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

摘要

abstract_textpA 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./p/abstract_text