2917-02-4Relevant articles and documents
Pyrimidinone derivative, preparation method thereof and application thereof in resisting mycobacterium tuberculosis infection
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Paragraph 0151-0156, (2020/11/25)
The invention discloses a pyrimidinone derivative, a preparation method thereof and an application thereof in resisting mycobacterium tuberculosis infection. The structure of the pyrimidinone derivative is shown as a formula I, wherein R1, m, X, Y, Z, R2
Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine receptor
Cosimelli, Barbara,Greco, Giovanni,Laneri, Sonia,Novellino, Ettore,Sacchi, Antonia,Collina, Simona,Rossi, Daniela,Cosconati, Sandro,Barresi, Elisabetta,Taliani, Sabrina,Trincavelli, Maria Letizia,Martini, Claudia
, p. 81 - 86 (2018/02/07)
Three A3 adenosine receptor (AR) antagonists (1-3) selected from 4-acylamino-6-alkyloxy-2-alkylthiopyrimidines previously investigated by us were modified by inserting a methyl group on their ether or thioether side chains. These compounds gave
Synthesis of new derivatives of 5-(3,4-dihydro-2Н-pyrrol-5-yl)-pyrimidine
Gasparyan,Alexanyan,Arutyunyan,Kocharov,Martirosyan,Tamazyan,Ayvazyan,Panosyan,Danagulyan
, p. 1646 - 1653 (2017/01/28)
By one-stage condensation of 6-(arylamino)pyrimidine-2,4(1Н,3Н)-diones with pyrrolidin-2-one new potential antiviral compounds were obtained, analogs of pyrrolinylpyrimidine containing structural fragments of known drugs AZT and HEPT used in treating HIV-infections.
Enantiomeric 4-Acylamino-6-alkyloxy-2 Alkylthiopyrimidines As Potential A3Adenosine Receptor Antagonists: HPLC Chiral Resolution and Absolute Configuration Assignment by a Full Set of Chiroptical Spectroscopy
Rossi, Daniela,Nasti, Rita,Marra, Annamaria,Meneghini, Silvia,Mazzeo, Giuseppe,Longhi, Giovanna,Memo, Maurizio,Cosimelli, Barbara,Greco, Giovanni,Novellino, Ettore,Da Settimo, Federico,Martini, Claudia,Taliani, Sabrina,Abbate, Sergio,Collina, Simona
, p. 434 - 440 (2017/02/10)
The chiral separation of enantiomeric couples of three potential A3adenosine receptor antagonists: (R/S)-N-(6-(1-phenylethoxy)-2-(propylthio)pyrimidin-4-yl)acetamide (1), (R/S)-N-(2-(1-phenylethylthio)-6-propoxypyrimidin-4-yl)acetamide (2), and
New approach to synthesize symmetrical and unsymmetrical 6-(N-Alkyl(Aryl)amino)-and 6-(N, N-dialkyl(Aryl)amino)-2,4-bis(Alkyl(Aryl)Thio) pyrimidines as anti-platelet agents
Liu, Guocheng,Xu, Jiaxi,Yu, Mingwu,Chen, Ning,Zhang, Si,Ding, Zhongren,Du, Hongguang
scheme or table, p. 650 - 659 (2012/06/01)
A new and straightforward procedure has been developed for the preparation of symmetrical and unsymmetrical 6-(N-alkyl(aryl)amino)-and 6-(N,N- bisalkyl(aryl)amino)-2,4-bis(alkyl(aryl)thio)pyrimidines. The two identical or different alkylthio groups were s
Novel synthesis approach and antiplatelet activity evaluation of 6-alkylamino-2,4-dialkyl(aryl)thiopyrimidines
Liu, Guocheng,Xu, Jiaxi,Park, Ki Chul,Chen, Ning,Zhang, Si,Ding, Zhongren,Wang, Feng,Du, Hongguang
experimental part, p. 5156 - 5161 (2011/07/31)
A new and efficient procedure has been designed for the preparation of 6-alkylamino-2,4-dialkyl(aryl)thiopyrimidines. The first alkylthio group was introduced into the pyrimidine ring by S-alkylation. The introduction of the second one was successfully ac
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists
Cosimelli, Barbara,Greco, Giovanni,Ehlardo, Marina,Novellino, Ettore,Da Settimo, Federico,Taliani, Sabrina,La Motta, Concettina,Bellandi, Marusca,Tuccinardi, Tiziano,Martinelli, Adriano,Ciampi, Osele,Trincavelli, Maria Letizia,Martini, Claudia
, p. 1764 - 1770 (2008/12/22)
A number of derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine (5) were synthesized and biologically evaluated as A3 adenosine receptor (A3 AR) antagonists. The new compounds were designed as open chain analogues of a triazolopyrimidinone derivative displaying submicromolar affinity for the A3 AR, which had been previously identified using a 3D database search. Substituents R, R′, and R″ attached to the parent compound 5 were chosen according to factorial design and stepwise lead optimization approaches, taking into account the essentially hydrophobic nature of the A3 AR binding site. As a result, 5m (R = n-C3H 7, R′ = 4-ClC6H4CH2, R″ = CH3) was identified among the pyrimidine derivatives as the ligand featuring the best combination of potency and selectivity for the target receptor. This compound binds to the A3 AR with a Ki of 3.5 nM and is devoid of appreciable affinity for the A1, A 2A, and A2B ARs.