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Novel series of 1,3,4-thiadiazole and piperazine substituted quinazoline derivatives have been designed, synthesized, and tested  in vitro  for antimycobacterial activity. The synthetic procedure involved Suzuki C-C cross-coupling on a quinazoline ring and subsequently by the formation of 1,3,4-thiadiazole based piperazines. Many synthesized analogs were observed active against  Mycobacterium  H37Rv strain in preliminary analysis using the BACTEC MGIT method. A secondary antimycobacterial assay using the Lowenstein-Jensen MIC method indicates that bromo ( 7c ), trifluoromethyl ( 7f ), and hydroxy ( 7 h ) groups substituted analogs have shown strong efficacy in the range of 3.12–6.25 µg/mL. Active compounds were also tested for their cytotoxic activity against Human cervical (HeLa) cells at their MICs. The synthesized analogs were analyzed by IR, 1H NMR, 13 C NMR, MS, and elemental analysis for their structure determination.

Development of 1,3,4-Thiadiazole and Piperazine Fused Hybrid Quinazoline Derivatives as Dynamic Antimycobacterial Agents