- Pyrido[1,2-a]pyrimidin-4-one derivatives as a novel class of selective aldose reductase inhibitors exhibiting antioxidant activity
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2-Phenyl-pyrido[1,2-a]pyrimidin-4-one derivatives bearing a phenol or a catechol moiety in position 2 were tested as aldose reductase (ALR2) inhibitors and exhibited activity levels in the micromolar/submicromolar range. Introduction of a hydroxy group in
- La Motta, Concettina La,Sartini, Stefania,Mugnaini, Laura,Simorini, Francesca,Taliani, Sabrina,Salerno, Silvia,Marini, Anna Maria,Da Settimo, Federico,Lavecchia, Antonio,Novellino, Ettore,Cantore, Miriam,Failli, Paola,Ciuffi, Mario
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- New efficient approach for the synthesis of 2-alkyl(aryl) substituted 4H-pyrido[1,2-a]pyrimidin-4-ones
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A new, efficient and easy route for the preparation of a series of 2-alkyl(aryl) substituted 4-oxo-4H-pyrido[l,2-a]pyrimidines, where alkyl = CH3; aryl = C6H5, 4-FC6H 4,4-ClC6H4,
- Bonacorso, Helio G.,Righi, Fernando J.,Rodrigues, Isadora R.,Cechinel, Cleber A.,Costa, Michelle B.,Wastowski, Arci D.,Martins, A. P. Marcos,Zanatta, Nilo
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- Silver-catalyzed highly efficient synthesis of pyrido[1,2-a]pyrimidin-4-ones from 2-aminopyridines and alkynoates
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Pyrimidinone is one of the important nitrogen containing heterocycles due to their wide range of bioactivities. An efficient silver-catalyzed intermolecular cyclization of 2-aminopyridines with various alkynoates has been developed. 2-Substituted 4H-pyrido[1,2-a]pyrimidin-4-ones containing a wide range of functional groups are synthesized in the standard conditions. This transformation is conducted under convenient conditions and affords products in good yields.
- Chen, Zhengwang,Wen, Yuelu,Ding, Hao,Luo, Guotian,Ye, Min,Liu, Liangxian,Xue, Jun
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Read Online
- Identification of novel SIRT1 activators endowed with cardioprotective profile
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Drugs targeting epigenetic mechanisms are attracting the attention of scientists since it was observed that the modulation of this post-translational apparatus, could help to identify innovative therapeutic strategies. Among the epigenetic druggable targe
- Brogi, Simone,Calderone, Vincenzo,Flori, Lorenzo,La Motta, Concettina,Petrarolo, Giovanni,Testai, Lara
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- Transition-metal-free lactamization of C(sp3)-H bonds with CO2: Facile generation of pyrido[1,2-: A] pyrimidin-4-ones
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A novel carbonylation of C(sp3)-H bonds in pyridylamines with one atmosphere of CO2 is reported to synthesize important pyrimidinones in good yields. This transition-metal-free and redox-neutral process features the use of a nontoxic
- Zhang, Zhen,Zhou, Xiao-Yu,Wu, Jin-Gui,Song, Lei,Yu, Da-Gang
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supporting information
p. 28 - 32
(2020/01/13)
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- Method for synthesizing pyrimidinone compound under participation of CO2
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The invention provides a method for synthesizing a pyrimidinone compound under the participation of CO2, the structural formula of the pyrimidinone compound is shown as a formula (I), and a reaction substrate is shown as a formula (II); wherein R1, R2 and
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Paragraph 0043; 0048-0052; 0057; 0061
(2020/03/05)
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- Practical synthesis of 4H-pyrido[1, 2-a]pyrimidin-4-ones using ethylene glycol as a promoting solvent
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A simple and useful protocol leading to different 4H-pyrido[1, 2-a] pyrimidin-4-ones have been established by cyclization of various 2-amino pyridines with β-oxo ester or alkynoate. The use of ethylene glycol was demonstrated to facilitate this condensati
- Hussain, Mustafa,Liu, Jianhui
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supporting information
(2020/08/13)
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- Manganese-Catalyzed Carbonylative Annulations for Redox-Neutral Late-Stage Diversification
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An inexpensive, nontoxic manganese catalyst enabled unprecedented redox-neutral carbonylative annulations under ambient pressure. The manganese catalyst outperformed all other typically used base and precious-metal catalysts. The outstanding versatility o
- Liang, Yu-Feng,Steinbock, Ralf,Münch, Annika,Stalke, Dietmar,Ackermann, Lutz
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supporting information
p. 5384 - 5388
(2018/04/09)
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- Scaffold-hopping of bioactive flavonoids: Discovery of aryl-pyridopyrimidinones as potent anticancer agents that inhibit catalytic role of topoisomerase IIα
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A strategy of scaffold-hopping of bioactive natural products, flavones and isoflavones, leading to target-based discovery of potent anticancer agents has been reported for the first time. Scaffold-hopped flavones, 2-aryl-4H-pyrido[1,2-a]pyrimidin-4-ones and the scaffold-hopped isoflavones, 3-aryl-pyrido[1,2-a]pyrimidin-4-ones were synthesized via Pd-catalyzed activation–arylation methods. Most of the compounds were found to exhibit pronounced human topoisomerase IIα (hTopoIIα) inhibitory activities and several compounds were found to be more potent than etoposide (a hTopoIIα-inhibiting anticancer drug). These classes of compounds were found to be hTopoIIα-selective catalytic inhibitors while not interfering with topoisomerase I and interacted with DNA plausibly in groove domain. Cytotoxicities against various cancer cells, low toxicity in normal cells, and apoptotic effects were observed. Interestingly, compared to parent flavones/isoflavones, their scaffold-hopped analogs bearing alike functionalities showed significant/enhanced hTopoIIα-inhibitory and cytotoxic properties, indicating the importance of a natural product-based scaffold-hopping strategy in the drug discovery.
- Priyadarshani, Garima,Amrutkar, Suyog,Nayak, Anmada,Banerjee, Uttam C.,Kundu, Chanakya N.,Guchhait, Sankar K.
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- Simple and efficient protocol for synthesis of pyrido[1,2-a]pyrimidin-4-one derivatives over solid heteropolyacid catalysts
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Aluminium exchanged tungstophosphoric acid salts with Keggin structure (AlxH3-xPW12O40) were prepared by simple ion exchange method. The prepared heteropolyacid salts were characterized by various techniques suc
- Basahel, Sulaiman N.,Ahmed, Nesreen S.,Narasimharao, Katabathini,Mokhtar, Mohamed
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p. 11921 - 11932
(2016/02/12)
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- Synthesis of 2-Arylpyridopyrimidinones, 6-Aryluracils, and Tri- and Tetrasubstituted Conjugated Alkenes via Pd-Catalyzed Enolic C-O Bond Activation-Arylation
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A new and efficient approach for the synthesis of biologically important 2-aryl-4H-pyrido[1,2-a]pyrimidin-4-ones and 6-aryluracils via previously unknown Pd-catalyzed enolic C-OH activation-arylation of pyridopyrimidin-2,4-diones and barbituric acids, res
- Guchhait, Sankar K.,Priyadarshani, Garima
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p. 6342 - 6349
(2015/06/30)
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- Pd-catalyzed carbonylative cycloamidation of ketoimines for the synthesis of pyrido[1,2-a]pyrimidin-4-ones
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The Pd(ii)-catalyzed pyridine-directed carbonylative cycloamidation of ketoimines has provided an efficient protocol for assembly of pyrido[1,2-a]pyrimidin-4-ones. This journal is
- Xie, Ying,Chen, Tengfei,Fu, Shaomin,Jiang, Huanfeng,Zeng, Wei
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supporting information
p. 9377 - 9380
(2015/06/02)
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- Solvent-free synthesis of 4H-Pyrido[1,2-a]pyrimidin-4-ones catalyzed by BiCl3: A green route to a privileged backbone
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An extensive array of 4H-pyrido[1,2-a]pyrimidin-4-ones have been synthesized from commercially available 2-aminopyridines and β-oxo esters with excellent yields under solvent-free conditions. The reaction, catalyzed by cheap and nontoxic BiCl3,
- Roslan, Irwan I.,Lim, Qiu-Xuan,Han, Aijuan,Chuah, Gaik-Khuan,Jaenicke, Stephan
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supporting information
p. 2351 - 2355
(2015/04/22)
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- COMPOUNDS OF ESTROGEN-RELATED RECEPTOR MODULATORS AND THE USES THEREOF
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The compounds according to formula (I), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modula
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Page/Page column 20
(2011/05/05)
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- Suzuki-Miyaura cross-coupling reactions of halo derivatives of 4H-pyrido[1,2-a]pyrimidin-4-ones
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The palladium-catalyzed Suzuki-Miyaura cross-coupling reactions of halo derivatives of 4H-pyrido[1,2-a]pyrimidin-4-one with (het)arylboronic acids allow easy access to (het)aryl and vinyl derivatives of this bicycle in good to excellent yields, even from chloro derivatives. The sequence of reactivity of the halogen in the different positions of the ring system was also investigated. 6-Phenyl-4H-pyrido[1,2-a]pyrimidin-4-one could be prepared by thermal cyclization of isopropylidene (6-phenylpyrid-2-ylamino)methylenemalonate, together with a small amount of 7-phenyl-1,4-dihydro-1,8-naphthyridin-4-one.
- Molnar, Annamaria,Kapros, Anita,Parkanyi, Laszlo,Mucsi, Zoltan,Vlad, Gabor,Hermecz, Istvan
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supporting information; experimental part
p. 6559 - 6565
(2011/11/05)
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- Identification of pyrido[1,2-α]pyrimidine-4-ones as new molecules improving the transcriptional functions of estrogen-related receptor α
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The nuclear estrogen-related receptor α (ERRα) plays a central role in the regulation of expression of the genes involved in mitochondrial biogenesis and oxidative metabolism. We have successfully identified a series of pyrido[1,2-a]pyrimidin-4-ones as new agonists enhancing the transcriptional functions of ERRα. The compounds potently elevated the mRNA levels and the protein levels of ERRα downstream targets. Consequently, the compounds improved the glucose and fatty acid uptake in C2C12 muscle cells.
- Peng, Lijie,Gao, Xuefei,Duan, Lei,Ren, Xiaomei,Wu, Donghai,Ding, Ke
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experimental part
p. 7729 - 7733
(2012/01/06)
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- Method for treating tumors using 2-aryl-naphthyridin-4-ones
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The present invention provides compounds of Formula I: STR1 wherein A and R1 -R8 are defined herein. The compounds of Formula I inhibit the polymerization of tubulin and possess antimitotic activity. The compounds of Formula I may be useful for the treatment of psoriasis, gout, papiloma, warts, and a variety of tumors.
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