Howard Newman

α-Nitro-epoxides, a new class of compounds

The first examples of α-nitro-epoxides have been prepared; some chemical properties are reported.

A short, simple synthetic route to 3-dehydrosphinganine and related compounds

A brief, versatile synthesis of 3-dehydrosphinganine (1) and derivatives is described which features, as its key step, the reaction of diazoketones and trialkylboranes. Compatibility with chiral reagents is indicated.

Chapter 14. Antifungal Agents

Publisher Summary This chapter describes the development of antifungal agents. Amphotericin B has been found useful in treatment of the diseases such as rhinocerebral phycomycosis, rhino-orbital mucormy lastomycosis, and mycotic endocarditis due to Cryptococcus neoformans . The degree of susceptibility of a variety of C. neoformans strains to amphotericin B was shown by an in vitro study in which 65 human and 25 environmental isolates of C.n. were treated with various concentrations of the antibiotic. A mode of action study of azalomycin F on Candida albican indicates that at its minimum growth inhibitory concentration, the antibiotic strongly inhibited amino acid incorporation into cellular protein and generally prevented the substrate respiration of amino acids. In an effort to obtain an increased concentration of griseofulvin in the blood the 4′-oxime and 4′-alcohol derivatives were prepared and then tested in rabbits. Oral dosing gave plasma levels of griseofulvin as high as or higher than when the antibiotic itself was used but the high levels were of short duration. A critical review and evaluation of the laboratory investigations and clinical uses of the antifungal drug tolnaftate (IV) have also been presented in the chapter.