Published:  Jul 30, 2018DOI: 10.7324/JAPS.2018.8704
In the present designed work, we have synthesized imidazo[2,1-b][1,3,4]thiadiazole derivatives (6a1-a6 to 6d1-d6) by reaction of compound 3 with appropriate α-haloaryl ketones produce substituted imidazo thiadiazole derivatives (4a-d). In the next step, these compounds (4a–d) undergoes the Vilsmeier reaction to introduce formyl group on the substituted arylimidazo[2,1-b][1,3,4]thiadiazole derivatives to form carbaldehyde derivatives (5a–d) and finally in the last step of the reaction for the synthesis of designed molecules, a one-pot synthetic procedure was used. For this, the one-pot reaction of 5a–d, thiosemicarbazide and substituted α-haloaryl ketones were reacted together in different reaction condition in ethanol solvent at an optimum temperature around 80°C produces a corresponding derivatives (6a1-a6 to 6d1-d6) with a better yield. The IR, 1H-NMR, and mass spectroscopy techniques were used to confirm the structure of final products and all synthesized molecules were tested for anti-TB and anti-fungal activity. The compounds 6a1, 6a2, 6a3, 6c1, 6c6 and 6d1 with MIC 1.6-6.25 μgm/ml displayed very good antitubercular and 6a1, 6a4, 6a5, and 6d1 displayed very good antifungal activity with MIC 5 μgm/ml due to electron withdrawing groups at 4th position to both phenyl rings which are attached to the thiazole of the imidazo thiadiazole and imidazo thiadiazole ring.
Syed MA, Reddy YRP, Chandrasekhar KB. Design, One-pot Synthesis and Biological Evaluation of Imidazo[2,1-b] [1,3,4] Thiadiazole Derivatives for their Anti-Tubercular and AntiFungal Activity. J App Pharm Sci, 2018; 8(07): 021-027.
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