Assuntos
Anti-Hipertensivos/síntese química , Dinoprostona/análogos & derivados , Prostaglandinas E Sintéticas/farmacologia , Administração Oral , Administração Tópica , Animais , Pressão Sanguínea/efeitos dos fármacos , Prostaglandinas E Sintéticas/administração & dosagem , Ratos , Fatores de TempoRESUMO
The interesting bronchodilator activity of l-11-deoxy-11 alpha-[(2-hydroxyethyl)thio]prostaglandin E2 methyl ester (3a) is described. The preparation of 3a and its analogues by Michael-type additions to various members of the PGA series or by total synthesis using the lithiocuprate conjugate addition process is also described. Structure-activity relationships in this series are discussed.
Assuntos
Broncodilatadores/síntese química , Prostaglandinas E Sintéticas/síntese química , Resistência das Vias Respiratórias/efeitos dos fármacos , Animais , Cães , Cobaias , Hemodinâmica/efeitos dos fármacos , Métodos , Prostaglandinas E Sintéticas/farmacologia , EstereoisomerismoRESUMO
The synthesis and bronchodilator activity in the guinea pig of several 15-deoxy-16-hydroxy-16-methylprostaglandin analogs is described. The E2 (VIa) and E1 (VIb) analogs are potent bronchodilators comparable in activity to the natrual prostaglandins, but possessing a longer duration of effect. Replacement of the C13--C14 trans double bond by a cis double bond or an ethylene linkage causes a substantial diminishment of this activity.
Assuntos
Broncodilatadores , Prostaglandinas E Sintéticas/síntese química , Animais , Fenômenos Químicos , Química , Cobaias , Prostaglandinas E Sintéticas/farmacologiaRESUMO
dl-Erythro-16-methoxy-PGE2, PGA2, PGF2alpha, 11-deoxy PGE1, and 11-deoxy PGF1alpha have been prepared via the cuprate conjugate addition procedure. These congeners are less potent than the parent prostaglandins as stimulators of isolated gerbil colon contractions and as bronchodilators in the guinea pig Konzett assay.
