23814-12-2Relevant articles and documents
INDAZOLES AS LRRK2 INHIBITORS
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Page/Page column 99, (2020/10/09)
The present invention is directed to indazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
New geldanamycin derivatives with anti Hsp properties by mutasynthesis
Hermane, Jekaterina,Eichner, Simone,Mancuso, Lena,Schr?der, Benjamin,Sasse, Florenz,Zeilinger, Carsten,Kirschning, Andreas
supporting information, p. 5269 - 5278 (2019/06/07)
Mutasynthetic supplementation of the AHBA blocked mutant strain of S. hygroscopicus, the geldanamycin producer, with 21 aromatic and heteroaromatic amino acids provided new nonquinoid geldanamycin derivatives. Large scale (5 L) fermentation provided four new derivatives in sufficient quantity for full structural characterisation. Among these, the first thiophene derivative of reblastatin showed strong antiproliferative activity towards several human cancer cell lines. Additionally, inhibitory effects on human heat shock protein Hsp90α and bacterial heat shock protein from H. pylori HpHtpG were observed, revealing strong displacement properties for labelled ATP and demonstrating that the ATP-binding site of Hsps is the target site for the new geldanamycin derivatives.
The discovery of new scaffold of plant activators: From salicylic acid to benzotriazole
Chang, Kang,Chen, Jian-Qin,Shi, Yan-Xia,Sun, Mei-Jian,Li, Peng-Fei,Zhao, Zhen-Jiang,Zhu, Wei-Ping,Li, Hong-Lin,Xu, Yu-Fang,Li, Bao-Ju,Qian, Xu-Hong
, p. 919 - 926 (2017/05/16)
Started from salicylic acid (SA) and related commercialized plant activators, based on molecular three-dimensional shape and pharmacophore similarity comparison (SHAFTS), a new lead compound benzotriazole was predicted and a series of benzotriazole derivatives were designed and synthesized. The bioassay showed that benzotriazole had high activity against a broad spectrum of diseases including fungi and oomycetes in vivo, but no activity in vitro. And the introduction of proper groups at the 1’-position and 5’-position was beneficial to the activity. So, they had the potential to be exploited as novel plant activators.
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Page/Page column 43, (2012/11/08)
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
Compound and use
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, (2008/06/13)
A compound contains a ligand group and at least one group of the general formula --XRn where X is a linking group which contains at least one hetero-atom, R is a saturated hydrocarbyl group containing at least six carbon atoms or is an unsaturated hydrocarbyl group containing at least three carbon atoms. The ligand group can be a polyhydroxyhydrocarbyl, a triazole, an imidazole, an indazole, a thiazole, an oxazole, a carbamate, an xanthate or a phthalazine. The compounds can be used to improve bonding between a metal and a coating material in contact with the metal surface. The metal may be a tire cord and the coating material rubber or a rubber composition.
Hydrolytic Stability of Alkyl 1H-Benzotriazolecarboxylates
Jacobi, Sylvia,Hoffmann, Hermann
, p. 89 - 92 (2007/10/02)
Hydrolysis of 1H-benzotriazolecarboxylates was studied in 0.1 M NaOH, phosphate buffer pH 7.4 and using a microsomal esterase preparation.Results obtained for the alkaline hydrolysis qualitatively resembled those of enzymatic hydrolysis.In phosphate buffer pH 7.4 the esters were sufficiently stable concerning their use as potential substrates for in vitro biotransformation studies.
