Invited Speaker

Novel Pharmacophores from Natural Sources-Discovery Development
M. Iqbal Choudhary and Atta-ur-Rahman
Pakistan

The nature is full of surprises and wonders that not only fascinates and excites humanity but are important for the long term human survival. The most complex manifestation of the nature is in living organisms, each one of them contains a fascinating array of natural products. The unique structural features, novel biological activities and structural modifications of the natural products make them a potential candidate for new drugs

Natural product chemistry is the tool to discover the chemical diversity hidden in biodiversity. This is a science which explores unexpected chemical structures and unimaginable biological properties on daily basis. It is known that only a fraction of living organisms have been investigated for their bioactive chemicals. The journey of discovery of fascinating molecular leads is yet to begin and excitement of natural product chemistry is seemingly an endless voyage.

Pakistan and other developing nations have an unbroken traditions of the use of plants products as remedies in their folk systems of medicines. Based on these ethnomedicinal information, we selected several medicinal plants of Pakistan for bioassay-guided phytochemical investigations which resulted in the identification of a large number of bioactive constituents. These compounds were systematically screened for in vitro and in vivo biological activities by employing high-throughput and mechanism-based bioassay screenings and disease animal models. Several new classes of potent enzyme inhibitors of urease, α-glucosidase, acetyl- and butyryl-cholinesterases, phosphodiesterases, thymidine phosphorylase, lipoxygenase were discovered, along with novel and anti-epileptic agents.

These studies have resulted in the discovery of several classes of noval pharmacophores, which were then used to built libraries of analogues to study their structure-activity relationship. During this plenary presentation, underlying philosophy and results of these exciting studies will be presented.