayed acceptable activity (MIC90=3.99 μM) against MTB H37Rv.
Compounds containing arylpyrrole-, 1,2,4-triazole- and hydrazone structural frameworks have been widely studied and demonstrated to exhibit a wide range of pharmacological properties. Herein, an exploratory series of new 1,2,4-triazole derivatives designed by amalgamation of arylpyrrole and 1,2,4-triazole structural units via a hydrazone linkage is reported. The synthesised compounds were tested in vitro for their potential activity against Mycobacterium tuberculosis (MTB) H37Rv strain. The most promising compound 13 – the derivative without the benzene ring appended to the pyrrole unit displayed acceptable activity (MIC90=3.99 μM) against MTB H37Rv, while other compounds from the series exhibited modest to weak antimycobacterial activity with MIC90 values in the range between 7.0 and >125 μM. Furthermore, in silico results, predicated using the SwissADME web tool, show that the prepared compounds display desirable ADME profile with parameters within acceptable range.Zum Volltext
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