Prodrugs ampicillin-derived

Latentiation of ampicillin can also be achieved by tying up the proximate amino and amide functions as an acetone aminal. Inclusion of acetone in the reaction mixture allows 6-APA to be condensed directly with the acid chloride from 24. There is thus obtained directly the prodrug hetacillin (34). Although this compound has little antibiotic activity in its own right, it hydrolyzes to ampicillin in the body. The p-hydroxy derivative amoxycillin (35) shows somewhat better oral activity. A similar sequence using formaldehyde gives metampicillin (36). °... 

Use antibacterial, semisynthetic p-lactam antibiotic, derivative of ampicillin (prodrug for ora application)... 

Sultamicillin (SS) Double terof ampicillin and sulbacEam Combination penicillin derivative and P lactamase inhibitor combined into a single prodrug Pfirer brand. Unasyn, claimed 1.6% of world marker in 1991 as fourteenth leading antibiotic. 

Lenampicillin [86273-18-9], antibacterial, semisynthetic -lactam antibiotic, derivative of ampicillin (prodrug for oral application), 145. The key reagent, the substituted vinyl-ene carbonate 144, is prepared by the phosgenation of acetoin 143 [103-111]. 

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