Target intelligence / Profile preview

Activity against gram-negative bacteria

01

Overview

"Activity against Gram-negative bacteria" refers to the efficacy of an antibiotic or antimicrobial agent to inhibit or kill bacteria classified as Gram-negative on the basis of their cell envelope structure. Gram-negative bacteria possess an outer membrane with lipopolysaccharide, making them intrinsically more resistant to many antibiotics; successful drugs must penetrate this barrier and reach intracellular targets such as penicillin-binding proteins, ribosomes, or DNA gyrase. "Activity against gram-negative bacteria" therefore does not correspond to a unique molecular target but rather to the ability of an agent to circumvent or overcome multiple, distinct bacterial defense mechanisms

02

Mechanism of action

For drugs with activity against Gram-negative bacteria, mechanisms of action reflect their molecular targets: - Inhibition of cell wall synthesis (e.g., penicillins, cephalosporins, carbapenems, monobactams) - Disruption of bacterial outer membrane integrity (e.g., polymyxins/colistin) - Inhibition of protein synthesis (e.g., aminoglycosides, tetracyclines) - Inhibition of DNA gyrase/topoisomerase (e.g., quinolones) - Inhibition of folate biosynthesis (e.g., trimethoprim, sulfonamides)

03

Biological functions

Other
04

Disease associations

Infection
05

Safety considerations

Development and spread of antimicrobial resistanceToxicity associated with drugs (e.g., nephrotoxicity with aminoglycosides, neurotoxicity with polymyxins)Selection for resistant pathogens (e.g., ESBL, carbapenemase producers) leading to limited treatment options
06

Interacting drugs

Beta-lactams (e.g., ampicillin, amoxicillin, piperacillin, ceftriaxone, ceftazidime, carbapenems)

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