91066-67-0Relevant articles and documents
Heterocyclic compounds as well as preparation method and application thereof
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Paragraph 0116; 0117; 0118; 0152; 0153, (2018/07/30)
The invention belongs to the field of medicines and particularly relates to heterocyclic compounds with the structural characteristics shown in formula (I) or pharmaceutically acceptable salts, a preparation method and an application of the heterocyclic compounds as a nucleotide oxidative damage repairase MTH1 inhibitor. Pharmacological experiment results indicate that the compounds have significant inhabitation effects on the activity of MTH1 and can be used for preventing and treating clinical diseases related to MTH1.
Triamino pyrimidines and pyridines as histamine H4 receptor modulators
Meduna, Steven P.,Savall, Brad M.,Cai, Hui,Edwards, James P.,Thurmond, Robin L.,McGovern, Patricia M.
supporting information; experimental part, p. 3113 - 3116 (2011/06/26)
Two series of triamino pyrimidines and a series of triamino pyridines have been synthesized and their structure-activity relationships evaluated for activity at the H4 receptor in competitive binding and functional assays. Small structural changes in these three hetereoaromatic cores influenced the functional activity of these compounds.
2,4-Diaminopyrimidines as histamine H4 receptor ligands-Scaffold optimization and pharmacological characterization
Sander, Kerstin,Kottke, Tim,Tanrikulu, Yusuf,Proschak, Ewgenij,Weizel, Lilia,Schneider, Erich H.,Seifert, Roland,Schneider, Gisbert,Stark, Holger
experimental part, p. 7186 - 7196 (2010/03/03)
The human histamine H4 receptor (hH4R) is a promising new target in the therapy of inflammatory diseases and disorders of the immune system. For the development of new H4R antagonists a broad ligand-based virtual screening was performed resulting in two hits. The dissection of their common annelated aromatic core into its heteromonocyclic components showed that 2,4-diaminopyrimidine is a potent hH4R affinity scaffold, which was comprehensively investigated. Structure-activity relationship studies revealed that slight structural changes evoke extensive differences in functional activities and potencies: while o- and p-substituted benzyl amines mainly showed partial agonism, m-substituted and rigidified ones exhibited inverse agonist efficacy.