DEVELOPMENT OF NOVEL ANTIMICROBIAL TETRACYCLINE ANALOG B (IODOCYCLINE) BY CHEMO-INFORMATICS.

Document Type : Original Article

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Instructor of molecular biology, microbiology,immunology,faculty of pharmacy,Cairo university,Egypt Specialist of pharmacology, toxicology and clinical pharmacy.

Abstract

Background: Bacterial resistance to antibiotics is an overwhelming solemn challenge worldwide. This calls for exploratory for novel origins of antibacterial drugs. Tetracycline resistance is mediated via mutations within the ribosomal binding site and/or the attainment of mobile genetic elements bearing tetracycline-specific resistance genes. The aim of the study: Design of novel antimicrobial tetracycline analogs and screening of their in vitro antibacterial activity. Methodology: Our study type was a screening experimental study. In this work, in vitro antimicrobial novel tetracycline, analog activity semi-synthetically produced from Streptomyces species was evaluated by standard agar dilution technique determining their minimum inhibitory concentrations (MICs) of growth of different pathogenic bacteria in Egypt. Tetracycline was purified by aqueous two-phase systems consisting of cholinium-based salts and polyethylene glycol, then modified by chemo-informatics. The addition of electron-with drawing Iodide anion at carbon 7 position to tetracycline originated tetracycline analog B (iodocycline). Results and discussion iodocycline(tetracycline analog B) antibiotic was a more active bacteriostatic antibacterial agent than tetracycline but demonstrated less bacterial resistance. Tetracycline analog B showed MICs of less than 10 micrograms/ml for bacterial growth which reflected its powerful antimicrobial activity in a comparison with the chloramphenicol prototype antibiotic.

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Ain Shams Medical Journal
Volume 73, Issue 4
December 2022
Pages 969-981

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