On January 1, 2021, Hao, Guiyun; Li, Hao; Yang, Fei; Dong, Duoling; Li, Zezhong; Ding, Yingying; Pan, Wei; Wang, Enduo; Liu, Rujuan; Zhou, Huchen published an article.Computed Properties of 53136-21-3 The title of the article was Discovery of benzhydrol-oxaborole derivatives as Streptococcus pneumoniae leucyl-tRNA synthetase inhibitors. And the article contained the following:
1-Hydroxy-2,1-benzoxaboroles I were prepared and examined for inhibitory activity against leucyl-tRNA synthetase (LeuRS) and antibacterial activity against multidrug-resistant S. pneumoniae pathogen. Pneumonia caused by bacterium S. pneumoniae is a severe acute respiratory infectious disease with high morbidity and mortality, especially for children and immunity-compromised patients. The emergence of multidrug-resistant S. pneumoniae also presents a challenge to human health. Leucyl-tRNA synthetase (LeuRS) catalyzes the attachment of L-leucine to tRNALeu, which plays an essential role in protein translation and is considered an attractive antimicrobial drug target. In the present work, benzhydrol-oxaborole hybrid compounds were designed and synthesized as inhibitors of S. pneumoniae LeuRS. Exploration of the Ph ring near Lysine 389 eventually yielded compounds 46 and 54 with submicromolar inhibitory potency. The co-crystal of compound 54 in the editing domain pocket of SpLeuRS was obtained and confirmed the formation of an addnl. hydrogen bond between the carbonyl of 54 and Lysine 389. It also showed anti-pneumococcal activity in vitro. The structure-activity relationship was discussed. This work will provide an essential foundation for the further development of anti-pneumococcal agents by targeting LeuRS. The experimental process involved the reaction of Benzyl(4-bromophenyl)sulfane(cas: 53136-21-3).Computed Properties of 53136-21-3
The Article related to benzoxaborole boronate preparation leucyl trna synthetase inhibitor antibacterial agent, streptococcus pneumoniae leucyl trna synthetase inhibitor antibacterial agent preparation, anti-pneumonia, benzhydrol-oxaborole, s. pneumonia leurs (spleurs), structure-activity relationship and other aspects.Computed Properties of 53136-21-3
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