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An update on small molecule strategies targeting leishmaniasis

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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 157, 期 -, 页码 339-367

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.08.012

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Leishmaniasis; Resistance; Oxindole; Benzimidazole; Quinazoline

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Leishmaniasis is an infectious disease caused by various species of protozoan parasite known as Leishmania, which is transmitted to its mammalian host via bite of an infected sandfly. Clinically, Leishmaniasis appears as following four conditions: Cutaneous Leishmaniasis, Mucocutaneous Leishmaniasis, Visceral Leishmaniasis/Kala-azar, Post Kala azar dermal Leishmaniasis. Current therapies include pentavalent antimonials, Amphotericin B, Paromomycin, Miltefosine, Pentamidine, Sitamaquine. Presence of diverse survival pathways in the parasite to carry out various physiological functions has rendered targeting via drugs inefficient and troublesome. Moreover, emerging resistance mechanisms in the well-established key targets are affecting the use of current drug treatment options thus leading to treatment failure. Therefore, development of novel anti-leishmanial compounds with alternative and efficient mechanisms of actions is required to eradicate this disease. This review provides an overview of leishmaniasis along with the main emphasis on novel heterocycles reported for their anti-leishmanial activity in recent years. (C) 2018 Elsevier Masson SAS. All rights reserved.

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