Safa Fitouri, S. Mohamed, A. Sager, Z. Abood, S. Basheer, A. Gbaj, M. Al-Forgany, I. A. Mureema and S. M. Bensaber

National Medical Research Center, Zawia, Libya

Abstract:

Tuberculosis (TB) is the second leading cause of morbidity worldwide caused by a single infectious organism. There is an urgent need to find new Anti - TB that are efficacious, affordable and compatible with HIV and other Anti - TB used in developing countries, where the disease is prevalent. One such lead compound which may be developed to meet these criteria is thiolactomycin (TLM). This naturally occurring antibiotic has been shown to be active against M.tuberculosis by inhibiting the FAS II condensing enzymes mtFabH, KasA and KasB involved in mycolic acid biosynthesis. We thus embarked on a project to design and synthesize analogues of TLM, as new lead molecules for consideration as potential Anti - TB. Molecular modelling studies for all the targeted compounds was performed using AutoDock 4.2 program for rigid docking, and the obtained results indicated that this type of TLM analogues may have good activity in comparison with the lead TLM. The activity of the synthesized compounds against Mycobacteria tuberculosis indicated that compounds MCS16, MCS31, MCS37 and MCS40 are active as they inhibited the growth the Mycobacteria.