ABSTRACT
Four methods of the synthesis of model glycosides with 11-deoxyprostaglandin E1 and a connecting polymethylene chain as the aglycone are compared. Interaction of potassium salt of prostaglandin PG with omega-iodoalkylglycosides is the most promising approach.
Subject(s)
Alprostadil/analogs & derivatives , Glycosides/chemistry , Prostaglandins E/chemical synthesis , Alprostadil/chemical synthesis , Esters/chemical synthesis , Magnetic Resonance SpectroscopyABSTRACT
Hydroxyl-containing 11-deoxyprostaglandin E1 esters were synthesised by using the methods of mixed anhydrides and nucleophilic displacement.
Subject(s)
Alprostadil/analogs & derivatives , Alprostadil/chemical synthesis , Alprostadil/isolation & purification , Chemical Phenomena , Chemistry , Chromatography, Thin Layer , Esters/chemical synthesis , Esters/isolation & purification , Mass SpectrometryABSTRACT
2,6-Dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)-1, 4-dihydropyridine (ryodipine, PP-1466) at oral administration in the form of a suspension with Tween (polysorbate) 80 addition is comparatively rapidly absorbed in the gastro-intestinal tract and circulates in blood for a long period of time. PP-1466 practically does not bind to plasma proteins. The drug is mainly excreted via the kidneys and with faeces by 49 and 46% of the dose administered after 96 h, respectively. PP-1466 metabolites are present in rat urine-2,6-dimethyl-4-arylpyridine-3,5-dicarbonic acid derivatives: oxidation product of PP-1466 dihydropyridine cycle into pyridine one, products of partial or complete hydrolysis of ester groups of PP-1466 oxidized form, lactones. There have been performed the synthesis of labelled 14C-PP-1466 as well as counter-synthesis of PP-1466 metabolites. Unchanged PP-1466 is not detected in urine.