SYNTHESIS OF A SERIES OF HEXITOL AND AMINODEOXYHEXITOL MONONITRATE DERIVATIVES CONTAINING A SULFUR GROUP AND PHARMACOLOGICAL EVALUATION ON ISOLATED RAT AORTAS
Jp. Nallet et al., SYNTHESIS OF A SERIES OF HEXITOL AND AMINODEOXYHEXITOL MONONITRATE DERIVATIVES CONTAINING A SULFUR GROUP AND PHARMACOLOGICAL EVALUATION ON ISOLATED RAT AORTAS, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, (5), 1998, pp. 933-943
As part of our research into new organic nitrates for the treatment of
angina pectoris, we have investigated a series of hexitol and aminode
oxyhexitol mononitrate derivatives containing a sulfur group. Since th
e depletion of tissue stores of sulfhydryl groups appears to play an i
mportant role in the development of this phenomenon, the addition of a
sulfur group to a nitrate derivative could prevent the development of
nitrate tolerance during a long-term treatment. Before studying the d
uration of action, and the possible influence on tolerance phenomenon,
it was important to check the vasorelaxing effects of our compounds c
ompared to those of commercial organic nitrates of similar structures
such as isosorbide mononitrate or isosorbide dinitrate. All the compou
nds were tested on isolated rat aortas; some of these products exhibit
ed an interesting activity.