Sam Ananthan, Ph.D.

Medicinal Chemist
Manager, CNS Discovery/Computational Chemistry
Southern Research Institute
2000 Ninth Avenue South
Birmingham, AL 35205
Phone: 205-581-2822
E-mail: ananthan@southernresearch.org

Biography

Dr. Ananthan obtained his Ph.D. in Synthetic Organic/Medicinal Chemistry in 1984 from Gujarat University, India, and received further postdoctoral training at the Ohio State University with Professor Donald T. Witiak. He joined Southern Research in 1987, where he is currently a Senior Research Scientist and Manager of Computational Chemistry and CNS Discovery Chemistry Groups. He is an Adjunct Professor of Chemistry in the University of Alabama at Birmingham (UAB) Department of Chemistry.

Dr. Ananthan's primary research interests include drug design, medicinal chemistry, organic synthesis, and application of computer-assisted methods. His research efforts involving the design and synthesis of potential drug candidates are targeted toward enzymes, membrane-bound receptors (GPCRs), ion channels and neurotransmitter transporters of the central nervous system. These research efforts are primarily supported by the National Institutes of Health (NIH) through investigator-initiated R01 grants and contracts. Dr. Ananthan also serves as a co-investigator on a number of projects and is involved in computational analysis and data-mining efforts associated with high-throughput screening (HTS) of molecular libraries for lead discovery and lead optimization.

He is a member of the American Chemical Society, the Society for Neuroscience, and the American Association of Pharmaceutical Scientists. He has played an active role in the Medicinal Chemistry Division of the American Chemical Society and has served as a member of the Long Range Planning Committee. He serves on the peer review panels of a number of medicinal chemistry journals and is a member of the Editorial Advisory Board of Central Nervous System Agents in Medicinal Chemistry and Recent Patents on CNS Drug Discovery. He has authored or co-authored more than 50 scientific publications and holds several patents.

Research Focus: Drug Design and Synthetic Medicinal Chemistry

Drug design and medicinal chemistry efforts span a range of targets, including G-protein coupled receptors (GPCRs), ion channels, and neurotransmitter transporters of the central nervous system. A current research focus involves the design, synthesis, and development of opioid ligands as novel analgesic agents. The pursuit of these efforts is based on emerging evidence indicating that compounds possessing mixed mu agonist/delta antagonist activities are likely to display analgesic activity devoid of tolerance, dependence, and gastrointestinal side effects. The design of novel ligands with these dual interaction profiles is guided by structure-based drug design strategies using homology models of the target receptors and by predictive 3D-QSAR (CoMFA) models developed using functional acidity data on a series of ligands possessing a morphinan scaffold.

In another project, drug design and synthetic efforts are directed toward the design and synthesis of antagonist or partial agonist ligands with high selectivity for dopamine D3 subtype of receptors. Rational drug design approaches using homology-based models of the dopamine D3 and D2 dopamine receptors are currently being explored to design compounds with improved binding affinity and selectivity toward the D3 subtype of receptors.

Also being pursued are efforts directed toward lead discovery and optimization of allosteric modulators of biogenic amine transporters (dopamine transporter, norepinephrine transporter and 5-hydroxytryptamine transporter) with the potential for therapeutic application in several CNS disorders, including addiction.

Publications