Abstract:
The rise in cases of tuberculosis worldwide fuelled by the HIV/Aids pandemic highlights the need for new
drugs that can shorten the duration of treatment, effectively treat MDR and XDR TB and be non interactive
with available HIV/Aids treatment drugs. Fourty ethnobotanically selected phytocompounds and four
conventional TB treatment drugs were screened for their in vitro inhibitory activity against two strains of
Mycobacterium tuberculosis at the Central Reference Laboratory for TB (CRL) in Nairobi using the absolute
concentration method at concentrations ranging from 0.05 to 120μg/ml. Compounds with better minimum
inhibitory concentrations (MIC), than that of any of the four conventional TB treatment drugs, were identified
as promising Leads. The study identified six promising Leads; three benzoquinones (114, 121 and 116), a
flavone (141) an isoflavone (145) and an alkaloid (151). Structure activity relationships (SARs) and
Quantitative structure activity relationships (QSARs) were generated for the flavonoid and the benzoquinone
series members. QSARs were used in the prediction of structural modifications necessary for activity
improvement and in the prediction of activity of untested compounds.
