Studies on some new thiosemicarbazones as potential antitubercular agents

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Microbiology

Background:

• Tuberculosis remains a significant global health challenge, necessitating the development of novel therapeutic agents.
• Thiosemicarbazones are a class of organic compounds with a known history of exhibiting biological activities, including antimicrobial properties.

Purpose of the Study:

• To synthesize novel vanillin-4-aryl-3-thiosemicarbazone derivatives.
• To evaluate the in vitro antitubercular activity of the synthesized compounds against Mycobacterium tuberculosis.

Main Methods:

• Synthesis of 21 4-aryl-3-thiosemicarbazides and their corresponding vanillin-4-aryl-3-thiosemicarbazones.
• Antitubercular activity screening of five selected compounds against Mycobacterium tuberculosis strain H37 Ra using Löwenstein-Jensen medium.
• Characterization of compounds using Infrared (IR) spectroscopy and Thin-Layer Chromatography (TLC).

Main Results:

• Successful synthesis of 21 4-aryl-3-thiosemicarbazides and their vanillin-4-aryl-3-thiosemicarbazone derivatives in good yields.
• Identification of five vanillin-4-aryl-3-thiosemicarbazone derivatives exhibiting notable antitubercular activity.
• Confirmation of compound structures and purity through spectroscopic and chromatographic analyses.

Conclusions:

• The synthesized vanillin-4-aryl-3-thiosemicarbazones represent a promising scaffold for the development of new antitubercular drugs.
• Further investigation into the structure-activity relationship and mechanism of action of the active compounds is warranted.