Pyrimidine derivatives. 4. Synthesis and antihypertensive activity of 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives
摘要:
A series of 30 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives was prepared and tested for their ability to reduce blood pressure in conscious, spontaneously hypertensive rates (SHR). A number of these compounds, notably 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazolines 3a (R1 = H; R2 = Ph), 3j (R1 = H; R2 = 4-EtOPh), and 5a (R1 = H; R2 = 2-furyl), showed activity at oral doses of 0.3-10 mg/kg. The effects of the 4-substituents of the piperazino group on activity are discussed. Compounds 3a, 3j, and 5a were effective in renal hypertensive rats at oral doses of 3 and 10 mg/kg and showed alpha-adrenoceptor blocking effects in isolated aortas of rats. A 5-day consecutive oral administration of 3a and 3j in SHR did not lead to development of tolerance.
A highly efficient iridium-catalyzedhydrogenation of alpha,beta-unsaturated carboxylic acids has been developed by using chiral spiro-phosphino-oxazoline ligands, affording alpha-substituted chiral carboxylic acids in exceptionally high enantioselectivities and reactivities.
Furopyridine sulfonamides and their opthalmological compositions
申请人:Merck & Co., Inc.
公开号:US04808595A1
公开(公告)日:1989-02-28
Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.
Furopyridine磺酰胺是一种碳酸酐酶抑制剂,可用于治疗眼内压升高及其相关的疾病,如青光眼。
Polya; Spotswood, Recueil des Travaux Chimiques des Pays-Bas, 1951, vol. 70, p. 146,153
作者:Polya、Spotswood
DOI:——
日期:——
Kasiwagi, Bulletin of the Chemical Society of Japan, 1927, vol. 2, p. 317