28593-25-1Relevant academic research and scientific papers
Preparation and application of triazole heterocyclic compound containing heteroaryl amide structure
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Paragraph 0121; 0125; 0126, (2019/11/14)
The invention discloses a triazole heterocyclic compound containing a heteroaryl amide structure, a geometrical isomer of triazole heterocyclic compound containing the heteroaryl amide structure and pharmacologically acceptable salt, hydrate, solvate or p
Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors
Liscio, Paride,Carotti, Andrea,Asciutti, Stefania,Karlberg, Tobias,Bellocchi, Daniele,Llacuna, Laura,Macchiarulo, Antonio,Aaronson, Stuart A,Schüler, Herwig,Pellicciari, Roberto,Camaioni, Emidio
supporting information, p. 2807 - 2812 (2014/04/17)
Searching for selective tankyrases (TNKSs) inhibitors, a new small series of 6,8-disubstituted triazolo[4,3-b]piridazines has been synthesized and characterized biologically. Structure-based optimization of the starting hit compound NNL (3) prompted us to the discovery of 4-(2-(6-methyl-[1,2,4] triazolo[4,3-b]pyridazin-8-ylamino)ethyl)phenol (12), a low nanomolar selective TNKSs inhibitor working as NAD isostere as ascertained by crystallographic analysis. Preliminary biological data candidate this new class of derivatives as a powerful pharmacological tools in the unraveling of TNKS implications in physiopathological conditions.
Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against plasmodium falciparum dihydroorotate dehydrogenase
Marwaha, Alka,White, John,El-mazouni, Farah,Creason, Sharon A,Kokkonda, Sreekanth,Buckner, Frederick S.,Charman, Susan A.,Phillips, Margaret A.,Rathod, Pradipsinh K.
, p. 7425 - 7436 (2012/11/07)
Plasmodium falciparum causes approximately 1 million deaths annually. However, increasing resistance imposes a continuous threat to existing drug therapies. We previously reported a number of potent and selective triazolopyrimidine-based inhibitors of P.
