Design, Synthesis and Microbiological Evaluation of Novel Compounds as Potential Staphylococcus aureus Phenylalanine tRNA Synthetase Inhibitors

被引：3

作者：

Elbaramawi, Samar S. ^{[1
,2
]}

Hughes, Casey ^{[3
]}

Richards, Jennifer ^{[4
]}

Gupta, Arya ^{[5
]}

Ibrahim, Samy M. ^{[2
]}

Lashine, El-Sayed M. ^{[2
]}

El-Sadek, Mohamed E. ^{[2
]}

O'Neill, Alex J. ^{[5
]}

Wootton, Mandy ^{[4
]}

Bullard, James M. ^{[3
]}

Simons, Claire ^{[1
]}

机构：

[1] Cardiff Univ, Sch Pharm & Pharmaceut Sci, King Edward VII Ave, Cardiff CF10 3NB, S Glam, Wales

[2] Zagazig Univ, Fac Pharm, Dept Med Chem, Zagazig 44519, Egypt

[3] Univ Texas Rio Grande Valley, Dept Chem, 1201 W Univ Dr, Edinburg, TX 78541 USA

[4] Univ Hosp Wales, Specialist Antimicrobial Chemotherapy Unit, Heath Pk, Cardiff CF14 4XW, S Glam, Wales

[5] Univ Leeds, Fac Biol Sci, Sch Mol & Cellular Biol, Garstang Bldg, Leeds LS2 9JT, W Yorkshire, England

来源：

EGYPTIAN JOURNAL OF CHEMISTRY | 2018年 / 61卷

基金：

美国国家卫生研究院;

关键词：

Staphylococcus aureus; Phenylalanine tRNA synthetase; Drug design; Benzimiduzole; Indole; Adenine;

D O I：

10.21608/EJCHEM.2018.4070.1357

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

AS THE RESISTANCE of Staphylococcus aureus to antibiotics represents a major threat to global health, anti-infectives with novel mechanisms must be developed. Novel compounds were generated as potential phenylalanine tRNA synthetase (PheRS) inhibitors based on the published homology model of S. aureus PheRS to aid the design process using Molecular Operating Environment (MOE) software. PheRS was selected as it is structurally unique enzyme among the aminoacyl-tRNA synthetases (aaRS), it is considerably different from human cytosolic and human mitochondrial aaRS and it is essential and conserved across bacterial species. The designed compounds were synthesized according to different clear schemes. The compounds were confirmed by H-1 NMR, C-13 NMR, HRMS and/or microanalysis, and they were microbiologically evaluated.

引用

页码：9 / 25

页数：17

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