51646-17-4Relevant academic research and scientific papers
Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins
Raux, Brigitt,Voitovich, Yuliia,Derviaux, Carine,Lugari, Adrien,Rebuffet, Etienne,Milhas, Sabine,Priet, Stéphane,Roux, Thomas,Trinquet, Eric,Guillemot, Jean-Claude,Knapp, Stefan,Brunel, Jean-Michel,Fedorov, Alexey Yu.,Collette, Yves,Roche, Philippe,Betzi, Stéphane,Combes, Sébastien,Morelli, Xavier
supporting information, p. 1634 - 1641 (2016/03/05)
A midthroughput screening follow-up program targeting the first bromodomain of the human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor. This compound binds with an affinity in the low micromolar range yet exerts suitable unexpected selectivity in vitro against the other members of the bromodomain and extra-terminal domain (BET) family. A structure-based program pinpointed a role of the ZA loop, paving the way for the development of potent and selective BET-BRDi probes.
SUBSTITUTED TRIAZOLO-PYRIMIDINE COMPOUNDS FOR MODULATING CELL PROLIFERATION, DIFFERENTIATION AND SURVIVAL
-
Paragraph 0551; 0552, (2014/05/25)
Disclosed herein are erythropoietin-mimetic compounds of Formula I, which modulate the survival, function, or differentiation of, for example, kidney cells, neurons, erythroid cells, or other erythropoietin-responsive cells. The present invention also relates to compounds and methods that preferentially modulate cells expressing the tissue-protective erythropoietin receptor. The compounds of the invention are useful in preventing and treating diseases, such as anemia, organ injury, and diseases of the central nervous system, and as an adjunct to cellular treatments, such as stem cell therapies.
Synthesis and antimicrobical evaluation of a novel class of 1,3,4-thiadiazole: Derivatives bearing 1,2,4-triazolo[1,5-a]pyrimidine moiety
Luo, Yin,Zhang, Shuai,Liu, Zhi-Jun,Chen, Wu,Fu, Jie,Zeng, Qing-Fu,Zhu, Hai-Liang
, p. 54 - 61 (2013/07/11)
A series of novel 1,3,4-thiadiazole derivatives bearing 1,2,4-triazolo[1,5-a]pyrimidine moiety were synthesized by the method of splicing active substructures. Among these derivatives, compounds 12, 13, 15-22 and 24-31 were firstly reported. All the compounds were assayed for antimicrobial activities against five fungi strains and four bacteria strains. The preliminary results indicated that compounds 25 and 28-31 showed good antifungal activities against Physaclospora piricola and Rhizoctonia solani. Compound 26 exhibited good antifungal activities against Cercospora beticola and R. solani. Most of the compounds showed better antibacterial activities against Gram-negative bacteria strains than Gram-positive bacteria strains. Compounds 25 and 28 showed the best activities against Pseudomonas fluorescence while compounds 30-31 showed good activities against Escherichia coli.
Synthesis and antifungal evaluation of 1,2,4-triazolo[1,5-α] pyrimidine bearing 1,2,4-triazole heterocycle derivatives
Chen,Xiang,Fu,Zeng,Zhu
scheme or table, p. 602 - 608 (2012/01/02)
In order to search novel fungicides with higher activity, 28 new 1,2,4-triazolo[1,5-α]pyrimidine derivatives bearing 1,2,4-triazole heterocycle were synthesized. Their structures were characterized by 1H NMR spectroscopy, mass spectrometry and elemental analyses. With triadimefon, validamycin and carbendazim as positive controls, the antifungal activities of 28 compounds against Fusarium oxysporum f. sp. vasinfectum, Gibberella sanbinetti, Cercospora beticola Sacc., Physaclospora piricola and Rhizoctonia solani were evaluated. Compound 2-[(5-(2,6- difluorobenzylthio)-4- phenyl-4H-1,2,4-triazol-3-yl)methylthio]-5,7-dimethyl[1,2,4]triazolo[1, 5-α]pyrimidine (19) showed potent antifungal activities against G. sanbinetti, C. beticola, P. piricola and R. solani. On the basis of the biological results, structure-activity relationships of these compounds were also discussed.
Substituted 1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamides, compositions containing them, and their utility as herbicides
-
, (2008/06/13)
Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonamides, e.g., 5,7-dimethyl-N-(2,6-dichlorophenyl)-1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamide and their agriculturally acceptable salts are prepared. These compounds and compositions containing them are useful for the control of unwanted vegetation. Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonyl chlorides and substituted anilines and their use as intermediates are also described.
Novel substituted 1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamides and compositions and method for inhibiting pollen formation in corn
-
, (2008/06/13)
Novel compounds, e.g., 5,7-dimethyl-N-(2,6-dichlorolphenyl)-1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamide and their compositions and use in the control of weeds and in the suppression of nitrification of ammonium nitrogen in soil. Other novel compounds and their compositions and use in the inhibition of bolting in sugar beets. Other novel compounds and their compositions and use as plant gametocides.
2-(Alkylthio)-1,2,4-triazolo[1,5-a]pyrimidines as adenosine cyclic 3',5'-monophosphate phosphodiesterase inhibitors with potential as new cardiovascular agents
Novinson,Springer,O'Brien,Scholten,Miller,Robins
, p. 420 - 426 (2007/10/02)
A series of new 2-(alkylthio)-5,7-disubstituted-1,2,4-triazolo[1,5-a]pyrimidines have been prepared as inhibitors of cAMP phosphodiesterase from various tissues. These derivatives were prepared via ring closure of various requisite 3-amino-1,2,4-triazole
