Two novel prodrugs of amoxicillin and cephalexin (amoxicillin ProD 1 and cephalexin ProD
1, respectively) were designed and synthesized to improve the stability and bitter sensation …

A number of marketed antibacterial drugs suffer several problems, such as bitter sensation
and low stability which lead to patient incompliance. The prodrug approach is considered …

Publisher Summary Studies have clarified the confusion between the terms prodrug and soft
drug. These terms represent opposite concepts: a prodrug is inactive by design and it is …

Seven new ester prodrugs of ampicillin with hydrolysis half-lives ranging from 65 to 308 min
were synthesized. The cellular accumulation of two of them (in J774 mouse macrophages) …

To improve the aqueous solubility of anti-methicillin-resistant Staphylococcus aureus
cephalosporin RWJ-333441 for parenteral administration, acyl derivatives of the C-3 primary …

In present work, secnidazole and ciprofloxacin were linked as mutual prodrugs to get
antibiotics with broader spectrum of activity by acting on aerobic and anaerobic bacteria …

Ceftizoxime (CZX), a parenteral cephalosporin, has potent and broad antibacterial activity.
To improve its oral absorption, we synthesized a series of monofunctional and bifunctional …

抄録 Enamine derivatives of ampicillin, amoxicillin and cephalexin were prepared by
reacting the drugs with ethyl acetoacetate under mild conditions. The enamine structures of …

A series of cephalosporins bearing a 5, 5-fused ring system, an (imidazo [5, 1-b] thiazolium-
6-yl) methyl group, at the C-3 position were synthesized and evaluated for in vitro …

The synthesis and biological activities of a series of non-classical penicillins are described.
These compounds were synthesized by treating the pivaloyloxymethyl ester of 6 …