Synthesis and anti-microbial studies of new series of 1,2,3,4-tetrazole integrated thieno[2,3-d]pyrimidine derivatives

The present study describes synthesis of a novel series of 1,2,3,4-tetrazole integrated thieno[2,3-d]-pyrimidine hybrid 11a-l. Further, in vitro anti-microbial activities of the synthesized analogues 11a -l were evaluated against Gram-positive bacteria and Gram-negative bacteria, and fungal pathogens respectively. As a result, the analogues 11d and 11l were shown potent anti-bacterial activities 0.09-0.48 mu g/mL and 0.07-0.51 mu g/mL, respectively against tested pathogens and compared with standard Ciprofloxacin (0.08-0.34 mu g/mL). As well, the compounds 11 h and 11l have also shown highest inhibition zones (ZOIs) ranging from 13.20 +/- 0.57 to16.70 +/- 0.50; and 17.00 +/- 0.00 to 17.50 +/- 1.04 mm, respectively against nominated fungal pathogens. Subsequently, the conducted molecular docking studies with the active site of DNA gyrase of Staphylococcue aureus and Esterase of Aspergillus niger were shown that all the synthesized derivatives 11a -l exhibited good docking scores of between-9.2 and-8.8 kcal/mol and were better as compared with standard drugs.