100881-32-1Relevant articles and documents
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Mariella,R.P.,Zelko,J.J.
, p. 647 - 648 (1960)
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Iron-Catalyzed Alkyne-Based Multicomponent Synthesis of Pyrimidines under Air
Chakraborty, Gargi,Guin, Amit Kumar,Mondal, Rakesh,Paul, Nanda D.,Sarkar, Susmita
, p. 13186 - 13197 (2021/10/01)
An iron-catalyzed sustainable, economically affordable, and eco-friendly synthetic protocol for the construction of various trisubstituted pyrimidines is described. A wide range of trisubstituted pyrimidines were prepared using a well-defined, easy to prepare, bench-stable, and phosphine-free iron catalyst featuring a redox-noninnocent tridentate arylazo pincer under comparatively mild aerobic conditions via dehydrogenative functionalization of alcohols with alkynes and amidines.
The discovery of novel antitrypanosomal 4-phenyl-6-(pyridin-3-yl)pyrimidines
Robinson, William J.,Taylor, Annie E.,Lauga-Cami, Solange,Weaver, George W.,Arroo, Randolph R.J.,Kaiser, Marcel,Gul, Sheraz,Kuzikov, Maria,Ellinger, Bernhard,Singh, Kuldip,Schirmeister, Tanja,Botana, Adolfo,Eurtivong, Chatchakorn,Bhambra, Avninder S.
, (2020/10/21)
Human African trypanosomiasis, or sleeping sickness, is a neglected tropical disease caused by Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense which seriously affects human health in Africa. Current therapies present limitations in their application, parasite resistance, or require further clinical investigation for wider use. Our work herein describes the design and syntheses of novel antitrypanosomal 4-phenyl-6-(pyridin-3-yl)pyrimidines, with compound 13, the 4-(2-methoxyphenyl)-6-(pyridine-3-yl)pyrimidin-2-amine demonstrating an IC50 value of 0.38 μM and a promising off-target ADME-Tox profile in vitro. In silico molecular target investigations showed rhodesain to be a putative candidate, supported by STD and WaterLOGSY NMR experiments, however, in vitro evaluation of compound 13 against rhodesain exhibited low experimental inhibition. Therefore, our reported library of drug-like pyrimidines present promising scaffolds for further antikinetoplastid drug development for both phenotypic and target-based drug discovery.
