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4-Substituted picolinohydrazonamides as a new class of potential antitubercular agents

descriptionPublicationkeyboard_double_arrow_right Article 01 Mar 2020 Poland English Publisher:Elsevier BVJournal:European Journal of Medicinal Chemistry, volume 190, page 112,106 (issn: 0223-5234,

Authors: Krzysztof Bojanowski; Danuta Siluk; Dagmara Ziembicka; Henryk Foks; Agnieszka Głogowska; Katarzyna Gobis; Izabela Korona-Glowniak; +2 Authors

doi: 10.1016/j.ejmech.2020.112106

pmid: 32061963

4-Substituted picolinohydrazonamides as a new class of potential antitubercular agents

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Abstract

The series of new 4-substituted picolinohydrazonamides were synthesized (6-25) and evaluated for tuberculostatic activity. Compounds having a hydrophilic cyclic amine such as morpholine and pyrrolidine at the end of the thiosemicarbazide chain, exhibited the highest antimycobacterial activity. The antimycobacterial activity of compounds 6, 11, and 15 (MIC 0.4-0.8 μg/mL) was higher than that of reference drugs. Moreover, derivative 15 exhibited lower activity against other tested microorganism such as bacteria gram-positive, gram-negative or fungi. Thus, this compound is characterized by the selectivity of antimicrobial activity. Antiproliferative study conducted against human dermal fibroblasts (HDF) and mouse melanoma cell line (B16-F10) revealed low cytotoxicity of compound 15. Conducted research allowed to identify compound 15 as leading for further research.

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Poland

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Keywords

Thiosemicarbazones, synthesis, Bacteria, Molecular Structure, Pyridines, Antitubercular Agents, Microbial Sensitivity Tests, thiosemicarbazide, Mice, tuberculosis, Yeasts, Animals, Humans, microscopic observation, cytotoxic activity

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