Deng, Lisheng; Diao, Jiasheng; Chen, Pinhong; Pujari, Venugopal; Yao, Yuan; Cheng, Gang; Crick, Dean C.; Prasad, B. V. Venkataram; Song, Yongcheng published an article in Journal of Medicinal Chemistry. The title of the article was 《Inhibition of 1-Deoxy-d-Xylulose-5-Phosphate Reductoisomerase by Lipophilic Phosphonates: SAR, QSAR, and Crystallographic Studies》.Application In Synthesis of (4-Phenylpyridin-2-yl)methanol The author mentioned the following in the article:
1-Deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) is a novel target for developing new antibacterial (including antituberculosis) and antimalaria drugs. Forty-one lipophilic phosphonates, representing a new class of DXR inhibitors, were synthesized, among which 5-phenylpyridin-2-ylmethylphosphonic acid possesses the most activity against E. coli DXR (EcDXR) with a Ki of 420 nM. Structure-activity relationships (SAR) are discussed, which can be rationalized using our EcDXR:inhibitor structures, and a predictive quant. SAR (QSAR) model is also developed. Since inhibition studies of DXR from Mycobacterium tuberculosis (MtDXR) have not been performed well, 48 EcDXR inhibitors with a broad chem. diversity were found, however, to generally exhibit considerably reduced activity against MtDXR. The crystal structure of a MtDXR:inhibitor complex reveals the flexible loop containing the residues 198-208 has no strong interactions with the 3,4-dichlorophenyl group of the inhibitor, representing a structural basis for the reduced activity. Overall, these results provide implications in the future design and development of potent DXR inhibitors. The results came from multiple reactions, including the reaction of (4-Phenylpyridin-2-yl)methanol(cas: 55218-73-0Application In Synthesis of (4-Phenylpyridin-2-yl)methanol)
(4-Phenylpyridin-2-yl)methanol(cas: 55218-73-0) belongs to hydroxy-containing compounds. Hydroxy-containing compounds engage in intermolecular hydrogen bonding increasing the electrostatic attraction between molecules and thus to higher boiling and melting points than found for compounds that lack this functional group. Organic compounds, which are often poorly soluble in water, become water-soluble when they contain two or more hydroxy groups, as illustrated by sugars and amino acid.Application In Synthesis of (4-Phenylpyridin-2-yl)methanol
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