title: Antibacterial evaluation of structurally amphipathic, membrane active small cationic peptidomimetics: synthesized by incorporating 3-amino benzoic acid as peptidomimetic element.
abstract: A new series of small cationic peptidomimetics were synthesized by incorporating 3-amino benzoic acid (3-ABA) in a small structural framework with the objective to mimic essential properties of natural antimicrobial peptides (AMPs). The new design approach resulted into improvement of activity and selectivity in comparison to linear peptides and allowed us to better understand the influence of structural amphipathicity on biological activity. Lead peptidomimetics displayed antibacterial activities against resistant pathogens (MRSA & MRSE). A calcein dye leakage experiment revealed a membranolytic effect of 4g and 4l which was further confirmed by fluorescence microscopy. In addition, proteolytic stability and no sign of resistance development against Staphylococcus aureus and MRSA demonstrate their potential for further development as novel antimicrobial therapeutics.
authors: Department of Pharmacy, Jaypee University of Information Technology, Solan 173234, India.
authors: Sandeep
authors: S
authors: Lohan
authors: Environmental Biotechnology & Microbial Biochemistry, Institute of Microbial Technology, Chandigarh 160036, India.
authors: Swaranjit Singh
authors: SS
authors: Cameotra
authors: Department of Pharmacy, Jaypee University of Information Technology, Solan 173234, India. Electronic address: bishtchemjuit@rediffmail.com.
authors: Gopal Singh
authors: GS
authors: Bisht
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D019817:Benzoic Acid / Q000737:chemistry*; D002460:Cell Line; D002462:Cell Membrane / Q000187:drug effects*; D015195:Drug Design; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D004355:Drug Stability; D004912:Erythrocytes / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D055624:Methicillin-Resistant Staphylococcus aureus / Q000166:cytology / Q000187:drug effects; D008958:Models, Molecular; D008968:Molecular Conformation; D057786:Peptidomimetics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000900:Anti-Bacterial Agents; D057786:Peptidomimetics; D019817:Benzoic Acid
keywords: 3-Amino benzoic acid; Antibacterial peptidomimetics; Antibiotic resistance; Plasma stability