Tailoring of novel morpholine-sulphonamide linked thiazole moieties as dual targeting DHFR/DNA gyrase inhibitors: synthesis, antimicrobial and antibiofilm activities, and DFT with molecular modelling studies
Moaz M. Abdou, Essam M. Eliwa, Mohamed Ahmed Mahmoud Abdel Reheim, Ahmed Abu‐Rayyan, Shimaa M. Abd El‐Gilil, Mohammed Abu‐Elghait, Mohamed H. Sharaf, Mohamed H. Kalaba, Ahmed H. Halawa, Walid E. Elgammal
Abstract
Herein, the chemical synthesis of new thiazole-based benzenesulfonamide-linked morpholine 4a,b–7 via late-stage thiazolation of the corresponding thiosemicarbazone 3 is reported.
Topics & Concepts
ChemistryMorpholineThiazoleDNA gyraseSemicarbazoneAntimicrobialCombinatorial chemistryThioamideSulfonamideStereochemistryBiochemistryEscherichia coliMedicinal chemistryOrganic chemistryGeneSynthesis and biological activitySynthesis and Catalytic ReactionsSynthesis and Biological Evaluation