1122-74-3Relevant articles and documents
Studies toward the total synthesis of the variolins: Rapid entry to the core structure
Anderson, Regan J.,Morris, Jonathan C.
, p. 311 - 313 (2001)
The pyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidine core structure of the variolins has been synthesized in three steps from commercially available materials. The key reaction involves the deoxygenation and concomitant cyclization of a triarylmethanol using the
In vitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L. major casein kinase 1 inhibition
Bazin, Marc-Antoine,Cojean, Sandrine,Pagniez, Fabrice,Bernadat, Guillaume,Cavé, Christian,Ourliac-Garnier, Isabelle,Nourrisson, Marie-Renée,Morgado, Cathy,Picot, Carine,Leclercq, Olivier,Baratte, Blandine,Robert, Thomas,Sp?th, Gérald F.,Rachidi, Najma,Bach, Stéphane,Loiseau, Philippe M.,Le Pape, Patrice,Marchand, Pascal
, (2020/11/05)
Leishmaniasis constitutes a severe public health problem, with an estimated prevalence of 12 million cases. This potentially fatal disease has a worldwide distribution and in 2012, the fatal Visceral Leishmaniasis (VL) was declared as new emerging disease in Europe, mainly due to global warming, with expected important public health impact. The available treatments are toxic, costly or lead to parasite resistance, thus there is an urgent need for new drugs with new mechanism of action. Previously, we reported the discovery of CTN1122, a potent imidazo[1,2-a]pyrazine-based antileishmanial hit compound targeting L-CK1.2 at low micromolar ranges. Here, we described structurally related, safe and selective compounds endowed with antiparasitic properties, better than miltefosine, the reference therapy by oral route. L-CK1.2 homology model gave the first structural explanations of the role of 4-pyridyl (CTN1122) and 2-aminopyrimidin-4-yl (compound 21) moieties, at the position 3 of the central core, in the low micromolar to nanomolar L-CK1.2 inhibition, whereas N-methylpyrazole derivative 11 remained inactive against the parasite kinase.
Azine and Diazine Functionalization Using 2,2,6,6-Tetramethylpiperidino-Based Lithium-Metal Combinations: Application to the Synthesis of 5,9-Disubstituted Pyrido[3′,2′:4,5]pyrrolo[1,2- c ]pyrimidines
Marquise, Nada,Nguyen, Tan Tai,Chevallier, Floris,Picot, Laurent,Thiéry, Valérie,Lozach, Olivier,Bach, Stéphane,Ruchaud, Sandrine,Mongin, Florence
, p. 2811 - 2816 (2015/12/18)
The synthesis of triaryl methanols was investigated by reacting different 4-metalated 2-substituted pyrimidines with diaryl ketones, the latter being generated by deprotocupration-aroylation of azine and diazine substrates. Cyclization of the triaryl meth
