Rearrangement of the decalin system of pravastatin under S N 2 0 Mitsunobu conditions and subsequent selective hydrolysis and oxidation afforded a key dienone 23, which upon copper-catalyzed addition of a 1E-propenyl moiety established the carbon framework of BB-476 3 in high diastereomeric excess.
Therapeutic efficacy of the HMG-CoA-reductase inhibitor pravastatin in hyperlipoproteinaemia type II
β Scribed by H. Saxenhofer; P. Weidmann; W. F. Riesen; C. Beretta-Piccoli; C. Fragiacomo; R. Wunderlin; G. Noseda
- Publisher
- Springer
- Year
- 1990
- Tongue
- English
- Weight
- 533 KB
- Volume
- 39
- Category
- Article
- ISSN
- 0031-6970
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β¦ Synopsis
The efficacy and safety of the HMG-CoA-reductase inhibitor pravastatin was assessed in a double-blind, placebo controlled study. Thirty patients (51 y) with hyperlipoproteinaemia Type IIa (N = 22) or IIb (N = 8) received for 16 weeks either pravastatin 5 mg b.d. for 8 weeks followed by 10 mg b.d. for 8 weeks (Group I), or 10 mg b.d. for 8 weeks followed by 20 mg b.d. to 16 weeks (Group II), or placebo (Group III). In Groups I and II, mean serum total cholesterol was reduced by -26% and -22%, respectively; low-density lipoprotein (LDL)-cholesterol decreased by -28% and -27%, apolipoprotein B by -25% and -23%, and apolipoprotein E by -9% (NS) and -16%, respectively. Serum high-density lipoprotein (HDL)-cholesterol was increased by 11% in Group II, and so the total/HDL-cholesterol ratio fell by 33%. Apoprotein A1 and A2 were not significantly changed. No serious clinical and laboratory abnormalities were observed. The data suggest considerable therapeutic efficacy of pravastatin in the treatment of Type II hyperlipoproteinaemia.
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