Synthesis of Benzylpenicillin esters and evaluate the change in the anti-bacterial effects by Docking and bacteriological study

Abdulrahman alsheikhly, Omar and R. Ganjo, Aryan and Sardar Abdulrahman, Hayman and Y. Issa, Sanaa (2024) Synthesis of Benzylpenicillin esters and evaluate the change in the anti-bacterial effects by Docking and bacteriological study. Diyala Journal of Medicine, 26 (1). ISSN 2617-8982

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Abstract

Background: Benzylpenicillin is an antibiotic that possesses effectiveness mainly against gram-positive and some gram-negative bacteria. The carboxylic acid of beta-lactam is essential for its antibacterial activity. However, many prodrugs have been produced through the esterification of this carboxylic acid group, like Pivampicillin. Objective: To evaluate the antibacterial effects of Benzylpenicillin when the free carboxylic acid mask with different chemical groups of different polarity. Patients and Methods: Four Benzylpenicillin derivatives (compounds p1-p4) were chemically synthesized through the esterification of the carboxylic acid group with different groups of different polarity, and the antibacterial activities were examined by docking and bacteriological studies. Results: All the compounds showed different antibacterial results. The docking results showed that; the compound of the highest polarity (compound p1) has the best Binding energy. Also; The results of in vitro antibacterial activity showed that; compound p1 had the largest zones of inhibition and the highest antibacterial activity among all the other compounds. Conclusion: Masking the free carboxylic acid of benzylpenicillin with polar group will enhance the antibacterial activity.

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