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Keywords = di-substituted urea-derivatives

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9 pages, 1057 KiB  
Brief Report
Activity of the Di-Substituted Urea-Derived Compound I-17 in Leishmania In Vitro Infections
by José Vitorino dos Santos, Jorge Mansur Medina, Karina Luiza Dias Teixeira, Daniel Marcos Julio Agostinho, Michael Chorev, Aurora Diotallevi, Luca Galluzzi, Bertal Huseyin Aktas and Ulisses Gazos Lopes
Pathogens 2024, 13(2), 104; https://doi.org/10.3390/pathogens13020104 - 24 Jan 2024
Cited by 1 | Viewed by 1555
Abstract
Protein synthesis has been a very rich target for developing drugs to control prokaryotic and eukaryotic pathogens. Despite the development of new drug formulations, treating human cutaneous and visceral Leishmaniasis still needs significant improvements due to the considerable side effects and low adherence [...] Read more.
Protein synthesis has been a very rich target for developing drugs to control prokaryotic and eukaryotic pathogens. Despite the development of new drug formulations, treating human cutaneous and visceral Leishmaniasis still needs significant improvements due to the considerable side effects and low adherence associated with the current treatment regimen. In this work, we show that the di-substituted urea-derived compounds I-17 and 3m are effective in inhibiting the promastigote growth of different Leishmania species and reducing the macrophage intracellular load of amastigotes of the Leishmania (L.) amazonensis and L. major species, in addition to exhibiting low macrophage cytotoxicity. We also show a potential immunomodulatory effect of I-17 and 3m in infected macrophages, which exhibited increased expression of inducible Nitric Oxide Synthase (NOS2) and production of Nitric Oxide (NO). Our data indicate that I-17, 3m, and their analogs may be helpful in developing new drugs for treating leishmaniasis. Full article
(This article belongs to the Special Issue Host-Pathogen Interactions during Leishmania Infections—a Special Issue in Honor of Prof. Dr. John David)
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16 pages, 1766 KiB  
Article
Amination of 5-Spiro-Substituted 3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones
by Ekaterina E. Khramtsova, Ekaterina A. Lystsova, Evgeniya V. Khokhlova, Maksim V. Dmitriev and Andrey N. Maslivets
Molecules 2021, 26(23), 7179; https://doi.org/10.3390/molecules26237179 - 26 Nov 2021
Cited by 4 | Viewed by 2421
Abstract
The 3-hydroxy-1,5-dihydro-2H-pyrrol-2-one motif is a valuable scaffold in drug discovery. The replacement of the 3-oxy fragment in 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones-based compounds with a 3-amino one (3-amino analogs of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones, 3-amino-1,5-dihydro-2H-pyrrol-2-ones) can play a crucial role in their [...] Read more.
The 3-hydroxy-1,5-dihydro-2H-pyrrol-2-one motif is a valuable scaffold in drug discovery. The replacement of the 3-oxy fragment in 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones-based compounds with a 3-amino one (3-amino analogs of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones, 3-amino-1,5-dihydro-2H-pyrrol-2-ones) can play a crucial role in their biological effect. Thus, approaches to 3-amino-1,5-dihydro-2H-pyrrol-2-ones are of significant interest. We developed an approach to 5-spiro-substituted 3-amino-1,5-dihydro-2H-pyrrol-2-ones that could not be obtained using previously reported approaches (reactions of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones with amines). The developed approach is based on the thermal decomposition of 1,3-disubstituted urea derivatives of 5-spiro-substituted 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones, which were prepared via their reaction with carbodiimides. Full article
(This article belongs to the Special Issue Modern Trends in Heterocyclic Chemistry)
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9 pages, 192 KiB  
Article
Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
by Nicolas Delattin, Dorothée Bardiot, Arnaud Marchand, Patrick Chaltin, Katrijn De Brucker, Bruno P. A. Cammue and Karin Thevissen
Molecules 2012, 17(10), 12243-12251; https://doi.org/10.3390/molecules171012243 - 18 Oct 2012
Cited by 10 | Viewed by 7067
Abstract
We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values C. albicans, in particular compounds 1, 5 and 6 characterized by MFC values [...] Read more.
We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values < 15 µM. The 6-amide derivatives displayed the highest fungicidal activity against C. albicans, in particular compounds 1, 5 and 6 characterized by MFC values of 6.25–12.5 µM. Compounds 1 and 5 of this series displayed fungicidal activity against the emerging pathogen Candida glabrata (MFC < 50 µM). The 6-amide derivatives 1, 2, 5, and 6 and the 6-urea derivatives 10, 12, 13 and 15 could also eradicate C. albicans biofilms. We found that the 6-urea derivatives 10, 13, and 15 induced accumulation of endogenous reactive oxygen species in Candida albicans biofilms. Full article
(This article belongs to the Special Issue Advances in Medicinal Chemistry of Antibiotics)
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