Publications by authors named "O Khoumeri"

The enterovirus is a genus of single-stranded, highly diverse positive-sense RNA viruses, including Human Enterovirus A-D and Human Rhinovirus A-C species. They are responsible for numerous diseases and some infections can progress to life-threatening complications, particularly in children or immunocompromised patients. To date, there is no treatment against enteroviruses on the market, except for polioviruses (vaccine) and EV-A71 (vaccine in China).

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Article Synopsis
  • A series of 61 thiazolidine-2,4-dione compounds with a styryl group was synthesized, analyzed for structure, and tested for their effectiveness against the kinetoplastid parasite and HepG2 cells.
  • Some compounds, particularly those with a nitro group, showed promising antileishmanial activity, with one compound demonstrating a low EC of 7 µM and low toxicity in human cell lines.
  • Mechanistically, this effective compound is identified as a prodrug activated by nitroreductase 1, producing cytotoxic metabolites that damage the parasite, while maintaining favorable lipophilicity and water solubility.
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Cancer is a complex and heterogeneous disease and is still one of the leading causes of morbidity and mortality worldwide, mostly as the population ages. Despite the encouraging advances made over the years in chemotherapy, the development of new compounds for cancer treatments is an urgent priority. In recent years, the design and chemical synthesis of several innovative hybrid molecules, which bring different pharmacophores on the same scaffold, have attracted the interest of many researchers.

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The quinoxaline core is a promising scaffold in medicinal chemistry. Multiple quinoxaline derivatives, such as the topoisomerase IIβ inhibitor XK-469 and the tissue transglutaminase 2 inhibitor GK-13, have been evaluated for their antiproliferative activity. Previous work reported that quinoxaline derivatives bearing an oxirane ring present antiproliferative properties against neuroblastoma cell lines SK-N-SH and IMR-32.

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. The past decades have seen numerous efforts to develop new antitubercular agents. Currently, the available regimens are lengthy, only partially effective, and associated with high rates of adverse events.

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