Compounds bearing thiazole and chalcone pharmacophores have been reported to possess excellent antitubercular and anticancer activities. In view of this, we designed, synthesized and characterized a novel series of thiazole−chalcone hybrids (1–20) and further evaluated them for antitubercular and antiproliferative activities by employing standard protocols. Among the twenty compounds, chalcones 12 and 7, containing 2,4-difluorophenyl and 2,4-dichlorophenyl groups, showed potential antitubercular activity higher than the standard pyrazinamide (MIC = 25.34 µM) with MICs of 2.43 and 4.41 µM, respectively. Chalcone 20 containing heteroaryl 2-thiazolyl moiety exhibited promising antiproliferative activity against the prostate cancer cell line (DU-145), higher than the standard methotrexate (IC50 = 11 ± 1 µM) with an IC50 value of 6.86 ± 1 µM. Furthermore, cytotoxicity studies of these compounds against normal human liver cell lines (L02) revealed that the target molecules were comparatively less selective against L02. Additional computational studies using AutoDock predicted the key binding interactions responsible for the activity and the SwissADME tool computed the in silico drug likeliness properties. The lead compounds generated through this study, create a way for the optimization and development of novel drugs against tuberculosis infections and prostate cancer.

Oxidative stress is one of the common problems seen in a variety of diseases. Chalcones and in particular heteroaryl chalcones had reported with promising antioxidant activities. Hence, in the present work, we reported the antioxidant activity of twenty thiazole ring bearing chalcone derivatives (1-20). Among the tested compounds, compounds 17, 19 and 20 containing 2-pyridinyl, 3-pyridinyl and 2-thiazolyl scaffolds showed superior antioxidant activity than the standard with their IC50 values 4±1µg/mL, 3±1 µg/mL and 5±1 µg/mL respectively. The compound 19 is an interesting lead for the development of newer antioxidant agents.

In an effort to study the effect of 1,3,4-thidiazole based molecules on bacteria, fungal and tuberculosis species, we synthesized a series of Schiff bases (2a-2m) by reacting a variety of carbonyl compounds with 5-amino-1,3,4- thiadiazole-2-thiol. Molecular structure of these compounds was retrieved by spectral methods and elemental analysis. All these compounds were evaluated for their antibacterial, antifungal and antitubercular activities employing standard biological protocols. The compounds 2m and 2l substituted with the electron withdrawing fluorine and nitro groups showed excellent inhibitory activity against Staphylococcus aureus, Aspergillus niger and Candida tropicalis with an MIC of 8 µg/mL whereas 2i containing the electron releasing dimethylamino group showed potent activity against Proteus vulgaris. Additionally, 2m along with 2j, 2k and 2l also exhibited superior antimycobacterial activity than the standard pyrazinamide. The activity data for these compounds pave the way for the development of new antimicrobial and antitubercular drugs.

Design, synthesis and biological screening of 2,4-dichlorothiazole-5-carboxaldehyde derived chalcones as potential antitubercular and antiproliferative agents Design, synthesis and biological screening of 2,4-dichlorothiazole-5carboxaldehyde derived chalcones as potential antitubercular and antiproliferative agents