Roberto Di Santo
University of Rome “La Sapienza”, Italy
Keynote: Med Chem
Neglected tropical diseases (NTDs) represent a major health problem and huge
economic burden in developing countries. Among them, trypanosomatid
diseases, including leishmaniases, Chagas disease and African sleeping sickness, are
categorized by WHO as the most challenging NTDs affecting more than 20 million
people worldwide. Additionally, they are expanding their frontiers worldwide and
becoming relevant global health concerns. New treatment options against these
diseases are lacking due to the poor interest of big Pharma towards such neglected
therapeutic area, and the current chemoteraphy is based on few old drugs endowed
with limited efficacy and high toxicity. Thus, the search for new effective agents able to
overcome these limits is always a hot topic.
Drug repurposing represents one of the most prominent and successful strategies to
furnish new compounds and tools for the treatment of diseases for which no or very
few drugs are available. We applied this approach to find agents able to defeat NTDs.
According to this, our inhouse series of azole antifungal drugs designed several years
ago, which showed good activity both in vitro against C. albicans and spp, and in vivo
in rabbit model of cutaneous fungal infection were screened against clinically relevant
parasites. A number of them displayed nanomolar activities against T. cruzi, resulting
much more active than the reference drug and showing high selectivity towards
parasite. Interestingly, the most active derivative displayed efficacy in in vivo model
of infection. Starting from these data, we designed and synthesized a new series of
azole compounds endowed with nanomolar potencies against T. cruzi and capable to
effectively reduce parasitemia higher than 99% in 4-day in vivo models.
Key words: neglected tropical diseases, trypanosomatid diseases, azole
Roberto Di Santo is Full Professor in Medicinal Chemistry at University of Rome “La Sapienza”. He is engaged in drug design and Discovery of new chemotherapeutic agents. His current focus is on the Discovery of antimicrobial agents with attention to new chemical entities useful to defeat microbial neglected diseases. He is the director of Drug Design and Discovery Laboratory in Chemistry and Technology of Drugs Department of Rome University “La Sapienza”. He has published more than 130 papers on high impact peer reviewed journals and has been serving as an editorial board member of repute.
E-mail: roberto.disanto@uniroma1.it
Medicinal Chemistry received 6627 citations as per Google Scholar report
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