Drug Discovery in Preclinical Research (Track)


Asaad Khalid Ahmed

Medicinal and Aromatic Plants Research Institute, National Center for Research, P.O. Box: 2404, Khartoum-11111, Sudan


Just like Eldorado (legendary lost city of gold), the road to the discovery of successful drug from medicinal plants could be packed with challenges and adventures. The myriad of structurally diverse compounds found in nature makes them play an important role as a unique source for drug discovery, but they often skillfully play Hide-and-seek and/or hard-to-get. Even though, most of the FDA approved drugs are either natural products or natural product-derived compounds. Natural products are characterized by its unorthodox and often unanticipated chemical structures that offer novel leads of clinically useful drugs. Studies have demonstrated that the hit rate of natural products is on average 3-10%, compared with ~ 0.03% of that of compounds from synthetic origin [2,3].

Drug discovery could follow any of the two approaches i.e. cell-based and/or target-based. Enzymes represent the major class of drug targets. Recent reports show that about 50% of small molecule drugs are enzyme inhibitors [1].

This lecture will give an overview of our research on the inhibition of neglected diseases-related enzymes. Our cell-based research will also be highlighted. This research has led to the identification of very interesting anti-mycobacterium properties of some Sudanese medicinal plants.


[1]        Copeland, R. A. 2005. Evaluation of enzyme inhibitors in drug discovery: a guide for medicinal chemists and pharmacologists. John Wiley & Sons, Inc., Hoboken, N.J

[2]        Kinghorn AD. In: Gullo V, editor. The Discovery of Natural Products with Therapeutic Potential. Stoneham: Butterworth-Heinemann; 1994. p. 81-108.

[3]        Koch MA, Wittenberg LO, Basu S, Jeyaraj DA, Gourzoulidou E, Reinecke K, et al. Compound library development guided by protein structure similarity clustering and natural product structure. Proc Natl Acad Sci U S A 2004;101(48):16721-6.