Multidrug-resistant bacterial infections have become a global threat. We recently disclosed that the known IKK-β inhibitor IMD-0354 and subsequent analogues abrogate colistin resistance in several Gram-negative strains. Herein, we report the activity of a second-generation library of IMD-0354 analogues incorporating a benzimidazole moiety as an amide isostere. We identified several analogues that show increased colistin potentiation activity against Gram-negative bacteria.
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http://dx.doi.org/10.1021/acsinfecdis.1c00463 | DOI Listing |
Antimicrob Agents Chemother
October 2024
Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana, USA.
ACS Catal
August 2024
Department of Biochemistry and Molecular Biology, University of Georgia, Athens, Georgia 30602, United States.
Tryptophan indole lyase (TIL; [E.C. 4.
View Article and Find Full Text PDFLangmuir
April 2024
Department of Chemistry, Virginia Commonwealth University, Richmond, Virginia 23284, United States.
Chem Biol Drug Des
August 2023
Department of Pharmaceutical Sciences, School of Pharmacy, Lovely Professional University, Punjab, India.
Cancer is the second leading cause of death globally, with 9.6 million deaths yearly. As a life-threatening disease, it necessitates the emergence of new therapies.
View Article and Find Full Text PDFArch Pharm (Weinheim)
February 2023
Medicinal Chemistry Department, Faculty of Pharmacy, Minia University, Minia, Egypt.
A series of new 1,3,4-oxadiazole-chalcone/benzimidazole hybrids 9a-o and 10a-k were designed and synthesized as potential antiproliferative agents. Hybrids 9a-o exhibited remarkable antiproliferative activities on different NCI-60 cell lines in a single-dose assay. The antiproliferative activities of the newly synthesized compounds were evaluated against a panel of four human cancer cell lines (A-549, MCF-7, Panc-1, and HT-29).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!