A series of some 36 new imidazo[2,1-b] thiazoles (4a1-a6 to 4f1-f6) was synthesized involving multi-steps method starting from commercially available 2-aminothiazole (1). All the compounds were screened for antitubercular and antifungal activity. The compounds 4a1, 4a2, 4b3, 4b4, 4d5, and 4e4 with minimum inhibitory concentration (MIC) 1.6 mu g/mL displayed very good antitubercular and 4a2, 4b4, 4c4, and 4d2 displayed very good antifungal activity with MIC 25 mu g/mL. The few active molecules were subjected to molecular docking studies against three enzymes, pantothenate synthetase, enoyl-acyl carrier protein reductase (InhA), and aminoglycoside 2'-N-acetyltransferase of Mycobacterium tuberculosis (TB), which have been validated as effective anti-TB targets. [GRAPHICS] .