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Synthesis of Pyrido[2,3‐d]Azolopyrimidinones: Design and Epidermal Growth Factor Receptor‐Targeted Molecular Docking Toward Novel Anticancer Leads [PDF]

ChemistryOpen
A new class of pyrido[2,3‐d][1,2,4]triazolo[4,3‐a]pyrimidinones and pyrido[2,3‐d]thiazolo[3,2‐a]pyrimidinones was synthesized by reacting 5‐phenyl‐2‐thioxo‐2,3‐dihydropyrido[2,3‐d]pyrimidin‐4(1H)‐one with hydrazonoyl halides and α‐bromoketones via a ...
Sobhi M. Gomha, Sami A. Al‐Hussain, Basant Farag, AbdElAziz A. Nayl, Wesam Hussein, Abdelwahed R. Sayed, Magdi E. A. Zaki   +6 more
doaj   +3 more sources

Synthesis of 6-Amino-5-cyano-1,4-disubstituted-2(1H)-Pyrimidinones via Copper-(I)-catalyzed Alkyne-azide ‘Click Chemistry’ and Their Reactivity [PDF]

Molecules, 2010
In this paper we present the room temperature synthesis of a novel serie of 1,4-disubstituted-1,2,3-triazoles 4a-l by employing the (3 + 2) cycloaddition reaction of pyrimidinones containing alkyne functions with different model azides in the presence of
Fakher Chabchoub, Romain Duval
exaly   +6 more sources

The Persistence of Hydrogen Bonds in Pyrimidinones: From Solution to Crystal [PDF]

ACS Organic & Inorganic Au
Pyrimidinone scaffolds are present in a wide array of molecules with synthetic and pharmacological utility. The inherent properties of these compounds may be attributed to intermolecular interactions analogous to the interactions that molecules tend to ...
Fellipe F. S. Farias, Mateus Mittersteiner, Amanda M. Kieling, Priscila S. V. Lima, Gustavo H. Weimer, Helio G. Bonacorso, Nilo Zanatta, Marcos A. P. Martins   +7 more
doaj   +3 more sources

Competitive cyclization of ethyl trifluoroacetoacetate and methyl ketones with 1,3-diamino-2-propanol into hydrogenated oxazolo- and pyrimido-condensed pyridones [PDF]

Beilstein Journal of Organic Chemistry
The use of 1,3-diamino-2-propanol with competitive N- and O-nucleophilic centers in a three-component cyclization with ethyl 4,4,4-trifluoroacetoacetate and methyl ketones enables the synthesis to be carried out for octahydropyrido[1,2-a]pyrimidin-6-ones
Svetlana O. Kushch, Marina V. Goryaeva, Yanina V. Burgart, Marina A. Ezhikova, Mikhail I. Kodess, Pavel A. Slepukhin, Alexandrina S. Volobueva, Vladimir V. Zarubaev, Victor I. Saloutin   +8 more
doaj   +2 more sources

Surveillance of the antiviral activity and mechanism of action of newly synthesized spirocyclic thio-pyrimidinones against human adenovirus type 40 [PDF]

Virology Journal
Human adenoviruses (HAdVs) cause multiple common human infections; they are responsible for several upper and lower respiratory system and gastrointestinal diseases.
Esraa A. Manie, Sherif S. Ragab, Ayman M. Sweed, Sherif Nasser, Abdou K. Allayeh, Emad M. Elzayat   +5 more
doaj   +2 more sources

Pyrrolopyrimidines: Design, Synthesis and Antitumor Properties of Novel Tricyclic Pyrrolo [2,3-d]pyrimidine Derivatives [PDF]

Molecules
The pyrrolo[2,3-d]pyrimidine (7-deazapurine) scaffold is a unique heterocyclic system included in the composition of most nucleotides. In this study, series of the pyrrolo[2,3-d]pyrimidine-imines and 3-halo-substituted pyrrolo[2,3-d]pyrimidines were ...
Buer Song, Zarifa Murtazaeva, Lifei Nie, Rustamkhon Kuryazov, Shukhrat Gaybullaev, Chao Niu, Khurshed Bozorov, Haji Akber Aisa, Jiangyu Zhao   +8 more
doaj   +2 more sources

Design, Synthesis, and Evaluation of Naphthyl Pyrazino‐Pyrido‐Pyrimidinones Targeting the Phosphoinositide 3‐Kinase/Alpha‐Serine/Protein Kinase B/Mammalian Target of Rapamycin Pathway [PDF]

ChemistryOpen
Cancer remains a leading global cause of death and a major public health concern, with rising incidence and mortality rates. Current treatments are often limited by tumor complexity and heterogeneity, emphasizing the need for novel, targeted, and ...
Marcelo F. Marchiori, Gabriel da Silva, Daniel F. Kawano, Andréia M. Leopoldino, Enrique Madruga, Ana Martinez, Ivone Carvalho   +6 more
doaj   +2 more sources

Connecting chemical structure to single cell signaling profiles [PDF]

Communications Biology
A challenge in chemical biology is to study structure-activity relationships (SAR) in vivo in cells. Multiplexed activity profiling (MAP), developed for natural product discovery, is well-suited to address this challenge as it is high throughput ...
Hannah L. Thirman, Madeline J. Grider-Hayes, Laura C. Geben, Rebecca A. Ihrie, Lauren E. Brown, John A. Porco, Jonathan M. Irish   +6 more
doaj   +2 more sources

Novel Trifluoromethyl Pyrimidinone Compounds With Activity Against Mycobacterium tuberculosis

Frontiers in Chemistry, 2021
The identification and development of new anti-tubercular agents are a priority research area. We identified the trifluoromethyl pyrimidinone series of compounds in a whole-cell screen against Mycobacterium tuberculosis.
Erik Hembre, Julie V. Early, Joshua Odingo, Catherine Shelton, Olena Anoshchenko, Junitta Guzman, Lindsay Flint, Devon Dennison, Matthew B. McNeil, Aaron Korkegian, Yulia Ovechkina, Yulia Ovechkina, Paul Ornstein, Thierry Masquelin, Philip A. Hipskind, Tanya Parish, Tanya Parish   +16 more
doaj   +1 more source

Crystal structures of (E)-2-amino-4-methylsulfanyl-6-oxo-1-(1-phenylethylideneamino)-1,6-dihydropyrimidine-5-carbonitrile and (E)-2-amino-4-methylsulfanyl-6-oxo-1-[1-(pyridin-2-yl)ethylideneamino]-1,6-dihydropyrimidine-5-carbonitrile

Acta Crystallographica Section E: Crystallographic Communications, 2021
The title compounds 3a, C14H13N5OS, and 3b, C13H12N6OS, both show an E configuration about the N=C bond and a planar NH2 group. The molecules, which only differ in the presence of a phenyl (in 3a) or pyridyl (in 3b) substituent, are closely similar ...
Reham A. Mohamed-Ezzat, Galal H. Elgemeie, Peter G. Jones   +2 more
doaj   +1 more source