DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME TRIAZOLE SCHIFF'S
BASE DERIVATIVES AS POTENTIALS ANTI – TUBERCULAR AGENTS
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
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.