Journal article

Natural Product-Based Phenols as Novel Probes for Mycobacterial and Fungal Carbonic Anhydrases

Rohan A Davis, Andreas Hofmann, Asiah Osman, Rebecca A Hall, Fritz A Muehlschlegel, Daniela Vullo, Alessio Innocenti, Claudiu T Supuran, Sally-Ann Poulsen

Journal of Medicinal Chemistry | AMER CHEMICAL SOC | Published : 2011

Abstract

In order to discover novel probes that may help in the investigation and control of infectious diseases through a new mechanism of action, we have evaluated a library of phenol-based natural products (NPs) for enzyme inhibition against four recently characterized pathogen β-family carbonic anhydrases (CAs). These include CAs from Mycobacterium tuberculosis, Candida albicans, and Cryptococcus neoformans as well as α-family human CA I and CA II for comparison. Many of the NPs selectively inhibited the mycobacterial and fungal β-CAs, with the two best performing compounds displaying submicromolar inhibition with a preference for fungal over human CA inhibition of more than 2 orders of magnitude..

View full abstract

University of Melbourne Researchers