2. Academic Validation
  3. NO-Donors, part 3: nitrooxyacylated thiosalicylates and salicylates - synthesis and biological activities(#)

NO-Donors, part 3: nitrooxyacylated thiosalicylates and salicylates - synthesis and biological activities(#)

  • Eur J Med Chem. 1999 Nov 1;34(11):895-901. doi: 10.1016/s0223-5234(99)00110-5.
S Endres 1,  A Hacker,  E Noack,  G Kojda,  J Lehmann
Affiliations

Affiliation

  • 1 Pharmazeutisches Institut, Rheinische Friedrich-Wilhelms-Universität Bonn, An der Immenburg 4, D-53121, Bonn, Germany
PMID: 10889315 DOI: 10.1016/s0223-5234(99)00110-5
Abstract

Organic nitrates release nitric oxide when incubated with thiosalicylic acid. S-Nitrooxyacylated esters and amides of thiosalicylic acid, together with the corresponding salicylates, were synthesized in order to perform a first in vitro evaluation of these new nitrate-thiol-hybrid prodrugs. These prodrugs might release NO in vivo after biotransformation without the use of endogenous reductives. None of these prodrugs released NO spontaneously when dissolved in buffer solution, but they did activate soluble guanylyl cyclase and induced vasodilatation of phenylephrine-pretreated male Wistar rat aorta in a potency range between that of isosorbiddinitrate and glycerole trinitrate.

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