Title:Ninety Years of Pentamidine: The Development and Applications of
Pentamidine and its Analogs
Volume: 29
Issue: 26
Author(s): Bo Zhang, Yushan Jin, Lei Zhang, Hongshuang Wang*Xiaohui Wang*
Affiliation:
- Laboratory of Chemical Biology, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences,
Changchun, Jilin, China
- Laboratory of Chemical Biology, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences,
Changchun, Jilin, China
- School of Applied Chemistry and Engineering, University of Science and Technology
of China, Hefei, Anhui, China
Keywords:
Pentamidine, antimicrobial drug, DNA minor groove ligands, SARS-CoV-2, 3a channel, inhibitors of PPIs, amidine.
Abstract: Pentamidine, an FDA-approved human drug for many protozoal infections,
was initially synthesized in the late 1930s and first reported to be curative for parasitosis
in the 1940s. After ninety years of sometimes quiet growth, pentamidine and its derivatives
have gone far beyond antibacterial agents, including but not limited to the ligands
of DNA minor groove, modulators of PPIs (protein-protein interactions) of the transmembrane
domain 5 of lateral membrane protein 1, and the blockers of the SARS-CoV-2 3a
channel. This mini-review highlights the development and applications of pentamidine
and its analogs, aiming to provide insights for further developing pentamidine derivatives
in the following decades.
