81585-34-4Relevant academic research and scientific papers
Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease
Chioua, Mourad,Buzzi, Eleonora,Moraleda, Ignacio,Iriepa, Isabel,Maj, Maciej,Wnorowski, Artur,Giovannini, Catia,Tramarin, Anna,Portali, Federica,Ismaili, Lhassane,López-Alvarado, Pilar,Bolognesi, Maria Laura,Jó?wiak, Krzysztof,Menéndez, J. Carlos,Marco-Contelles, José,Bartolini, Manuela
supporting information, p. 839 - 846 (2018/06/29)
Notwithstanding the combination of cholinesterase (ChE) inhibition and calcium channel blockade within a multitarget therapeutic approach is envisaged as potentially beneficial to confront Alzheimer's disease (AD), this strategy has been scarcely investigated. To explore this promising line, a series of 5-amino-4-aryl-3,4,6,7,8,9-hexahydropyrimido [4,5-b]quinoline-2(1H)-thiones (tacripyrimidines) (4a-l) were designed by juxtaposition of tacrine, a ChE inhibitor (ChEI), and 3,4-dihydropyrimidin-2(1H)-thiones, as efficient calcium channel blockers (CCBs). In agreement with their design, all tacripyrimidines, except the unsubstituted parent compound and its p-methoxy derivative, acted as moderate to potent CCBs with activities generally similar or higher than the reference CCB drug nimodipine and were modest-to-good ChEIs. Most interestingly, the 3′-methoxy derivative (4e) emerged as the first well balanced ChEI/CCB agent, acting as low micromolar hChEI (3.05 μM and 3.19 μM on hAChE and hBuChE, respectively) and moderate CCB (30.4% at 1 μM) with no significant hepatotoxicity toward HepG2 cells and good predicted oral absorption and blood brain barrier permeability.
Synthesis and evaluation of cytotoxicity of 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles
Atapour-Mashhad, Hoda,Soukhtanloo, Mohammad,Massoudi, Abdolhossien,Shiri, Ali,Bakavoli, Mehdi
, p. 316 - 322 (2016/07/06)
Several derivatives of 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles were synthesized via Biginelli type reaction and tested for their anti-proliferative activity on human breast cancer (MCF-7) and human colon carcinoma (HT29) cell
Synthesis of some new pyrimidine and pyrimido[4,5-d]pyrimidine derivatives
Fadda, Ahmed A.,El-Latif, Ehab Abd,Bondock, Samir,Samir, Ahmed
body text, p. 4352 - 4368 (2009/04/11)
A convenient synthesis of a series of pyrimidine carbonitrile, thiopyrimidine, and pyrimidopyrimidine derivatives, via the reactions of the versatile, readily accessible 6-aryl-4-oxo-2-thioxo-hexahydro-pyrimidine-5- carbonitrile with the appropriate reagents, is described. Copyright Taylor & Francis Group, LLC.
SYNTHESIS OF HETEROCYCLIC COMPOUNDS XXII. PREPARATION OF 6-ARYL-2-THIOXOPYRIMIDINES
Navio, Jose L. Garcia,Lorente, Antonio,Soto, Jose L.
, p. 305 - 311 (2007/10/02)
The reactions of different ethyl benzylidenecyanoacetates (I) and benzylidenemalononitriles (V) with thiourea in an alcohol-alkoxide medium, provide a new and simple method for the synthesis of 6-aryl-5-cyano-4-oxo-2-thioxohexahydropyrimidines (III) and 4
