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Category: Bacterial Pathogenesis
Antibiotics and Antibacterial Agents: Classifications and Structure-Activity Relationship, Page 1 of 2
< Previous page | Next page > /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap02-1.gif /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap02-2.gifAbstract:
This chapter focuses on the classification and structural-activity relationship of antibiotics and antibacterial agents. The β-lactam family comprises four groups of molecules: penams, penems, cephems, and monocyclic β-lactams. To these should be added the β-lactamase inhibitors, some of the structures of which are featured in the four main groups. The azetidinone nucleus alone can be replaced, and monobactams, monocarbams, monophosphatams, and other heterocycles can be distinguished according to the substituents of the nitrogen atom. Based on studies by researchers, who demonstrated the transferability of resistance to certain antibiotics between Escherichia coli and Shigella spp., other researchers were able to demonstrate that shigellae inactivated chloramphenicol. The majority of aminoglycosides have similar basic structures and are divided into four groups: streptomycin derivatives, 2-deoxystreptamine derivatives, spectinomycin derivatives, and fortimicin derivatives. The macrolides are macrocyclic antibiotics characterized by a central lactone ring containing 12 to 16 members, few double bonds, and no nitrogen atom; one or two amino sugars and/or neutral sugars are attached to the lactone or aglycone ring. More than 400 compounds constitute the family of peptide antibiotics. Dihydrofolate reductase (DHFR) inhibitors used therapeutically are the result of studies relating to the specificity of this enzyme for bacterial, parasitic, or epithelial cells. The antibacterial compounds display good antibacterial activity and a lack of inhibitory activity against epithelial cell DHFR.
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Classification of the β-lactams
Chemical classification of cephalosporins
Microbiological classification of the cephems
Aminoglycosides
Classification of aminoglycosides (I)
Classification of aminoglycosides (II)
Classification of aminoglycosides (III)
Classification of aminoglycosides (IV)
Classification of aminoglycosides (V)
Streptomycin derivatives
Aminoglycoside A, B, and C nuclei
Kanamycins: structure
Gentamicins C: structure
Spectinomycin
Spectinomycin in an aqueous medium
Group of fortimicins
derivatives
Classification of the macrolides
Degradation of erythromycin A in an acidic medium
Weak points of erythronolide A
Degradation of clarithromycin in acidic medium
Erythromycin A: modifications of positions C-6, C-8, and C-11 plus C-12
Semisynthesis of 9-erythromycin A derivatives
Azalides
Classification of the 4-quinolones
Fluoroquinolones: Antibacterial activity
General structure of glycopeptide antibiotics
Ansamycins
Chemical structures of the cyclines
Other derivatives of the cyclines
Glycylcycline and dactylocycline derivatives
Lincosamide derivatives
Chloramphenicol
2,4-Diaminobenzylpyrimidine
Sulfonamide prodrugs
Sulfonamides
Oral β-lactams
Antibacterial activities of the kanamycins
Antibacterial activities of members of the gentamicin C complex
Antibacterial activities of the azithromycin derivatives
Side effects of fluoroquinolones
K p s of cyclines
Half-lives of the sulfonamides