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Synthesis and pharmacological properties of certain analogs of pilocarpine |
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| Authors: | Hassan Y. Aboul‐Enein S.E. Ibrahim A.A. Al‐Badr M. Ismail |
| Affiliation: | 1. Department of Pharmaceutical Chemistry and Department of Pharmacology, College of Pharmacy , King Saud University , Riyadh, 11451, Saudi Arabia;2. Drug Development Laboratory, Radionuclide and Cyclotron Operations Department , King Faisal Specialist Hospital and Research Centre , Riyadh, 11211, Saudi Arabia;3. Department of Research and Quality Control , Egyptian International Pharmaceutical Industrial Co. , Cairo, Egypt;4. Department of Pharmaceutical Chemistry and Department of Pharmacology, College of Pharmacy , King Saud University , Riyadh, 11451, Saudi Arabia |
| Abstract: | The synthesis of 4‐(4'‐pyrimidinylmethyl)oxacyclohexan‐2‐one (2a) and 4‐(4'‐pyrimidinylmethyl)oxacycloheptan‐2‐one (3a) were achieved through the Michael addition of the anion derived from 4‐methylpyrimidine with oxacyclyo‐3‐hexen‐2‐one and oxacyclo‐3‐hepten‐2‐one respectively. These compounds 2a and 3a and their quaternary methiodide salts lack cholinomimetic activity. |
| Keywords: | Pilocarpine analogs synthesis cholinergic activity structure‐activity relationships (SAR) receptor site |