Pyrazolyl Thioureas and Carbothioamides with an NNSN Motif against MSSA and MRSA

Pyrazolyl Thioureas and Carbothioamides with an NNSN Motif against MSSA and MRSA

A novel series of copper-activatable drugs intended for use against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant S. aureus (MRSA) were synthesized, characterized, and tested against the MSSA strain Newman and the MRSA Lac strain (a USA300 strain), respectively. These...

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Bibliographic Details
Published in:ACS omega Vol. 6; no. 9; pp. 6088 - 6099
Main Authors: Delpe-Acharige, Anjana, Zhang, Man, Eschliman, Kayla, Dalecki, Alex, Covarrubias-Zambrano, Obdulia, Minjarez-Almeida, Azriel, Shrestha, Tejaswi, Lewis, Tanji, Al-Ibrahim, Fatimah, Leonard, Sophia, Roberts, Riana, Tebeje, Anteneh, Malalasekera, Aruni P, Wang, Hongwang, Kalubowilage, Madumali, Wolschendorf, Frank, Kutsch, Olaf, Bossmann, Stefan H
Format: Journal Article
Language:English
Published: United States American Chemical Society 09-03-2021
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Summary:A novel series of copper-activatable drugs intended for use against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant S. aureus (MRSA) were synthesized, characterized, and tested against the MSSA strain Newman and the MRSA Lac strain (a USA300 strain), respectively. These drugs feature an NNSN structural motif, which enables the binding of copper. In the absence of copper, no activity against MSSA and MRSA at realistic drug concentrations was observed. Although none of the novel drug candidates exhibits a stereocenter, sub-micromolar activities against SA Newman and micromolar activities against SA Lac were observed in the presence, but not in the absence, of bioavailable copper. Copper influx is a component of cellular response to bacterial infections, which is often described as nutritional immunity.
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ISSN:2470-1343
2470-1343
DOI:10.1021/acsomega.0c04513