Journal of Medicinal Chemistry p. 1110 - 1116 (1991)
Update date:2022-07-30
Topics: Synthesis Structure-Activity Relationship pKa Dependence Cephalosporins Amino heterocycles Antibacterial spectrum β-lactamase
Jung
Delvare
Boucherot
Hamon
Ackerley
Betts
Cephalosporins with new aminobenzimidazole and aminoimidazoline heterocycles at C-7 have been synthesized starting with versatile C-7 isocyanide dihalide synthons. The aminobenzimidazoles have a broad spectrum of antibacterial activity, including Gram-positive and Gram-negative organisms, but possess limited β-lactamase stability. In contrast, the aminoimidazolines have a narrow spectrum of antibacterial activity, limited to Gram-negative strains only, but possess outstanding β-lactamase stability. Structure-activity relationships are discussed in terms of their dependence on the pK(a) of the C-7 amino heterocycle, basic C-7 residues giving cephalosporins with exceptional β-lactamase stability.
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