Modern Medicine Has Been The Development Of Antibiotics1
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One of the significant advances in modern medicine has been the development of antibiotics1. Innumerable lives have been saved by the use of antibiotics, which still remain the backbone of therapy for bacterial infections. The first β-lactam, penicillin G (benzylpenicillin [fig 1, compound 1]), was discovered by Fleming in 1928, and introduced as a clinical antibacterial agent in the early 1950s. Penicillin was of great clinical significance and its success incited the exploration for and the development of further derivatives. This pursuit augmented the clinical use of β-lactam antibiotics in the present age (penicillins, narrow- and extended-spectrum cephalosporins, monobactams, and carbapenems [fig 1, compounds 1 to 7])2. All these…show more content… Bacteria are constantly developing antibiotic-resistance mechanisms to enhance their growth and survival. Therefore, there is an ever-present need for new and effective antimicrobial drugs (derivatives). In view of this emerging antimicrobial resistance, two major strategies have been advanced to sustain the efficacy of β-lactam antibiotics: (i) discover or design β-lactam antibiotics that are able to evade bacterial enzymatic inactivation conferred by β-lactamases, or (ii) inhibit β-lactamases so the partner, β-lactam can reach the penicillin binding proteins (PBPs), the target of β-lactam antibiotics7. Despite the resistance posed by β-lactamases in conjunction with DD-peptidases, PBPs still remain attractive targets for antibiotic compounds.
Mechanism of action of β-lactam Antibiotics β-lactam antibiotics are vital weapons for the treatment of bacterial infections. They demonstrate their bactericidal effects by inhibiting enzymes involved in cell wall synthesis. The bacterial cell wall is an integral component that maintains the cell shape of the bacteria in a hypertonic and hostile environment8. The rigid cell wall (peptidoglycan) provides the tensile strength needed to withstand high osmotic pressures that would otherwise cause the plasma membrane to rupture9. The peptidoglycan is made of alternating N-acetylmuramic acid (NAM) and