@article{Erasmus2021,
abstract = {A principal factor that contributes towards the failure to eradicate leishmaniasis and tuberculosis infections is the reduced efficacy of existing chemotherapies, owing to a continuous increase in multidrug-resistant strains of the causative pathogens. This accentuates the dire need to develop new and effective drugs against both plights. A series of naphthoquinone-triazole hybrids was synthesized and evaluated in vitro against Leishmania (L.) and Mycobacterium tuberculosis (Mtb) strains. Their cytotoxicities were also evaluated, using the human embryonic kidney cell line (HEK-293). The hybrids were found to be non-toxic towards human cells and had demonstrated micromolar cellular antileishmanial and antimycobacterial potencies. Hybrid 13, i.e. 2-{\{}[1-(4-methylbenzyl)-1H-1,2,3-triazol-4-yl]methoxy{\}}naphthalene-1,4-dione was the most active of all. It was found with MIC90 0.5 µM potency against Mtb in a protein free medium, and with half-maxima inhibitory concentrations (IC50) of 0.81 µM and 1.48 µM against the infective promastigote parasites of L. donavani and L. major, respectively, with good selectivity towards these pathogens (SI 22 - 65). Comparatively, the clinical naphthoquinone, atovaquone, although less cytotoxic, was found to be two-fold less antimycobacterial potent, and six- to twelve-fold less active against leishmania. Hybrid 13 may therefore stand as a potential anti-infective hit for further development in the search for new antitubercular and antileishmanial drugs. Elucidation of its exact mechanism of action and molecular targets will constitute future endeavour.},
author = {Erasmus, Chan{\'{e}} and Aucamp, Janine and Smit, Frans J and Seldon, Ronnett and Jordaan, Audrey and Warner, Digby F and N'Da, David D},
doi = {10.1016/J.BIOORG.2021.105118},
file = {:C$\backslash$:/Users/01462563/AppData/Local/Mendeley Ltd./Mendeley Desktop/Downloaded/Erasmus et al. - 2021 - Synthesis and comparison of iin vitroi dual anti-infective activities of novel naphthoquinone hybrids and atovaq.pdf:pdf},
issn = {0045-2068},
journal = {Bioorganic Chemistry},
keywords = {fund{\_}not{\_}ack,original},
mendeley-tags = {fund{\_}not{\_}ack,original},
month = {sep},
pages = {105118},
publisher = {Academic Press},
title = {{Synthesis and comparison of \textit{in vitro} dual anti-infective activities of novel naphthoquinone hybrids and atovaquone}},
volume = {114},
year = {2021}
}

{"_id":"MB3KGt6M5T2S8ABGz","bibbaseid":"erasmus-aucamp-smit-seldon-jordaan-warner-nda-synthesisandcomparisonofiinvitroidualantiinfectiveactivitiesofnovelnaphthoquinonehybridsandatovaquone-2021","author_short":["Erasmus, C.","Aucamp, J.","Smit, F. J","Seldon, R.","Jordaan, A.","Warner, D. F","N'Da, D. D"],"bibdata":{"bibtype":"article","type":"article","abstract":"A principal factor that contributes towards the failure to eradicate leishmaniasis and tuberculosis infections is the reduced efficacy of existing chemotherapies, owing to a continuous increase in multidrug-resistant strains of the causative pathogens. This accentuates the dire need to develop new and effective drugs against both plights. A series of naphthoquinone-triazole hybrids was synthesized and evaluated in vitro against Leishmania (L.) and Mycobacterium tuberculosis (Mtb) strains. Their cytotoxicities were also evaluated, using the human embryonic kidney cell line (HEK-293). The hybrids were found to be non-toxic towards human cells and had demonstrated micromolar cellular antileishmanial and antimycobacterial potencies. Hybrid 13, i.e. 2-\\[1-(4-methylbenzyl)-1H-1,2,3-triazol-4-yl]methoxy\\naphthalene-1,4-dione was the most active of all. It was found with MIC90 0.5 µM potency against Mtb in a protein free medium, and with half-maxima inhibitory concentrations (IC50) of 0.81 µM and 1.48 µM against the infective promastigote parasites of L. donavani and L. major, respectively, with good selectivity towards these pathogens (SI 22 - 65). Comparatively, the clinical naphthoquinone, atovaquone, although less cytotoxic, was found to be two-fold less antimycobacterial potent, and six- to twelve-fold less active against leishmania. Hybrid 13 may therefore stand as a potential anti-infective hit for further development in the search for new antitubercular and antileishmanial drugs. Elucidation of its exact mechanism of action and molecular targets will constitute future endeavour.","author":[{"propositions":[],"lastnames":["Erasmus"],"firstnames":["Chané"],"suffixes":[]},{"propositions":[],"lastnames":["Aucamp"],"firstnames":["Janine"],"suffixes":[]},{"propositions":[],"lastnames":["Smit"],"firstnames":["Frans","J"],"suffixes":[]},{"propositions":[],"lastnames":["Seldon"],"firstnames":["Ronnett"],"suffixes":[]},{"propositions":[],"lastnames":["Jordaan"],"firstnames":["Audrey"],"suffixes":[]},{"propositions":[],"lastnames":["Warner"],"firstnames":["Digby","F"],"suffixes":[]},{"propositions":[],"lastnames":["N'Da"],"firstnames":["David","D"],"suffixes":[]}],"doi":"10.1016/J.BIOORG.2021.105118","file":":C$\\$:/Users/01462563/AppData/Local/Mendeley Ltd./Mendeley Desktop/Downloaded/Erasmus et al. - 2021 - Synthesis and comparison of iin vitroi dual anti-infective activities of novel naphthoquinone hybrids and atovaq.pdf:pdf","issn":"0045-2068","journal":"Bioorganic Chemistry","keywords":"fund_not_ack,original","mendeley-tags":"fund_not_ack,original","month":"sep","pages":"105118","publisher":"Academic Press","title":"Synthesis and comparison of <i>in vitro</i> dual anti-infective activities of novel naphthoquinone hybrids and atovaquone","volume":"114","year":"2021","bibtex":"@article{Erasmus2021,\r\nabstract = {A principal factor that contributes towards the failure to eradicate leishmaniasis and tuberculosis infections is the reduced efficacy of existing chemotherapies, owing to a continuous increase in multidrug-resistant strains of the causative pathogens. This accentuates the dire need to develop new and effective drugs against both plights. A series of naphthoquinone-triazole hybrids was synthesized and evaluated in vitro against Leishmania (L.) and Mycobacterium tuberculosis (Mtb) strains. Their cytotoxicities were also evaluated, using the human embryonic kidney cell line (HEK-293). The hybrids were found to be non-toxic towards human cells and had demonstrated micromolar cellular antileishmanial and antimycobacterial potencies. Hybrid 13, i.e. 2-{\\{}[1-(4-methylbenzyl)-1H-1,2,3-triazol-4-yl]methoxy{\\}}naphthalene-1,4-dione was the most active of all. It was found with MIC90 0.5 µM potency against Mtb in a protein free medium, and with half-maxima inhibitory concentrations (IC50) of 0.81 µM and 1.48 µM against the infective promastigote parasites of L. donavani and L. major, respectively, with good selectivity towards these pathogens (SI 22 - 65). Comparatively, the clinical naphthoquinone, atovaquone, although less cytotoxic, was found to be two-fold less antimycobacterial potent, and six- to twelve-fold less active against leishmania. Hybrid 13 may therefore stand as a potential anti-infective hit for further development in the search for new antitubercular and antileishmanial drugs. 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