The long and winding road to convert an antimicrobial compound in an antimicrobial drug. An overview from a medicinal chemistry point of view.

ENRIZ R D; F SUVIRE; S. A. ANDUJAR, ; M. ALVAREZ; M VETTORAZZI; J. DOLAB; S. ROJAS

CURRENT ORGANIC CHEMISTRY

BENTHAM SCIENCE PUBL LTD

Lugar: Oak Park; Año: 2016

1385-2728

Fungi have emerged over the past decades as major causes of human infections, especially among immunocompromised hosts. Although it appears that we have a big armamentarium of antifungal drugs in clinical use, in fact only a modest number of drugs are available. Unfortunately all antifungal drugs available for the treatment of fungal infections are not fully effective and possess a certain degree of toxicity or some drawbacks in pharmacokinetic aspects such as do not possess an adequate solubility. As complement, fungi have developed a rapid resistance against them because of their large-scale use. Considering such situation, it is clear an urgent need to develop new and more effective antifungal drugs. For such reason in recent years there has been an incredible increase in the number of studies looking for new compounds with antifungal effects; in particular new structures obtained from natural products. While there have been reported a large number of compounds with antifungal activities (some of them with novel structures), very few have managed to be used therapeutically. In this review article, we have identified and discussed the main reasons for the poor results that have been obtained so far in order to find new antifungal drugs. Also we discussed here new strategies which could be the wayto improve the search for new antifungal agents for therapeutic use, remarking its scope and limitations.