Antibiotics and Bacterial Resistance—A Short Story of an Endless Arms Race

Abstract

Despite the undisputed development of medicine, antibiotics still serve as first-choice drugs for patients with infectious disorders. The widespread use of antibiotics results from a wide spectrum of their actions encompassing mechanisms responsible for: the inhibition of bacterial cell wall biosynthesis, the disruption of cell membrane integrity, the suppression of nucleic acids and/or proteins synthesis, as well as disturbances of metabolic processes. However, the widespread availability of antibiotics, accompanied by their overprescription, acts as a double-edged sword, since the overuse and/or misuse of antibiotics leads to a growing number of multidrug-resistant microbes. This, in turn, has recently emerged as a global public health challenge facing both clinicians and their patients. In addition to intrinsic resistance, bacteria can acquire resistance to particular antimicrobial agents through the transfer of genetic material conferring resistance. Amongst the most common bacterial resistance strategies are: drug target site changes, increased cell wall permeability to antibiotics, antibiotic inactivation, and efflux pumps. A better understanding of the interplay between the mechanisms of antibiotic actions and bacterial defense strategies against particular antimicrobial agents is crucial for developing new drugs or drug combinations. Herein, we provide a brief overview of the current nanomedicine-based strategies that aim to improve the efficacy of antibiotics.

Potentiating‐antibiotic activity and absorption, distribution, metabolism, excretion and toxicity properties (ADMET) analysis of synthetic thiadiazines against multi‐drug resistant (MDR) strains

“…The chemical methodology for the synthesis of thiadiazine derivatives is illustrated in Figure 1. N-substituted thiosemicarbazides [1][2][3][4] were initially obtained by reacting hydrazine with isothiocyanates, and the spectroscopic data were identical to those reported in the literature [23][24][25][26]. Then, the final compounds were prepared in one step by reactions 1-4 with substituted phenylacetyl bromides in methanol or acetonitrile [27].…”

“…The introduction of the clinical use of antibiotics in the 20th century revolutionized modern medicine, reducing the morbidity and mortality of individuals with bacterial infections [1]. On the other hand, there is currently an increase in the number of bacterial species resistant to antibiotics, which is considered a global public health problem [2].…”

Spectroscopic characterization, molecular docking and machine learning studies of sulphur containing hydrazide derivatives

“…7. The energy values for the HOMO (24) and LUMO (25) 1 and 2 clearly indicate p-p* transitions. The high energy difference in the HOMO-LUMO gap of TSCZ and the HOMO-LUMO gap of TCHZ suggests the higher kinetic energies and chemical reactivities of these molecules.…”

“…This in turn has recently become a global public health issue that affects patients and clinicians as bacteria can acquire resistance to specific antimicrobial agents through the transfer of genetic material that confers resistance in addition to intrinsic resistance. 25…”

“…This in turn has recently become a global public health issue that affects patients and clinicians as bacteria can acquire resistance to specific antimicrobial agents through the transfer of genetic material that confers resistance in addition to intrinsic resistance. 25 The search for new drug candidates with specific chemical, microbiological and pharmacological characteristics has become increasingly urgent. There is a need for new antibacterial drugs which will increase the treatment success rate for both drug susceptible and drug resistant bacterial strains.…”