136498-08-3Relevant articles and documents
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
One-pot synthesis of thiazolidino [3,2-a] pyrimidine derivatives
Jeanneau-Nicolle,Benoit-Guyod,Leclerc
, p. 1443 - 1454 (2007/10/02)
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.
