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Updated: Dec 28, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
4-Substituted picolinohydrazonamides as a new class of potential antitubercular agents
Malwina Krause1, Henryk Foks1, Dagmara Ziembicka1
1Department of Organic Chemistry, Medical University of Gdańsk, Gdańsk, Poland.
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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