Structure‐Based Design, Synthesis, and Biological Evaluation of Triazole‐Based smHDAC8 Inhibitors

Schistosomiasis is a neglected tropical disease caused by parasitic flatworms of the genus Schistosoma, which affects over 200 million people worldwide and leads to at least 300,000 deaths every year. In this study, initial screening revealed the triazole‐based hydroxamate 2 b (N‐hydroxy‐1‐phenyl‐1H...

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Veröffentlicht in:	ChemMedChem 2020-04, Vol.15 (7), p.571-584
Hauptverfasser:	Kalinin, Dmitrii V., Jana, Sunit K., Pfafenrot, Maxim, Chakrabarti, Alokta, Melesina, Jelena, Shaik, Tajith B., Lancelot, Julien, Pierce, Raymond J., Sippl, Wolfgang, Romier, Christophe, Jung, Manfred, Holl, Ralph
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antiparasitic agents Biochemistry, Molecular Biology Chemistry, Medicinal crystal structures Crystallography Drug Design Flatworms Histone deacetylase Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - chemistry Histone Deacetylase Inhibitors - pharmacology histone deacetylases Histone Deacetylases - metabolism Humans Inhibitors Life Sciences Life Sciences & Biomedicine Medication Microbiology and Parasitology Models, Molecular molecular docking studies Molecular Structure Parasitic diseases Parasitology Pharmaceutical sciences Pharmacology & Pharmacy Repressor Proteins - antagonists & inhibitors Repressor Proteins - metabolism Schistosoma mansoni Schistosoma mansoni - enzymology Schistosomiasis Schistosomiasis - drug therapy Schistosomiasis - metabolism Science & Technology Selectivity Structural Biology triazole derivatives Triazoles Triazoles - chemical synthesis Triazoles - chemistry Triazoles - pharmacology Tropical diseases
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