Synthesis of 1,2,3-triazole-piperazin-benzo[b][1,4]thiazine 1,1-dioxides: antibacterial, hemolytic and in silico TLR4 protein inhibitory activities.

ABSTRACT: In this study, we designed and synthesized a number of novel 1,2,3-triazole-piperazin-benzo[b][1,4]thiazine 1,1-dioxide derivatives and investigated their in vitro antibacterial and hemolytic activity. When compared to the lead chemical, dicloxacillin, the majority of the compounds demonstrated acceptable activity. Among them, the most promising compounds 6e, 6g, 6i, 8d, and 8e exhibited excellent antibacterial activity against the methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), and vancomycin-resistant S. aureus (VRSA) with MIC values of 1.56 ± 0.22 to 12.5 ± 1.75 μg mL^-1, respectively, The percentage of hemolysis ranged from 21.3 μg mL^-1 to 33.8 μg mL^-1. Out of the six compounds (6i, 6e,

SUBMITTER: Ramu N 

PROVIDER: S-EPMC10945376 | biostudies-literature | 2024 Mar

REPOSITORIES: biostudies-literature