AntiBacterial

Agent

Mechanisms of antibacterial
action
▪ Inhibition of cell metabolism

▪ Inhibition of bacterial cell wall synthesis

▪ Interactions with the plasma membrane

▪ Disruption of protein synthesis

▪ Inhibition of nucleic acid transcription and replication

Antibacterial agents against cell metabolism .

amides). R 1 = H).e. Th e only exception is when R 1 = acyl (i. ▪ the sulphonamide nitrogen must be primary or secondary. ▪ the aromatic ring must be para -substituted only. Th us.Sulphonamides ▪ SAR ▪ the para -amino group is essential for activity and must be unsubstituted (i.e.5 ). 19. ▪ R2 is the only possible site that can be varied in sulphonamides. Th e amides themselves are inactive but can be metabolized in the body to regenerate the active compound ( Fig. . amides can be used as sulphonamide prodrugs ▪ the aromatic ring and the sulphonamide functional group are both required. Extra substitution eliminates activity for steric reasons. ▪ both the sulphonamide and amino group must be directly attached to the aromatic ring.

.

because it is an enzyme cofactor that provides one carbon units for the synthesis of the pyrimidine nucleic acid bases required for DNA synthesis .Mechanism of action ▪ The sulphonamides act as competitive enzyme inhibitors of dihydropteroate synthetase and block the biosynthesis of tetrahydrofolate in bacterial cells ▪ Tetrahydrofolate is important in both human and bacterial cells.

.

Antibacterial agents inhibit cell wall synthesis .

.

acetylglucosamine (NAG) ▪ Enzyme Transpetidase .acetylmuramic acid (NAM) ▪ N .▪ N .

.

.

SAR Penicillins .

▪ sulphur is usual but not essential ▪ the stereochemistry of the bicyclic ring with respect to the acylamino side chain is important. ▪ the free carboxylic acid is essential. ▪ the bicyclic system is important.▪ the strained β-lactam ring is essential. ▪ the acylamino side chain is essential. .

.

.

.

.

. ▪ variations of the 3-acetoxymethyl side chain.▪ variations of the 7-acylamino side chain. ▪ extra substitution at carbon 7.

.

Act on DNA Replication .

. then binds aminoacyl transfer RNA (tRNA) and catalyses the building of the protein chain. ▪ The 50S subunit combines with the 30S subunit-mRNA complex to form a ribosome. consisting of 60S and 40S subunits.▪ The bacterial ribosome is a 70S particle made up of a 30S subunit and a 50S subunit. ▪ The ribosomes of eukaryotic cells are bigger (80S). ▪ The 30S subunit binds messenger RNA (mRNA) and initiates protein synthesis.

Impair Protein Synthesis .

translation cannot even start ▪ Linezolid . ▪ As a result.Oxazolidinones ▪ Before protein synthesis can start. a 70S ribosome has to be formed by the combination of a 30S ribosome with a 50S ribosome. ▪ The oxazolidinones bind to the 50S ribosome and prevent this from happening.

Tugas : Hubungan Struktur Aktivitas ▪ Antiinfeksi local ▪ alcohol. ammonium kuartener ▪ Anthelmintik ▪ turunan vinilpiperidin ▪ Turunan benzimidazol & turunan kuinolin ▪ Analgetik ▪ Turunan morfin ▪ Turunan asam salisilat ▪ Turunan 5-pirazolidindion ▪ Turunan asam n-arilantranilat ▪ Turunan asam arilasetat .halogen ▪ fenol.

Tugas : Hubungan Struktur Aktivitas ▪ Diuretik ▪ Diuretik penghambat karbonik anhydrase ▪ Turunan tiazida ▪ Turunan asam fenoksiasetat ▪ Turunan sulfamoil benzoate ▪ Sedatif ▪ Turunan barbiturate ▪ Turunan benzodiazepine ▪ Antipsikotik ▪ Turunan fenotiazin ▪ Turunan florobutirofenon .

▪ Halusinogen ▪ Turunan feniletilamin ▪ Turunan asam lisergat ▪ Antituberkulosa ▪ Turunan hidrazida ▪ Turunan amida heterosiklik ▪ Antimalaria (turunan kuinolinometanol) .