Design of novel antimicrobial tetracycline analog by chemo-informatics

Kassab, Mohammed M

doi:10.21608/asmj.2022.157597.1039

Design of novel antimicrobial tetracycline analog by chemo-informatics

Articles in Press

Document Type : Original Article

Author

Mohammed M Kassab

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

10.21608/asmj.2022.157597.1039

Abstract

Background
Bacterial resistance to antibiotics is an irresistible earnest 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 objective 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 deciding 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-withdrawing nitro group at carbon 7 position to tetracycline originated tetracycline analog A(nitrocycline).
Results and discussion
Nitrocycline(tetracycline analog A) antibiotic was a more active bacteriostatic antibacterial agent than tetracycline but demonstrated less bacterial resistance. Tetracycline analog A showed MICs of less than 10 micrograms/ml for bacterial growth which reflected its potent antimicrobial activity in comparison with the tetracycline prototype antibiotic.

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