DRUG DISCOVERY OF NEWER ANALOGS OF ANTI-MICROBIALS THROUGH ENZYME-INHIBITION: A REVIEW
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2014, Vol 6, Issue 10
Abstract
There is a growing interest towards the development of new antibiotics from last decades due to emergence of newer pathogenic bacterial strains with high resistance to powerful antibiotics of last resort. This has caused decline in research for developing newer antibacterial agents. Hence, there is continuous need to develop newer antibiotics that interact with essential mechanisms in bacteria. Recently, enzymes responsible for bio synthesis of the essential amino acid lysine in bacteria have been targeted and it has augmented interest to develop novel antibiotics and to enhance lysine yields in over-producing organisms. Peptidoglycan layer consists of a beta-1,4-linked polysaccharide of alternating N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM) sugar units, cross linked by short pentapeptide (muramyl residues) side chain of general structure L-Ala-g-D-Glu-X- D-Ala-D-Ala, where X is either L–Lysine or meso-DAP. Formation of the cross-links makes bacterial cell wall resistant to lysis by intracellular osmotic pressure. Compounds which inhibit lysine or DAP biosynthesis could therefore be very effective antibiotics and novel targets. Lysine is a constituent in gram-positive bacteria while meso-DAP occurs in gram negative ones. In this review, substrate-based inhibitors of enzymes in the DAP pathway and inhibitors that allow better understanding of enzymology of the targets and provide insight for design of new inhibitors have been discussed. Resistant bacterial strains can be inhibited by using synthetic enzyme inhibitors of DAP pathway that are less toxic to mammals. Newer antimicrobial drugs can be thus developed by targeting the enzymes involved in this pathway.Â
Authors and Affiliations
Mayura Ajay Kale, Sayeed Sk Mohammad
Keywords
Related Articles
- EP ID EP579391
- DOI -
- Views 79
- Downloads 0
THE INFLUENCE OF ADDING ANTIBIOTIC IN TREATMENT OF RHEUMATOID ARTHRITIS PATIENTS ON STREPTOCOCCUS PYOGENES CARRIER RATE AND ON THE LIPIDS PROFILE
Objective: The main goal is to evaluate the clinical efficacy, safety, and tolerability of antibiotics and methotrexate (MTX) treatment on the disease severity, on Streptococcus pyogenes carrier rate and on the lipid pro...
PREPARATION AND EVALUATION OF METRONIDAZOLE SUSTAINED RELEASE FLOATING TABLETS
Objective: The objective of the present study is the preparation of metronidazole (MZ) floating tablets that are designed to retain in the stomach for a long time for better eradication of Helicobacter Pylori (H. pylori)...
INFLUENCE OF ZINC OXIDE NANOPARTICLES ON GROWTH OF SESAMUM INDICUM L. IN ZINC DEFICIENT SOIL
Objective: A comparative examine of L. aculeate mediated ZnO (BZnO) and synthesized chemical ZnO (CZnO) nanoparticles became done which will decide the impact of seed germination on Sesamum indicum (CO-1). Methods: Zinc...
PREVENTIVE AND CURATIVE MEASURES ADOPTED BY DENTISTS TO COMBAT OCCUPATIONAL HAZARDS–A CROSS SECTIONAL STUDY
Objectives: To assess various measures undertaken to overcome the occupational hazards among dentists in Bellary.Methods: This was a cross sectional questionnaire study.Results: Only nine dentists were still doing amalga...
ISOLATION AND CHARACTERISATION OF NOVEL IMPURITY OF LANSOPRAZOLE FORMED IN THERMAL STRESS CONDITION
Objective: The aim of the research work is to study the degradation of Lansoprazole in stress condition which is a proton pump inhibitor and controls the production of gastric acid in stomach. Thermal stress condition ha...