110598-56-6Relevant articles and documents
Diarylethenes display in vitro anti-TB activity and are efficient hits targeting the mycobacterium tuberculosis HU Protein
Suarez, María Angélica,Valencia, Jhesua,Cadena, Christian Camilo,Maiti, Raktim,Datta, Chandreyee,Puerto, Gloria,Isaza, José Hipólito,Juan, Homero San,Nagaraja, Valakunja,Guzman, Juan David
, (2017)
Tuberculosis continues to be a great source of concern in global health because of the large reservoir of humans infected with the bacilli and the appearance of clinical isolates resistant to a wide array of anti-tuberculosis drugs. New drugs with novel mechanisms of action on new targets are urgently required to reduce global tuberculosis burden. Mycobacterium tuberculosis nucleoid associated protein (NAP) HU has been shown to be druggable and essential for the organism’s survival. In this study, four diarylethenes were synthesized using a one-pot decarboxylated Heck-coupling of coumaric acids with iodoanisoles. The prepared compounds 1–4 were tested for their in vitro growth inhibition of M. tuberculosis H37Rv using the spot culture growth inhibition assay, displaying minimum inhibitory concentrations between 9 and 22 μM. Their cytotoxicity against BHK-21 cell line showed half inhibition at concentrations between 98 and 729 μM. The most selective hit (SI = 81), demonstrated inhibition of M. tuberculosis HU protein involved in maintaining bacterial genome architecture.
Hydroxyl Assisted, Photoredox/Cobalt Co-catalyzed Semi-Hydrogenation and Tandem Cyclization of o-Alkynylphenols for Access to 2,3-Dihydrobenzofurans
Tian, Wan-Fa,Zhu, Yao,He, Yong-Qin,Wang, Mei,Song, Xian-Rong,Bai, Jiang,Xiao, Qiang
supporting information, p. 730 - 736 (2020/12/15)
Herein, a hydroxyl assisted, photoredox/cobalt co-catalyzed semi-hydrogenation and tandem cyclization of o-alkynylphenols is developed towards direct assembly of 2,3-dihydrobenzofurans. Moderate to good yields were obtained for a range of sterically and electronically diverse 2-propynolphenols under mild conditions. Mechanistic studies demonstrated the inevitable role of the alcoholic hydroxyl group with (Z)-alkene as the real intermediate. Finally, a key low-valent cobalt catalyzed intramolecular hydroetherification of alkene is proposed. (Figure presented.).
Preparation method of benzofuran derivative
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Paragraph 0054-0058, (2020/11/12)
The invention belongs to the field of organic chemical synthesis, and particularly relates to a preparation method of a benzofuran derivative. According to the specific technical scheme, the preparation method of the benzofuran derivative comprises the fo
Late-Stage Direct o-Alkenylation of Phenols by PdII-Catalyzed C?H Functionalization
Dou, Yandong,Kenry,Liu, Jiang,Jiang, Jianze,Zhu, Qing
supporting information, p. 6896 - 6901 (2019/05/07)
o-Alkenylation of unprotected phenols has been developed by direct C?H functionalization catalyzed by PdII. This work features phenol group as a directing group and realizes highly site-selective C?H bond functionalization of phenols to achieve the corresponding products in moderate to excellent yields at 60 °C. The advantages of this reaction include unprecedented C?H functionalization using phenol as a directing group, high regioselectivity, good substrate scope, mild reaction conditions, and high efficiency. To the best of our knowledge, this is the first example of a regioselective C?H alkenylation of unprotected phenols utilizing phenolic hydroxyl group as a directing group. The alkenylation of unprotected tyrosine and intramolecular cyclization are also successfully carried out under this catalytic system in good yields. Furthermore, this novel method enables a late-stage modification of complex phenol-containing bioactive molecules toward a diversity-oriented drug discovery.
