Matches in SemOpenAlex for { <https://semopenalex.org/work/W2412672746> ?p ?o ?g. }
Showing items 1 to 70 of
70
with 100 items per page.
- W2412672746 endingPage "23" @default.
- W2412672746 startingPage "705" @default.
- W2412672746 abstract "The N,N-disubstituted 4-amino-2H-pyrido[1,2-a]pyrimidin-2-ones (III) and isomer 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones (IV) were obtained from the reaction of 2-aminopyridine with the N,N-disubstituted ethyl malonamate/phosphorus oxychloride reagent (II), in refluxing 1,2-dichloroethane. 2-[(N-Benzyl, N-ethyl)amino]derivative (IV b) was also prepared in excellent yield by treating 2-chloro-4H-pyrido[1,2-a]pyrimidin-4-one (V) with N-ethylbenzylamine. Finally, hydrogenation (Raney Nickel) of 4-[(N-ethyl,N-phenyl)amino]-2H-pyrido[1,2-a]pyrimidin-2-one (III e) afforded 6,7,8,9-tetrahydroderivative (VI) which in turn was treated with potassium borohydride to give 1,6,7,8,9,9a-hexahydroderivative (VII). Several compounds described in the present paper, along with some other compounds (III) and (IV) previously synthesized by us (1,2), were tested for various pharmacological activities. The antiallergic activity (PCA in the rat), even though found in several compounds examined, turned out to be submaximal in any case, in spite of the high dose administered (500 mg/kg p.o. as a rule). The most active compound (the activity being estimated at 0.42 times that of thiaramide hydrochloride) was the 4-aminoderivative (III e). The 2-aminoderivatives (IV) series, was found to have marked antiinflammatory properties (carrageenin oedema in the rat); nevertheless, this activity was related to toxic symptoms with the exception of compound (IV b), almost asymptomatic at the administered dose (200 mg/kg p.o.). Moreover the 2-aminoderivatives (IV) generally showed weak adrenolitic activity in vitro (rat seminal vesicles), which was estimated to be from 100 to 1000 times less than that of phenoxybenzamine." @default.
- W2412672746 created "2016-06-24" @default.
- W2412672746 creator A5028854670 @default.
- W2412672746 creator A5033476715 @default.
- W2412672746 creator A5053873069 @default.
- W2412672746 creator A5056030700 @default.
- W2412672746 creator A5064338206 @default.
- W2412672746 creator A5084743886 @default.
- W2412672746 creator A5088123169 @default.
- W2412672746 date "1988-09-01" @default.
- W2412672746 modified "2023-09-23" @default.
- W2412672746 title "[Derivatives of pyrimidine 1,2-condensate. IV. Synthesis and pharmacological properties of the N,N-disubstituted 4-amino-2H-pyrido(1,2-a)pyrimidin- 2-ones and 2-amino-4H-pyrido(1,2-a)pyrmidin-4-ones]." @default.
- W2412672746 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/3229496" @default.
- W2412672746 hasPublicationYear "1988" @default.
- W2412672746 type Work @default.
- W2412672746 sameAs 2412672746 @default.
- W2412672746 citedByCount "0" @default.
- W2412672746 crossrefType "journal-article" @default.
- W2412672746 hasAuthorship W2412672746A5028854670 @default.
- W2412672746 hasAuthorship W2412672746A5033476715 @default.
- W2412672746 hasAuthorship W2412672746A5053873069 @default.
- W2412672746 hasAuthorship W2412672746A5056030700 @default.
- W2412672746 hasAuthorship W2412672746A5064338206 @default.
- W2412672746 hasAuthorship W2412672746A5084743886 @default.
- W2412672746 hasAuthorship W2412672746A5088123169 @default.
- W2412672746 hasConcept C134121241 @default.
- W2412672746 hasConcept C155647269 @default.
- W2412672746 hasConcept C161790260 @default.
- W2412672746 hasConcept C178790620 @default.
- W2412672746 hasConcept C185592680 @default.
- W2412672746 hasConcept C191897082 @default.
- W2412672746 hasConcept C192562407 @default.
- W2412672746 hasConcept C2776460385 @default.
- W2412672746 hasConcept C2779321679 @default.
- W2412672746 hasConcept C2780048404 @default.
- W2412672746 hasConcept C40875361 @default.
- W2412672746 hasConcept C71240020 @default.
- W2412672746 hasConceptScore W2412672746C134121241 @default.
- W2412672746 hasConceptScore W2412672746C155647269 @default.
- W2412672746 hasConceptScore W2412672746C161790260 @default.
- W2412672746 hasConceptScore W2412672746C178790620 @default.
- W2412672746 hasConceptScore W2412672746C185592680 @default.
- W2412672746 hasConceptScore W2412672746C191897082 @default.
- W2412672746 hasConceptScore W2412672746C192562407 @default.
- W2412672746 hasConceptScore W2412672746C2776460385 @default.
- W2412672746 hasConceptScore W2412672746C2779321679 @default.
- W2412672746 hasConceptScore W2412672746C2780048404 @default.
- W2412672746 hasConceptScore W2412672746C40875361 @default.
- W2412672746 hasConceptScore W2412672746C71240020 @default.
- W2412672746 hasIssue "9" @default.
- W2412672746 hasLocation W24126727461 @default.
- W2412672746 hasOpenAccess W2412672746 @default.
- W2412672746 hasPrimaryLocation W24126727461 @default.
- W2412672746 hasRelatedWork W1971472325 @default.
- W2412672746 hasRelatedWork W2060931142 @default.
- W2412672746 hasRelatedWork W2097014657 @default.
- W2412672746 hasRelatedWork W2129735191 @default.
- W2412672746 hasRelatedWork W2158447163 @default.
- W2412672746 hasRelatedWork W2606019367 @default.
- W2412672746 hasRelatedWork W2949184651 @default.
- W2412672746 hasRelatedWork W2949540668 @default.
- W2412672746 hasRelatedWork W2950642343 @default.
- W2412672746 hasRelatedWork W2952722008 @default.
- W2412672746 hasVolume "43" @default.
- W2412672746 isParatext "false" @default.
- W2412672746 isRetracted "false" @default.
- W2412672746 magId "2412672746" @default.
- W2412672746 workType "article" @default.