- Preparation and application of triazole heterocyclic compound containing heteroaryl amide structure
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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
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Paragraph 0121-0124
(2019/11/14)
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- Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors
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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.
- Liscio, Paride,Carotti, Andrea,Asciutti, Stefania,Karlberg, Tobias,Bellocchi, Daniele,Llacuna, Laura,Macchiarulo, Antonio,Aaronson, Stuart A,Schüler, Herwig,Pellicciari, Roberto,Camaioni, Emidio
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supporting information
p. 2807 - 2812
(2014/04/17)
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- Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against plasmodium falciparum dihydroorotate dehydrogenase
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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.
- Marwaha, Alka,White, John,El-mazouni, Farah,Creason, Sharon A,Kokkonda, Sreekanth,Buckner, Frederick S.,Charman, Susan A.,Phillips, Margaret A.,Rathod, Pradipsinh K.
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p. 7425 - 7436
(2012/11/07)
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