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Dr. John Boulos
Synthesis of Selective Muscarinic Agonists for Alzheimer's Application

Research Objectives

The main objective of this research is to involve both chemistry and biology students at Barry University with synthetic organic research. The specific aims of the research project are:

  1. To design and synthesize M1 selective muscarinic agonists. Series of heterocyclic compounds are being synthesized and tested based upon a theoretical model of the structural requirements for muscarinic receptor activity. The compounds are intended as mimics of acetylcholine and other cholinergic agonists at muscarinic receptors in the brain. Muscarinic M1 receptors are currently therapeutic targets for the symptomatic treatment of Alzheimer's disease.
  2. To obtain information about the muscarinic pharmacophore by synthesizing analogs of pilocarpine, a partial muscarinic agonist currently in use to treat glaucoma.
  3. To determine the binding affinity, receptor selectivity and intrinsic cellular activity of the test compounds at muscarinic m1-m5 receptor subtypes expressed in recombinant CHO cells.

Publications

  1. Synthesis of Furanyl and Oxazolyl N- Substituted Piperidine and Imidazoline Salts as Potential Agonists of M1 muscarinic receptors. J. Heterocyclic. Chem., 44, 1, December 2007.
  2. Synthesis of Oxazolyl-Substituted Morpholinium Salts, J. Heterocyclic Chem., 43, 1, 2006.
  3. Soluble protein, Molar C:N Ratio, and Amino acid Composition in Green vs. Decayed Seagrass Leaves, Florida scientist, 68, 1, 2005.
  4. Synthesis of Oxazolyl- and Furanyl- Substituted Imidazole Hydrochlorides and Methiodides, J. Heterocyclic Chem., 35, 859, 1998.

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