Hydrazone-Tethered 5-(Pyridin-4-yl)-4H-1,2,4-triazole-3-thiol Hybrids: Synthesis, Characterisation, in silico ADME Studies, and inâ
vitro Antimycobacterial Evaluation and Cytotoxicity.
ChemMedChem
; 18(6): e202200572, 2023 03 14.
Article
in English
| MEDLINE | ID: covidwho-2310186
ABSTRACT
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 inâ
vitro for their potential activity against Mycobacterium tuberculosis (MTB) H37 Rv strain. The most promising compound 13 - the derivative without the benzene ring appended to the pyrrole unit displayed acceptable activity (MIC90 =3.99â
µM) against MTB H37 Rv, while other compounds from the series exhibited modest to weak antimycobacterial activity with MIC90 values in the range between 7.0 and >125â
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.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Mycobacterium tuberculosis
/
Antitubercular Agents
Type of study:
Experimental Studies
Language:
English
Journal:
ChemMedChem
Journal subject:
Pharmacology
/
Chemistry
Year:
2023
Document Type:
Article
Affiliation country:
Cmdc.202200572
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