318967-75-8Relevant articles and documents
Synthesis and BK channel-opening activity of 2-amino-1,3-thiazole derivatives
Cui, Yong-Mei,Ji, Tong-Tong,Jo, Heeji,Lin, Hai-Xia,Park, Chul-Seung,Qi, Xiao-Lei,Wang, Xue-Ying
, (2021/05/19)
A series of 2-amino-5-arylmethyl- or 5-heteroarylmethyl-1,3-thiazole derivatives were synthesized and evaluated for BK channel-opening activities in cell-based fluorescence assay and electrophysiological recording. The assay results indicated that the activities of the investigated compounds were influenced by the physicochemical properties of the substituent at benzene ring.
Design and synthesis of thiadiazoles and thiazoles targeting the Bcr-Abl T315I mutant: From docking false positives to ATP-noncompetitive inhibitors
Radi, Marco,Crespan, Emmanuele,Falchi, Federico,Bernardo, Vincenzo,Zanoli, Samantha,Manetti, Fabrizio,Schenone, Silvia,Maga, Giovanni,Botta, Maurizio
scheme or table, p. 1226 - 1231 (2011/02/21)
(Figure Presented) Overcoming resistance: In an effort to optimize our previously identified dual Src/Abl hits, a new series of 1,3,4-thiadiazoles and 1,3-thiazoles were designed and synthesized, paying particular attention to the reduction of their lipophilicity and to the improvement of the affinity towards the drug-resistant T315I mutant. Compound 5 was identified as a promising allosteric inhibitor of the T315I mutant.
ANTI-HIV COMPOUNDS
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Page/Page column 79-80, (2009/08/14)
Thiazole derivatives represented by Formula (I) are disclosed, where R1, R2, R3, A, X, Y, Z, R6 and R7 are disclosed herein. These thiazole derivatives and pharmaceutical compositions comprising these derivatives are useful in the treatment of HIV mediated diseases and conditions.
Heterocyclic compounds and medical use thereof
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, (2008/06/13)
The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.