Studies on new phosphodiesterase inhibitors. I. Synthesis of 1-(2,3-epoxypropoxy)-2(4)-fluorobenzenes and 1-(2-hydroxy-3-morpholinopropoxy and piperazino)fluorobenzene derivatives.
A series of 1-(2,3-epoxypropoxy)-2(4)-fluorobenzenes and their corresponding 1-(2-hydroxy-3-morpholinopropoxy and piperazino)fluorobenzene derivatives (8a--f) were synthesised via a short synthetic route in good chemical yields and were evaluated for inotropic and chronotropic activity in isolated guinea-pig atria preparation. The compounds act as potential phosphodiesterase (PDE) inhibitors with desirable biological activity and have considerable promise in heart therapy.
Baker
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NR
Division of Chemical and Biological Sciences, School of Natural and Environmental Sciences, Coventry University, England.
Byrne
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NG
Economides
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AP
Javed
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T
D000818:Animals; D004852:Epoxy Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D005464:Fluorobenzenes / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D009025:Morpholines / Q000138:chemical synthesis* / Q000494:pharmacology; D009200:Myocardial Contraction / Q000187:drug effects*; D010210:Papillary Muscles / Q000187:drug effects; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D017725:Ventricular Pressure / Q000187:drug effects
D004852:Epoxy Compounds; D005464:Fluorobenzenes; D009025:Morpholines; D010726:Phosphodiesterase Inhibitors; D010879:Piperazines