38544-16-0Relevant articles and documents
Exploring intermolecular contacts in multi-substituted benzaldehyde derivatives: X-ray, Hirshfeld surface and lattice energy analyses
Hosten, Eric C.,Hulushe, Siya T.,Louzada, Marcel,Manyeruke, Meloddy H.,Rigin, Sergei,Watkins, Gareth M.
, p. 16861 - 16874 (2020/05/18)
Crystal structures of six benzaldehyde derivatives (1-6) have been determined and their supramolecular networks were established by an X-ray crystallographic study. The study has shown that the compounds are linked by various intermolecular interactions s
3-Arylpropionylhydroxamic acid derivatives as Helicobacter pylori urease inhibitors: Synthesis, molecular docking and biological evaluation
Shi, Wei-Kang,Deng, Rui-Cheng,Wang, Peng-Fei,Yue, Qin-Qin,Liu, Qi,Ding, Kun-Ling,Yang, Mei-Hui,Zhang, Hong-Yu,Gong, Si-Hua,Deng, Min,Liu, Wen-Run,Feng, Qiu-Ju,Xiao, Zhu-Ping,Zhu, Hai-Liang
, p. 4519 - 4527 (2016/09/13)
Helicobacter pylori urease is involved in several physiologic responses such as stomach and duodenal ulcers, adenocarcinomas and stomach lymphomas. Thus, inhibition of urease is taken for a good chance to treat H. pylori-caused infections, we have therefore focused our efforts on seeking novel urease inhibitors. Here, a series of arylpropionylhydroxamic acids were synthesized and evaluated for urease inhibition. Out of these compounds, 3-(2-benzyloxy-5-chlorophenyl)-3-hydroxypropionylhydroxamic acid (d24) was the most active inhibitor with IC50of 0.15?±?0.05?μM, showing a mixed inhibition with both competitive and uncompetitive aspects. Non-linear fitting of kinetic data gives kinetics parameters of 0.13 and 0.12?μg·mL?1for Kiand Ki′, respectively. The plasma protein binding assays suggested that d24 exhibited moderate binding to human and rabbit plasma proteins.
Synthesis and evaluation of 3-hydroxy-3-phenylpropanoate ester-AZT conjugates as potential dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors
Manyeruke, Meloddy H.,Olomola, Temitope O.,Majumder, Swarup,Abrahams, Shaakira,Isaacs, Michelle,Mautsa, Nicodemus,Mosebi, Salerwe,Mnkandhla, Dumisani,Hewer, Raymond,Hoppe, Heinrich C.,Klein, Rosalyn,Kaye, Perry T.
, p. 7521 - 7528 (2015/12/18)
Novel 3-hydroxy-3-phenylpropanoate ester-azidothymidine (AZT) conjugates have been prepared using Baylis-Hillman methodology, and their potential as dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors has been explored using enzyme inhibition