446252-22-8Relevant academic research and scientific papers
3,4-Dihydropyrimidin-2(1 H)-ones as Antagonists of the Human A2BAdenosine Receptor: Optimization, Structure-Activity Relationship Studies, and Enantiospecific Recognition
Majellaro, María,Jespers, Willem,Crespo, Abel,Nú?ez, María J.,Novio, Silvia,Azuaje, Jhonny,Prieto-Díaz, Rubén,Gioé, Claudia,Alispahic, Belma,Brea, José,Loza, María I.,Freire-Garabal, Manuel,Garcia-Santiago, Carlota,Rodríguez-García, Carlos,García-Mera, Xerardo,Caama?o, Olga,Fernandez-Masaguer, Christian,Sardina, Javier F.,Stefanachi, Angela,El Maatougui, Abdelaziz,Mallo-Abreu, Ana,?qvist, Johan,Gutiérrez-De-Terán, Hugo,Sotelo, Eddy
supporting information, p. 458 - 480 (2021/01/13)
We present and thoroughly characterize a large collection of 3,4-dihydropyrimidin-2(1H)-ones as A2BAR antagonists, an emerging strategy in cancer (immuno) therapy. Most compounds selectively bind A2BAR, with a number of potent and selective antagonists fu
Zn2+/MCM-41 catalyzed Biginelli reaction of heteroaryl aldehydes and evaluation of the antimicrobial activity and cytotoxicity of the pyrimidone products
Ghasemi, Zarrin,Farshbaf Orafa, Farzaneh,Pirouzmand, Mahtab,Zarrini, Gholamreza,Nikzad Kojanag, Behnaz,Salehi, Roya
supporting information, p. 6393 - 6396 (2015/11/16)
The three component Biginelli condensation of various aryl aldehydes, 1,3-dicarbonyls and urea was investigated in the presence of free or MCM-41 supported ZnNO3. The pyrimidone products, which were obtained under solvent-free conditions, were
Discovery of 3,4-dihydropyrimidin-2(1 H)-ones as a novel class of potent and selective A2B adenosine receptor antagonists
Crespo, Abel,El Maatougui, Abdelaziz,Biagini, Pierfrancesco,Azuaje, Jhonny,Coelho, Alberto,Brea, Jose,Loza, Maria Isabel,Cadavid, Maria Isabel,Garcia-Mera, Xerardo,Gutierrez-De-Teran, Hugo,Sotelo, Eddy
, p. 1031 - 1036 (2013/12/04)
We describe the discovery and optimization of 3,4-dihydropyrimidin-2(1H)- ones as a novel family of (nonxanthine) A2B receptor antagonists that exhibit an unusually high selectivity profile. The Biginelli-based hit optimization process enabled a thoughtful exploration of the structure-activity and structure-selectivity relationships for this chemotype, enabling the identification of ligands that combine structural simplicity with excellent hA2B AdoR affinity and remarkable selectivity profiles.
