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Open AccessArticle

Novel Synthetic Approaches for Bisnaphthalimidopropyl (BNIP) Derivatives as Potential Anti-Parasitic Agents for the Treatment of Leishmaniasis

1
Regenerative and Restorative Medicine Research Center (REMER), Istanbul Medipol University, 34810 Istanbul, Turkey
2
Department of Biomedical Engineering, School of Engineering and Natural Sciences, Istanbul Medipol University, 34810 Istanbul, Turkey
3
Pharmacy Services, Vocational School of Health Services, Istanbul Medipol University, 34810 Istanbul, Turkey
4
Department of Medical Pharmacology, International School of Medicine, Istanbul Medipol University, 34810 Istanbul, Turkey
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(24), 4607; https://doi.org/10.3390/molecules24244607
Received: 19 October 2019 / Revised: 10 December 2019 / Accepted: 11 December 2019 / Published: 16 December 2019
(This article belongs to the Special Issue Application of Organic Synthesis to Bioactive Compounds)
Leishmaniasis is a neglected parasitic disease that is widely seen in more than 60 countries worldwide, including Turkey and its subcontinental region. There are several chemotherapy agents for the treatment of leishmaniasis, including pentavalent antimonials—i.e., sodium stibogluconate (Pentostan) and meglumine antimoniate (Glucantim), pentamidine, conventional amphotericin B deoxycholate, miltefosine, paramomycin (aminosidine), and liposomal amphotericin B. However, these therapies are usually unsatisfactory due to dose-limiting toxicity issues and limited efficacy. Furthermore, resistance gained by parasites endangers future success of these therapies. Addressing these issues, the development of novel drugs with high efficacy has a vital importance. Latest studies have shown that bisnaphthalimidopropyl (BNIP) derivatives display high activity against Leishmaniasis parasites by selectively targeting parasitic sirtuin proteins and interacting with DNA. Despite the promising anti-parasitic activity, the low solubility and toxicity on human macrophages are the limitations to overcome. This study describes the new synthesis strategies for existing—i.e., BNIPDaoct and BNIPDanon—and novel BNIP derivatives differing in respect of their alkyl linker chain lengths. The new synthesis approach provides certain advantages compared to its existing alternatives reported in the literature. The proposed methodology does not only decrease the number of synthesis steps and production time of BNIPDaoct and BNIPDanon, but also provides higher yields, thereby making the synthesis highly cost-effective. View Full-Text
Keywords: drug discovery for neglected rare diseases; bisnaphthalimidopropyl (BNIP) derivatives; Leishmaniasis; BNIPDaoct; BNIPDanon; novel anti-parasitic agents drug discovery for neglected rare diseases; bisnaphthalimidopropyl (BNIP) derivatives; Leishmaniasis; BNIPDaoct; BNIPDanon; novel anti-parasitic agents
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MDPI and ACS Style

Keskin, E.; Ucisik, M.H.; Sucu, B.O.; Guzel, M. Novel Synthetic Approaches for Bisnaphthalimidopropyl (BNIP) Derivatives as Potential Anti-Parasitic Agents for the Treatment of Leishmaniasis. Molecules 2019, 24, 4607.

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