Abstract
In this review, we present the potential use of the heterocyclic oxadiazole rings in the design and synthesis of new drugs to treat parasitic infections. We intend to compare herein all the four isomeric forms of oxadiazole rings as well as discuss the differences and similarities between them. In addition, we discuss aspects on their reactivity that justify the great importance of both 1,2,4- and 1,3,4-oxadiazoles isomers when compared with their other two isomers. Although some oxadiazole isomers satisfy Huckel's rule, there are differences concerning their aromaticity, which have a great impact on the possible interactions of the oxadiazole ring with biological receptors. The set of works selected from the literature and discussed herein points out the oxadiazole core as an important and versatile scaffold in the development of new chemical entities potentially useful as antiparasitic drugs.
Highlights
Nitrogen heterocycles play an important role in the drug discovery scenario.[1]
The nitrogenated cores commonly occur as fragments in the structure of most drugs with varied ring sizes; aromatic and nonaromatic rings; fused and bicyclic rings
Nitrogen heterocyclic drugs are present in all therapeutic areas including cardiovascular and metabolic illnesses, central nervous system (CNS) disorders, antiinflammatory, antineoplastic, anti-infective drugs, among others
Summary
Nitrogen heterocycles play an important role in the drug discovery scenario.[1] The nitrogenated cores commonly occur as fragments in the structure of most drugs with varied ring sizes; aromatic and nonaromatic rings; fused and bicyclic rings. Ketoconazole (5) is an important imidazolic antifungal that acts inhibiting the enzyme responsible for fungal ergosterol biosynthesis, 14α-demethylase.[4] Metronidazole (6) and benznidazole (7) are two antiprotozoal drugs acting through the generation of intracellular radical species which can damage both parasites’ DNA and other cellular machinery.[5] The antibacterial fluoroquinolone ciprofloxacin (8) acts through the damage of bacterial DNA.[6] Raltegravir (9) is an HIV-1 integrase inhibitor, useful for the treatment of HIV infections.[7]
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