Pyrazolyl Thioureas and Carbothioamides with an NNSN Motif against MSSA and MRSA
Year: 2021
Type: article
Abstract: 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.
Source: ACS Omega
Authors: Anjana Delpe-Acharige, Man Zhang, Kayla Eschliman, Alex Dalecki, Obdulia Covarrubias-Zambrano, Azriel Minjarez-Almeida, Tejaswi Shrestha, Tanji Lewis, Fatimah Al-Ibrahim, Sophia Leonard, Riana Roberts, Anteneh Tebeje, Aruni P. Malalasekera, Hongwang Wang, Madumali Kalubowilage, Frank Wolschendorf, Olaf Kutsch, Stefan H. Bossmann
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $1,250
OpenAlex ID: W3131645671