Semisynthetic derivatives of purpuromycin as potential topical agents for vaginal infections
Articolo
Data di Pubblicazione:
1997
Citazione:
Semisynthetic derivatives of purpuromycin as potential topical agents
for vaginal infections / A. Trani, C. Dallanoce, G. Panzone, F. Ripamonti, B.P. Goldstein, R. Ciabatti. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 40:6(1997), pp. 967-971. [10.1021/jm960672t]
Abstract:
Purpuromycin (1) is an antibiotic with a broad spectrum of antimicrobial
activity, encompassing bacteria, fungi, and protozoa, particularly those
involved in vaginal infections. With the aim of enhancing the solubility
and reducing the serum binding, a chemical program of modifications was
undertaken on the natural compound, and a new interesting series of
derivatives at the naphthoquinone system was synthesized and evaluated
as potential topical agents for vaginal infections. In particular three
semisynthetic derivatives, 7'-amino (8a), 7'-methylamino (8b),
7'-ethylamino (8c), of 7'-demethoxypurpuromycin seemed to be the most
promising. They were tested for in vitro activity against three of the
most important vaginal pathogens and showed activity similar to that of
purpuromycin against Candida isolates while they were significantly more
active against Trichomonas vaginalis and Gardnerella vaginalis, which
are cultured in media containing blood or serum. This is probably due to
the fact that the activity of the derivatives is less antagonized by
these supplements than that of purpuromycin.
Tipologia IRIS:
01 - Articolo su periodico
Elenco autori:
A. Trani, C. Dallanoce, G. Panzone, F. Ripamonti, B.P. Goldstein, R. Ciabatti
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