51646-17-4Relevant articles and documents
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.
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.
Novel substituted 1,2,4-triazolo- [1,5-a] pyrimidine-2-sulfonamides and compositions and methods of controlling undesired vegetation and suppressing the nitrification of ammonium nitrogen in soil
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, (2008/06/13)
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