New Antimicrobial Leads in Phenothiazine Scaffold: Synthesis, Biological Assay and Virtual Screening

被引：5

作者：

Onoabedje, Efeturi A. ^{[1
]}

Ibezim, Akachukwu ^{[2
]}

Onoabedje, Ufuoma S. ^{[2
]}

Egu, Samuel A. ^{[3
]}

Okoro, Uchechukwu C. ^{[1
]}

机构：

[1] Univ Nigeria, Dept Pure & Ind Chem, Nsukka, Enugu State, Nigeria

[2] Univ Nigeria, Fac Pharmaceut Sci, Nsukka, Enugu State, Nigeria

[3] Kogi State Coll Educ, Dept Chem, Ankpa, Kogi State, Nigeria

来源：

CHEMISTRYSELECT | 2017年 / 2卷 / 36期

关键词：

antibacterial; antifungal; antimicrobial; molecular docking; phenothiazine; phenoxazine and synthesis; OCCURRING ANTIBACTERIAL AGENT; PEPTIDE DEFORMYLASE; INHIBITORS; ACTINONIN; PREDICT;

D O I：

10.1002/slct.201701804

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A variety of 2-substituted 10H-phenothiazine were synthesized via palladium catalyzed cross-coupling reactions and showed good activity against bacillus cereus, staphylococcus aureus, escherichia coli, pseudomonas aeruginosa bacteria. Particularly, thiophenyl and furanyl derivatives exhibited broad spectrum of activities over phenyl, styryl, alkynyl and arynyl derivatized compounds. In addition, virtual screening revealed that all the phenothiazines stopped the activity of NMT at concentrations ranging from 147.00 nM to 9.11M. Two derivatives, 2-phenyl-10H-phenothiazine and 2-styryl-10H-phenothiazine, were identified as novel inhibitors of two validated antimicrobial drug targets (peptide deformylase and N-myristoyl transferase) according to theoretical binding free energy calculations.

引用

页码：11954 / 11958

页数：5

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