We report here the affinity and antibacterial activity of a structurally similar class of neomycin dimers. The affinity of the dimer library for rRNA was established by using a screen that measures the displacement of fluorescein-neomycin (F-neo) probe from RNA. A rapid growth inhibition assay using a single drug concentration was used to examine the antibacterial activity. The structure-activi...

The development of antibacterial drugs based on novel chemotypes is essential to the future management of serious drug resistant infections. We herein report the design, synthesis and SAR of a novel series of N-ethylurea inhibitors based on a pyridine-3-carboxamide scaffold targeting the ATPase sub-unit of DNA gyrase. Consideration of structural aspects of the GyrB ATPase site has aided the dev...

The present study was carried out to evaluate the antibacterial activities ofethanolicand aqueous extracts of Kigelia africana (Bignoniaceae) and Carica papaya (Caricaceae) against multi drug resistant Pseudomonas aeruginosa UTI causing pathogen. The bacterial sp was isolated from urine sample of UTI infected patient and identified with the help of colony characterization, gram staining and bio...

Apramycin is a unique aminoglycoside with a dissociation of antibacterial activity and ototoxicity. We assessed the antibacterial efficacy of apramycin in two murine models of infection, Mycobacterium tuberculosis aerosol infection and Staphylococcus aureus septicemia. In both infection models, the efficacy of apramycin was comparable to that of amikacin. These results suggest that apramycin ha...

OBJECTIVES To explore patient, caregiver and physician perceptions and attitudes regarding the balance of benefit and risk in using antibacterial drugs developed through streamlined development processes. DESIGN Semistructured focus groups and in-depth interviews were conducted to elicit perceptions and attitudes about the use of antibacterial drugs to treat multidrug-resistant infections. Pa...

Escherichia coli (E. coli) is associated with necrotizing fasciitis (type I) and can induce enough damage to tissue causing hypoxia. Three ester derivatives of the broad-spectrum antibiotic ciprofloxacin were placed into bacteria culture simultaneously with the parent ciprofloxacin (drug 1) to ascertain the level of antibacterial activity. The n-propyl (drug 2), n-pentyl (drug 3), and n-octyl (...

New antimicrobial hydrogels were prepared via reaction of functionalized-Tragacanth Gum biopolymer by glycidyltrimethylammonium chloride (QTG) with acrylamide (AM). Characterization of the QTG hydrogels with AM (QTG-AM) was carried out by thermogravimetric analysis (TGA), Fourier-transform infrared spectroscopy (FTIR), and 1HNMR. Swelling behaviour of the QTG hydrogels was investigated on the p...

Introduction Methicillin-Resistant Staphylococcus aureus (MRSA) and Vancomycin-Resistant Enterococcus (VRE) have accomplished important rates of colonization and infection in most intensive care units. These multidrug-resistant strains of MRSA and VRE have been causing serious problems in health care. The rising clinical importance of drug-resistant pathogens has lent necessity to drug developm...

Benzyl-substituted metallocarbene compounds synthesised by our group and others during the past 5 years give a new perspective on their activity as antibiotic and antitumoral drugs. N-heterocyclic carbenes containing an imidazole core were functionalised and their transition metal complexes (M = Ag, Au, Cu, Ru) have shown promising antibacterial as well as anticancer activity in vitro and in vi...

BACKGROUND Gold nanoparticles are useful candidate for drug delivery applications and are associated with enhancement in the bioavailability of coated drugs and/or therapeutic agent. Since, heterocyclic compounds are known to exhibit antimicrobial potential against variety of pathogens, we designed this study to evaluate the antibacterial effects of gold nanoparticles conjugation with new synth...