22720-75-8Relevant articles and documents
Inhibitors of tissue-nonspecific alkaline phosphatase: Design, synthesis, kinetics, biomineralization and cellular tests
Debray, Julien,Chang, Lei,Marquès, Stéphanie,Pellet-Rostaing, Stéphane,Le Duy, Do,Mebarek, Saida,Buchet, René,Magne, David,Popowycz, Florence,Lemaire, Marc
, p. 7981 - 7987 (2013)
Chronic kidney disease (CKD) is associated with numerous metabolic and endocrine disturbances, including abnormalities of calcium and phosphate metabolism and an inflammatory syndrome. The latter occurs early in the course of CKD and contributes to the development and progression of vascular calcification. A few therapeutic strategies are today contemplated to target vascular calcification in patients with CKD: vitamin K2, calcimimetics and phosphate binders. However, none has provided complete prevention of vascular calcification and there is an urgent need for alternate efficient treatments. Recent findings indicate that tissue-nonspecific alkaline phosphatase (TNAP) may represent a very promising drug target due to its participation in mineralization by vascular smooth muscle cells. We report the synthesis of four levamisole derivatives having better inhibition property on TNAP than levamisole. Their IC50, Ki and water solubility have been determined. We found that the four inhibitors bind to TNAP in an uncompetitive manner and are selective to TNAP. Indeed, they do not inhibit intestinal and placental alkaline phosphatases. Survival MTT tests on human MG-63 and Saos-2 osteoblast-like cells have been performed in the presence of inhibitors. All the inhibitors are not toxic at concentrations that block TNAP activity. Moreover, they are able to significantly reduce mineralization in MG63 and Saos-2 osteoblast-like cells, indicating that they are promising molecules to prevent vascular calcification.
Synthesis of substituted 2-mercaptobenzaldehydes and 2-substituted benzo[b]thiophenes
Gallagher, Timothy,Pardoe, David A.,Porter, Roderick A.
, p. 5415 - 5418 (2000)
Simple and rapid single-pot preparations of substituted 2- mercaptobenzaldehydes 5 and 2-substituted benzo[b]thiophenes 3 based on ortho-lithiation methodology are described. (C) 2000 Elsevier Science Ltd.
Investigation on the one-step preparation of 2-substituted benzo[B]thiophenes
Zhao, Qian,Qian, Chao,Chen, Xin-Zhi
, p. 873 - 878 (2013)
A convenient and efficient synthesis of 2-substituted benzo[b]thiophenes is described. This one-step reaction of alkylthiobenzaldehyde and activated electrophiles proceeded smoothly in toluene at 120 °C with magnesium oxide as a catalyst. The target 2-sub
Iron–PNP-Pincer-Catalyzed Transfer Dehydrogenation of Secondary Alcohols
Budweg, Svenja,Wei, Zhihong,Jiao, Haijun,Junge, Kathrin,Beller, Matthias
, (2019/05/10)
The well-defined iron PNP pincer complex catalyst [Fe(H)(BH4)(CO)(HN{CH2CH2P(iPr)2}2] was used for the catalytic dehydrogenation of secondary alcohols to give the corresponding ketones. Using acetone as inexpensive hydrogen acceptor enables the oxidation with good to excellent yields. DFT computations indicate an outer-sphere mechanism and support the importance of an acceptor to achieve this transformation under milder conditions.
Thiyl radical promoted chemo- and regioselective oxidation of CC bonds using molecular oxygen: Via iron catalysis
Xiong, Baojian,Zeng, Xiaoqin,Geng, Shasha,Chen, Shuo,He, Yun,Feng, Zhang
supporting information, p. 4521 - 4527 (2018/10/17)
The first example of the thiyl radical promoted ligand-free iron-catalyzed oxidative cleavage of alkenes using molecular oxygen (1 atm) has been developed. The reaction proceeds under mild reaction conditions with high efficiency and high chemo- and regioselectivity. It features a broad substrate scope and excellent functional group compatibility, enabling facile access to valuable molecules for application in medicinal chemistry. Preliminary mechanistic studies reveal that a vital intermediate dioxetane might be involved in the reaction and a thiyl radical plays a synergistic role in facilitating the selective oxidation of the CC bond.
