Development of Naphthalene-Derivative Bis-QACs as Potent Antimicrobials: Unraveling Structure–Activity Relationship and Microbiological Properties DOI Creative Commons
Nikita A. Frolov, Mary A. Seferyan, Elena V. Detusheva

и другие.

Molecules, Год журнала: 2024, Номер 29(23), С. 5526 - 5526

Опубликована: Ноя. 22, 2024

While the pandemic is behind us, world community faces a global threat of bacterial resistance outbreak. One key ways to combat spread multi-resistant bacteria infection prevention and control tactics using modern antiseptic disinfectant compositions. Herein, we continue path unravel structure–activity relationship (SAR) potent pyridine-derived biocide class bis-quaternary ammonium compounds (QACs). In this study, twenty dihydroxynaphthalene-derivative bis-QACs were subjected extensive microbiological analysis on planktonic cells biofilms ESKAPE microorganisms. Among them, hit superior in their bacteriostatic bactericidal action commercial mono-QACs comparable best bis-QAC market. SAR indicated that linker conformation does not significantly affect activity, though structure symmetry especially lipophilicity had an influence antibacterial performance. Furthermore, delve deeper investigation antimicrobial potential conducted variety assays, including time–kill kinetics, formation, cell morphology, cytotoxicity. Studies showed promising results for 5d 6d, indicating 2 3-fold less cytotoxicity hemotoxicity compared QACs. Moreover, SEM imaging revealed can cause severe membrane damage S. aureus P. aeruginosa strains, confirming great novel as disinfectant.

Язык: Английский

Design, Synthesis, Antiproliferative Activity and In Silico Studies of 2-Oxo-1,2-Dihydroquinolin Derivatives DOI
Eman A. E. El‐Helw, Eman A. Ghareeb, Naglaa F. H. Mahmoud

и другие.

Polycyclic aromatic compounds, Год журнала: 2025, Номер unknown, С. 1 - 16

Опубликована: Фев. 4, 2025

Язык: Английский

Процитировано

0
Naphthyl‐Based Chalcone Derivatives: A Multifaceted Player in Medicinal Chemistry DOI Creative Commons

Priyanka Mahesha,

Nitinkumar S. Shetty

ChemistrySelect, Год журнала: 2024, Номер 9(19)

Опубликована: Май 17, 2024

Abstract Research has placed a great deal of emphasis on molecule development and discovery with substantial biological profiling in recent years. Despite the significant side effects, medicinal chemists have long strived to synthesize drug molecules highest level therapeutic activity lowest possible toxicity. The naphthyl‐based chalcone derivatives drawn attention due their simple structures wide range pharmacological effects. main focus this review is outline biologically active based naphthyl moiety‐substituted developed over A synopsis screening, including relevant structure‐activity relationships, action mechanisms, applications, provided article. It true that prospective hybrids combining moiety different pharmacophores are needed address resistance improve specificity. Therefore, may be useful design new, highly successful drugs previously reported methodologies.

Язык: Английский

Процитировано

2
Development of Naphthalene-Derivative Bis-QACs as Potent Antimicrobials: Unraveling Structure–Activity Relationship and Microbiological Properties DOI Creative Commons
Nikita A. Frolov, Mary A. Seferyan, Elena V. Detusheva

и другие.

Molecules, Год журнала: 2024, Номер 29(23), С. 5526 - 5526

Опубликована: Ноя. 22, 2024

While the pandemic is behind us, world community faces a global threat of bacterial resistance outbreak. One key ways to combat spread multi-resistant bacteria infection prevention and control tactics using modern antiseptic disinfectant compositions. Herein, we continue path unravel structure–activity relationship (SAR) potent pyridine-derived biocide class bis-quaternary ammonium compounds (QACs). In this study, twenty dihydroxynaphthalene-derivative bis-QACs were subjected extensive microbiological analysis on planktonic cells biofilms ESKAPE microorganisms. Among them, hit superior in their bacteriostatic bactericidal action commercial mono-QACs comparable best bis-QAC market. SAR indicated that linker conformation does not significantly affect activity, though structure symmetry especially lipophilicity had an influence antibacterial performance. Furthermore, delve deeper investigation antimicrobial potential conducted variety assays, including time–kill kinetics, formation, cell morphology, cytotoxicity. Studies showed promising results for 5d 6d, indicating 2 3-fold less cytotoxicity hemotoxicity compared QACs. Moreover, SEM imaging revealed can cause severe membrane damage S. aureus P. aeruginosa strains, confirming great novel as disinfectant.

Язык: Английский

Процитировано

1