The History, Present, and Future of β-lactam Antibiotics

Research Article
Open access

The History, Present, and Future of β-lactam Antibiotics

Zirui Zhang 1*
  • 1 Changhe Senior High School, Hangzhou, 310052, China    
  • *corresponding author 27350374@qq.com
Published on 20 June 2025 | https://doi.org/10.54254/2753-8818/2025.24208
TNS Vol.116
ISSN (Print): 2753-8826
ISSN (Online): 2753-8818
ISBN (Print): 978-1-80590-197-6
ISBN (Online): 978-1-80590-198-3

Abstract

β-Lactam antibiotics, discovered in the 1920s with the development of penicillin by Alexander Fleming, revolutionized the treatment of bacterial infections. These antibiotics are characterized by their β-lactam ring as their typical structure, leading to the development of various derivatives such as cephalosporins and carbapenems. To date, they remain one of the most widely used and effective antibiotics. β-Lactam antibiotics exert their antibacterial action by inhibiting the synthesis of the bacterial cell wall, specifically by targeting and binding to penicillin-binding proteins. Furthermore, this binding disrupts the cross-linking of peptidoglycan chains, leading to cell wall weakening and ultimately causing bacterial cell lysis and death. The development of resistance to β-lactam antibiotics primarily occurs through the production of β-lactamases, which hydrolyze the β-lactam ring. Obviously, resistance to β-lactam antibiotics can also develop through other mechanisms, but this is the most significant and most urgent to address. In the wide history of β-Lactam antibiotics, researchers paid much effort to overcome the resistance and the side effects. Researchers have also increased the stability of β-lactam rings through chemical modifications, such as adding side chains or introducing enzyme-resistant groups, to withstand the hydrolytic action of β-lactamases produced by bacteria. By modifying the structure of the R group, medicinal chemists can design more effective and targeted antibiotics to address various bacterial infections. This review systematically reviews the development of β-lactam antibiotics and the influence of different side chains on the functionality of β-lactam antibiotics, such as side effects, clinical applications, drug stability, etc. Finally, we propose the future development of β-lactam antibiotics.

Keywords:

β-lactam antibiotic, side effects, chemical modifications, resistance

Zhang,Z. (2025). The History, Present, and Future of β-lactam Antibiotics. Theoretical and Natural Science,116,37-51.
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References

[1]. Fleming, A. (1929). On the antibacterial action of cultures of a Penicillium, with special reference to their use in the isolation of B. influenzae. British Journal of Experimental Pathology, 10(3), 226-236

[2]. Elizalde-Velázquez, A., Gómez-Oliván, L. M., Galar-Martínez, M., Islas-Flores, H., Dublán-García, O., & SanJuan-Reyes, N. (2016). Amoxicillin in the Aquatic Environment, Its Fate and Environmental Risk. In InTech eBooks.

[3]. KAUR, S. P., RAO, R., & NANDA, S. (2011). AMOXICILLIN: A BROAD SPECTRUM ANTIBIOTIC. In International Journal of Pharmacy and Pharmaceutical Sciences (Vols. 3–3, pp. 30–37)

[4]. Faine S, Harper M. 1973. Independent Antibiotic Actions of Hetacillin and Ampicillin Revealed by Fast Methods. Antimicrob Agents Chemother 3:.

[5]. Holmes, B., Richards, D.M., Brogden, R.N. et al. Piperacillin. Drugs 28, 375–425 (1984)

[6]. Brogden, R.N., Heel, R.C., Speight, T.M. et al. Ticarcillin: A Review of its Pharmacological Properties and Therapeutic Efficacy. Drugs 20, 325–352 (1980).

[7]. Prince, A. (n.d.). CEPHALOSPORINS AND VANCOMYCIN.

[8]. The American Society of Health-System Pharmacists. [2016-12-08]

[9]. Gootz, T. (1990). Discovery and Development of New Antimicrobial Agents. In Clinical Microbiology Reviews (Vol. 3, pp. 13–31). American Society for Microbiology.

[10]. Supplement Approval for Mefoxin (Cefoxitin for Injection, USP). (2011). In Food and Drug Administration

[11]. Supplement Approval for Mefoxin (Cefoxitin for Injection, USP). (2011). In Food and Drug Administration

[12]. Carmine, A.A., Brogden, R.N., Heel, R.C. et al. Cefotaxime. Drugs 25, 223–289 (1983).

[13]. Joan C. Fung-Tome, Ph.D. Department of Microbiology Bristol-Myers Squibb Company Wallingford, CT 06492.

[14]. Yahav D, Paul M, Fraser A, Sarid N, Leibovici L (May 2007). "Efficacy and safety of cefepime: a systematic review and meta-analysis". The Lancet. Infectious Diseases. 7 (5): 338–348.doi:10.1016/S1473-3099(07)70109-3.

[15]. Endimiani, A., Perez, F., & Bonomo, R. A. (2008). Cefepime: a reappraisal in an era of increasing antimicrobial resistance. In Expert Rev Anti Infect Ther (Vols. 6–6, pp. 805–824).

[16]. Endimiani, A., Perez, F., & Bonomo, R. A. (2008). Cefepime: a reappraisal in an era of increasing antimicrobial resistance. In Expert Rev Anti Infect Ther (Vols. 6–6, pp. 805–824).

[17]. Ronald N. Jones, Review of the in-vitro spectrum and characteristics of cefmetazole (CS-1170), Journal of Antimicrobial Chemotherapy, Volume 23, Issue suppl_D, 1989, Pages 1–12.

[18]. Fukuda M, Nabeta M, Oya S, et al. Severe drug-induced immune hemolytic anemia due to cefmetazole: A case report[J]. International Journal of Clinical Pharmacology and Therapeutics, 2022, 60(1): 52.

[19]. HELLINGER, W. C., & BREWER, N. S. (1991, October). Imipenem. In Mayo Clinic Proceedings (Vol. 66, No. 10, pp. 1074-1081). Elsevier.

[20]. HELLINGER, W. C., & BREWER, N. S. (1991, October). Imipenem. In Mayo Clinic Proceedings (Vol. 66, No. 10, pp. 1074-1081). Elsevier.

[21]. Madsen PO, Nielsen KT, and Craversen PH: Aztreonam: a critical evaluation of the first monobactam antibiotic in the treatment of urinary tract infections. 1 Urol 140: 925 0988).

[22]. Stutman HR: Clinical experience with aztreonam, Pediatr Infect Dis J (Suppl 9) 8: S109 (1989).

[23]. Swabb EA, Sugerman AA, Stern M: Oral bioavailability of the monobactam aztreonam (SQ 26,776) in healthy subjects. Antimicrob Agents Chemother 2:3:.548-.5,50, 1983

[24]. Swabb EA: Review of the clinical pharmacology of the monobactam antibiotic aztreonam. Am J Med 78(Suppl 2A):11-11), 1911,5

Cite this article

Zhang,Z. (2025). The History, Present, and Future of β-lactam Antibiotics. Theoretical and Natural Science,116,37-51.

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Volume title: Proceedings of the 3rd International Conference on Modern Medicine and Global Health

ISBN：978-1-80590-197-6(Print) / 978-1-80590-198-3(Online)
Editor：Sheiladevi Sukumaran
Conference website: https://2025.icmmgh.org/
Conference date: 20 January 2025
Series: Theoretical and Natural Science
Volume number: Vol.116
ISSN：2753-8818(Print) / 2753-8826(Online)

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References

[1]. Fleming, A. (1929). On the antibacterial action of cultures of a Penicillium, with special reference to their use in the isolation of B. influenzae. British Journal of Experimental Pathology, 10(3), 226-236

[2]. Elizalde-Velázquez, A., Gómez-Oliván, L. M., Galar-Martínez, M., Islas-Flores, H., Dublán-García, O., & SanJuan-Reyes, N. (2016). Amoxicillin in the Aquatic Environment, Its Fate and Environmental Risk. In InTech eBooks.

[3]. KAUR, S. P., RAO, R., & NANDA, S. (2011). AMOXICILLIN: A BROAD SPECTRUM ANTIBIOTIC. In International Journal of Pharmacy and Pharmaceutical Sciences (Vols. 3–3, pp. 30–37)

[4]. Faine S, Harper M. 1973. Independent Antibiotic Actions of Hetacillin and Ampicillin Revealed by Fast Methods. Antimicrob Agents Chemother 3:.

[5]. Holmes, B., Richards, D.M., Brogden, R.N. et al. Piperacillin. Drugs 28, 375–425 (1984)

[6]. Brogden, R.N., Heel, R.C., Speight, T.M. et al. Ticarcillin: A Review of its Pharmacological Properties and Therapeutic Efficacy. Drugs 20, 325–352 (1980).

[7]. Prince, A. (n.d.). CEPHALOSPORINS AND VANCOMYCIN.

[8]. The American Society of Health-System Pharmacists. [2016-12-08]

[9]. Gootz, T. (1990). Discovery and Development of New Antimicrobial Agents. In Clinical Microbiology Reviews (Vol. 3, pp. 13–31). American Society for Microbiology.

[10]. Supplement Approval for Mefoxin (Cefoxitin for Injection, USP). (2011). In Food and Drug Administration

[11]. Supplement Approval for Mefoxin (Cefoxitin for Injection, USP). (2011). In Food and Drug Administration

[12]. Carmine, A.A., Brogden, R.N., Heel, R.C. et al. Cefotaxime. Drugs 25, 223–289 (1983).

[13]. Joan C. Fung-Tome, Ph.D. Department of Microbiology Bristol-Myers Squibb Company Wallingford, CT 06492.

[14]. Yahav D, Paul M, Fraser A, Sarid N, Leibovici L (May 2007). "Efficacy and safety of cefepime: a systematic review and meta-analysis". The Lancet. Infectious Diseases. 7 (5): 338–348.doi:10.1016/S1473-3099(07)70109-3.

[15]. Endimiani, A., Perez, F., & Bonomo, R. A. (2008). Cefepime: a reappraisal in an era of increasing antimicrobial resistance. In Expert Rev Anti Infect Ther (Vols. 6–6, pp. 805–824).

[16]. Endimiani, A., Perez, F., & Bonomo, R. A. (2008). Cefepime: a reappraisal in an era of increasing antimicrobial resistance. In Expert Rev Anti Infect Ther (Vols. 6–6, pp. 805–824).

[17]. Ronald N. Jones, Review of the in-vitro spectrum and characteristics of cefmetazole (CS-1170), Journal of Antimicrobial Chemotherapy, Volume 23, Issue suppl_D, 1989, Pages 1–12.

[18]. Fukuda M, Nabeta M, Oya S, et al. Severe drug-induced immune hemolytic anemia due to cefmetazole: A case report[J]. International Journal of Clinical Pharmacology and Therapeutics, 2022, 60(1): 52.

[19]. HELLINGER, W. C., & BREWER, N. S. (1991, October). Imipenem. In Mayo Clinic Proceedings (Vol. 66, No. 10, pp. 1074-1081). Elsevier.

[20]. HELLINGER, W. C., & BREWER, N. S. (1991, October). Imipenem. In Mayo Clinic Proceedings (Vol. 66, No. 10, pp. 1074-1081). Elsevier.

[21]. Madsen PO, Nielsen KT, and Craversen PH: Aztreonam: a critical evaluation of the first monobactam antibiotic in the treatment of urinary tract infections. 1 Urol 140: 925 0988).

[22]. Stutman HR: Clinical experience with aztreonam, Pediatr Infect Dis J (Suppl 9) 8: S109 (1989).

[23]. Swabb EA, Sugerman AA, Stern M: Oral bioavailability of the monobactam aztreonam (SQ 26,776) in healthy subjects. Antimicrob Agents Chemother 2:3:.548-.5,50, 1983

[24]. Swabb EA: Review of the clinical pharmacology of the monobactam antibiotic aztreonam. Am J Med 78(Suppl 2A):11-11), 1911,5

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