Michaela SerpiARWA MOUSA MOHAMMED ALGHAMDI2022-05-292022-05-29https://drepo.sdl.edu.sa/handle/20.500.14154/50051Background: Antibiotic resistance is currently considered as a serious global threat of a growing concern to not only human health but also to animal and environmental health. Antibiotic resistance has limited the benefit of currently available antibiotic agents. The need for the development of a novel class of antibiotics that is not discovered by bacteria yet is undoubted. Lipoteichoic acid (LTA) is one of the promising newly discovered drug target. It is a cell wall polymer found in gram-positive bacteria. It has been reported that it contributes to bacterial homeostasis and virulence. LTA is synthesized by the activity of Lipoteichoic acid synthase enzyme (LtaS). Mutants of LtaS showed defects in the growth of the bacteria. Till date, compound 1771 is the first developed LtaS inhibitor to target gram positive bacteria. Aim and Objectives: to develop a more stable and effective analogues of compound 1771 an inhibitor of a novel drug target, Lipoteichoic acid synthase enzyme (LtaS) that target gram-positive bacteria. Methodology: Analogues of compound 1771, a LtaS inhibitor, will be designed, synthesized and analysed along with in-silico pharmacokinetic testing. Results: We were able to design three analogues of compound 1771: AM06, AM07 and AM08. The designed compound were tested in-silico for pharmacokinetic properties. Among the three designed compounds, AM06 and AM08 were successfully synthesized and confirmed by 1H, 13C, 19F-NMR and LR-MS.en