New antimicrobial tetracycline analogue A (Nitrocycline) designed using chemoinformatics

Kassab, Mohammed M

doi:10.21608/ijhegy.2023.213460.1029

New antimicrobial tetracycline analogue A (Nitrocycline) designed using chemoinformatics

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/ijhegy.2023.213460.1029

Abstract

Background

In every country around the globe, bacterial resistance to antibiotics is a serious problem. Investigating new antibacterial medication sources is necessary in light of this. Tetracycline resistance is brought about through changes to the ribosome binding site and/or the development of mobile genetic elements carrying genes for resistance to tetracycline's.

The objective of the study:

The creation of new tetracycline antimicrobial analogues and testing of their in vitro antibacterial activity.

Methodology:

The current investigation was a screening experimental study. This research determined the minimum inhibitory concentrations (MI-Cs) of growth of several pathogenic microbes in Egypt by evaluating the in vitro antibacterial new tetracycline analog activity semi-synthetically synthesized from Streptomyces species. Tetracycline was purified using aqueous two-phase systems with polyethylene glycol and salts based on cholinium, which were then altered using chemo-informatics. The tetracycline analog A (nitrocycline) was created by adding an electron-withdrawing nitro group at position 7 of the tetracycline.

Results:

Although it showed less bacterial resistance than tetracycline, the antibiotic nitrocycline (tetracycline analogue A) was a more effective bacteriostatic antibacterial agent. When compared to the tetracycline prototype antibiotic, tetracycline analogue A demonstrated MICs of less than 10 micrograms/ml for bacterial growth, reflecting its potent antimicrobial activity.

Conclusion:

The development of a nitrocycline antibiotic with a broad range of activity, which helps in addressing the formidable problem of bacterial resistance, made this study intriguing.

Keywords