DEUTERATED ANALOGS OF VERAPAMIL AND NIFEDIPINE - SYNTHESIS AND BIOLOGICAL-ACTIVITY

Citation
D. Rampe et al., DEUTERATED ANALOGS OF VERAPAMIL AND NIFEDIPINE - SYNTHESIS AND BIOLOGICAL-ACTIVITY, European journal of medicinal chemistry, 28(3), 1993, pp. 259-263
Citations number
18
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
28
Issue
3
Year of publication
1993
Pages
259 - 263
Database
ISI
SICI code
0223-5234(1993)28:3<259:DAOVAN>2.0.ZU;2-N
Abstract
The preparations of various deuterium analogs of verapamil and nifedip ine have been described. Deuterium is incorporated at specific positio ns in the molecules in 97% isotopic purity. The deuterated analogs 1d of verapamil and 2d of nifedipine lowered blood pressure in spontaneou sly hypertensive rats with a profile that was, for the most part. simi lar to the parent compounds. It was therefore concluded that deuterium substitutions fail to significantly alter the metabolism of verapamil or nifedipine in vivo.