New Potential Pharmaceuticals with Cyclopenta[d]pyridazines and the COX-2 (Cyclooxygenase-2) Connection.
Institution
Morehead State University
Faculty Advisor/ Mentor
Mark Blankenbuehler
Abstract
The expanding need for new medical treatments for a variety of disorders has driven research to discover new organic compounds as potential pharmaceuticals. Many of the current compounds used include a heterocycle of sulfur, oxygen or nitrogen in the structure. Applications from possible anticancer treatments to "bleaching" herbicidal activity or non-steroidal anti-inflammatory drugs are being explored. The chemistry of the fused-pyridazine, cyclopenta[d]-pyridazine, is largely unexplored. The challenge is to synthesize cyclopenta[d]pyridazine based compounds that are similar to existing pyridazines or pyrazoles with known biological activity such as Celebrex. Celebrex selectively inhibits the COX-2 enzyme which allows for the reduction of inflammation without typical side effects from inhibition of the COX-1 enzyme. Parent pyridazine derivatives and fused-pyridazines are being synthesized. The synthesis and characterization of N-substituted cyclopenta [d]pyridazines structurally similar to Celebrex via reaction of an appropriate hydroxyfulvene with 4- hydrazinobenzenesulfonamide will be discussed.
New Potential Pharmaceuticals with Cyclopenta[d]pyridazines and the COX-2 (Cyclooxygenase-2) Connection.
The expanding need for new medical treatments for a variety of disorders has driven research to discover new organic compounds as potential pharmaceuticals. Many of the current compounds used include a heterocycle of sulfur, oxygen or nitrogen in the structure. Applications from possible anticancer treatments to "bleaching" herbicidal activity or non-steroidal anti-inflammatory drugs are being explored. The chemistry of the fused-pyridazine, cyclopenta[d]-pyridazine, is largely unexplored. The challenge is to synthesize cyclopenta[d]pyridazine based compounds that are similar to existing pyridazines or pyrazoles with known biological activity such as Celebrex. Celebrex selectively inhibits the COX-2 enzyme which allows for the reduction of inflammation without typical side effects from inhibition of the COX-1 enzyme. Parent pyridazine derivatives and fused-pyridazines are being synthesized. The synthesis and characterization of N-substituted cyclopenta [d]pyridazines structurally similar to Celebrex via reaction of an appropriate hydroxyfulvene with 4- hydrazinobenzenesulfonamide will be discussed.