Our laboratory participates in multidisciplinary drug/probe discovery programs which include efforts in the areas of neurodegenerative tauopathies (in collaboration with the Center for Neurodegenerative Diseases Research – CNDR – at University of Pennsylvania) and parasitic infections (in collaboration with the Center for Discovery and Innovation in Parasitic Diseases – CDIPD – at UCSD).
Examples of completed and ongoing research include the discovery and development of (a) tau aggregation inhibitors [e.g., Bioorg. Med. Chem., 2012, 20, 4451–61]; (b) CNS-active microtubule-stabilizing agents [e.g., see J. Med. Chem., 2014, 57(14), 6116- 27 and ChemMedChem. 2018 09 06; 13(17), 1751-1754]; (c) thromboxane A2 receptor antagonists [e.g., see ACS Chem. Neurosci., 2012, 3(11): 928-40]; and (d) multi-targeted inhibitors of eicosanoid biosynthesis [e.g., see J. Med. Chem., 2017, 60(12), 5120-45].
Finally, our group is also actively involved in the investigation of basic, fundamental principles in medicinal chemistry, especially in the area of isosteric replacements [e.g., see J. Med. Chem., 2016, 59(7), 3183- 203].
CNS-active triazolopyrimidine stabilizes microtubule in vitro and in vivo
Small molecule polypharmacology as a possible strategy to treat Alzheimer’s disease
Characterization and development of novel surrogate structures of the carboxylic acid functional group with potential utility in drug design.