| Literature DB >> 29701144 |
Stephen Patterson1, Alan H Fairlamb1.
Abstract
Interest in nitroheterocyclic drugs for the treatment of infectious diseases has undergone a resurgence in recent years. Here we review the current status of monocyclic and bicyclic nitroheterocyclic compounds as existing or potential new treatments for visceral leishmaniasis, Chagas' disease and human African trypanosomiasis. Both monocyclic (nifurtimox, benznidazole and fexinidazole) and bicyclic (pretomanid (PA-824) and delamanid (OPC-67683)) nitro-compounds are prodrugs, requiring enzymatic activation to exert their parasite toxicity. Current understanding of the nitroreductases involved in activation and possible mechanisms by which parasites develop resistance is discussed along with a description of the pharmacokinetic / pharmacodynamic behaviour and chemical structure-activity relationships of drugs and experimental compounds. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.Entities:
Keywords: Chagas' disease; Human African trypanosomiasis; benznidazole; delamanid; fexinidazole; nifurtimox; nitro-drugs; pretomanid; visceral leishmaniasis.
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Year: 2019 PMID: 29701144 DOI: 10.2174/0929867325666180426164352
Source DB: PubMed Journal: Curr Med Chem ISSN: 0929-8673 Impact factor: 4.530