Abstract:
:The structure of fenoterol, a beta2-adrenoceptor agonist used in therapy, has been joined with furoxan NO-donor moieties to give new NO-donor beta2-agonists. The furazan analogues, devoid of the property to release NO, were also synthesized for comparison. All the compounds retained beta2-agonistic activity at micromolar or submicromolar concentration when tested on guinea pig tracheal rings precontracted with carbachol. Among the furoxan derivatives, the NO contribution to trachea relaxation was evident with product 15b at micromolar concentrations. All the new NO-donor hybrids were able to dilate rat aortic strips precontracted with phenylephrine. Both furoxan and furazan derivatives displayed antioxidant activity greater than that of fenoterol.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Buonsanti MF,Bertinaria M,Stilo AD,Cena C,Fruttero R,Gasco Adoi
10.1021/jm0704595subject
Has Abstractpub_date
2007-10-04 00:00:00pages
5003-11issue
20eissn
0022-2623issn
1520-4804journal_volume
50pub_type
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