Utilization of microbial iron assimilation processes for the development of new antibiotics and inspiration for the design of new anticancer agents.

Pathogenic microbes rapidly develop resistance to antibiotics. To keep ahead in the "microbial war", extensive interdisciplinary research is needed. A primary cause of drug resistance is the overuse of antibiotics that can result in alteration of microbial permeability, alteration of drug target binding sites, induction of enzymes that destroy antibiotics (ie.

Total synthesis of desferrisalmycin B.

The first total synthesis of a naturally occurring siderophore antibiotic, desferrisalmycin B, is described, and the configuration of the unknown stereocenter is assigned. The synthesis features a synthetic strategy of constructing the novel amino-heptopyranoside component by stereoselective dihydroxylation followed by a Bose-modified Mitsunobu reaction. Through this convergent approach, other members of salmycins should also be synthetically accessible.

Total synthesis of the siderophore danoxamine.

The total synthesis of the linear trihydroxamate siderophore, Danoxamine, is described. Danoxamine is a siderophore component of the naturally occurring siderophore-drug conjugates Salmycin A-D. The synthesis of Danoxamine features a series of coupling reactions involving N-(5-benzyloxypentyl)-O-benzylhydroxylamine being linked by a succinoyl linker to N-(benzyloxy)-1,5-pentanediamine.

The effect of vehicle on corneal penetration of triturated ketoconazole and itraconazole.

Background And Objectives: Triturated (crushed and suspended) ketoconazole has been recommended for the treatment of fungal keratitis when commercial antifungal eyedrops are unobtainable. The authors evaluated the in vivo corneal stromal concentration with different vehicles in the eyes of adult rabbits.

Materials And Methods: Ketoconazole and itraconazole tablets were triturated to 20 mg/ml in four vehicles: polyvinyl alcohol (PVA), boric acid, olive oil, and balanced salt solution (BSS).