136498-24-3Relevant academic research and scientific papers
One-pot synthesis of thiazolidino [3,2-a] pyrimidine derivatives
Jeanneau-Nicolle,Benoit-Guyod,Leclerc
, p. 1443 - 1454 (1991)
Reaction of 2-aminothiazoline with an aromatic aldehyde and an activated methylene group (malonitrile, diethylmalonate or ethylcyanoacetate) gave the title compounds. The structures are unambiguously assigned using spectroscopic data and chemical proofs.
New thiazolopyrimidine derivatives, synthesis and structure-activity relationships
Jeanneau-Nicolle, E,Benoit-Guyod, M,Namil, A,Leclerc, G
, p. 115 - 120 (2007/10/02)
Twenty-six derivatives of 5- and 7-oxo or 5- and 7-aminothiazolopyrimidines were prepared and evaluated as positive inotropic, anti-inflammatory and antihypertensive agents both in vitro and in vivo.The structures of the 5- and 7-isomers have been confirmed unambiguously by IR, UV, 1H and 13C NMR and MS.The structure of 1a was confirmed by the synthesis of compound 1 whose structure had been previously established by X-ray analysis.The 5-aminothiazolo-pyrimidine-6-carbonitrile derivatives 5a and 5e exhibited potent inotropic activities. 5e was more potent thanthe classical reference amrinone.Three compounds 5e, 5i and 5j displayed moderate antihypertensive activities.The 4-chlorophenyl derivative 5d exhibited an anti-inflammatory activity 2-fold that of aspirin.This study has demonstrated that thiazolopyrimidine compounds have interesting biological potentialities, particularly as inotropic agents, a field which had never been explored so far for this series. thiazolopyrimidines / cardiotonic / inotropic / antihypertensive / anti-inflammatory activity
