Synthesis and Potent Antimicrobial Activities of Some Novel Retinoidal Monocationic Benzimidazoles

Abstract

Several 2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-benzimidazole-5-carboxamidine analogues were synthesized for their antibacterial and antifungal activities against S. aureus, Methicillin-resistant S. aureus (MRSA), C. albicans, and C. krusei. MIC values of the targeted compounds 43-58 are comparable to those of Fluconazole and Sultamicillin. The most potent compounds, 51 and 53, showed MIC values as 0.78 and 1.56 microg/mL against S. aureus and C. albicans, respectively.

Synthesis and potent antistaphylococcal activity of some new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines

“…All new compounds were confirmed by 1 H-NMR, 13 C-NMR, COSY, HSQC, HMBC, LC-MS, and elemental analyze data. The in vitro antistaphylococcal activity revealed that all the carboxamidines showed moderate to potent inhibitory activity, against S. aureus and methicillin-resistant S. aureus (MRSA) strains and compound 28 displayed close activity to the reference clinical drugs.…”

One‐pot synthesis of novel benzimidazoles with a naphthalene moiety as antimicrobial agents and molecular docking studies

“…[ 26–28 ] Many studies have supported the antimicrobial effect of a naphthalene ring on bacterial and fungal strains. [ 29–31 ] In fact, several naphthalene‐containing drugs such as nafcillin, naftifine, tolnaftate, and terbinafine are currently available to treat microbial infections (Figure 1). Naphthalene derivatives bearing a functional group, especially an ‐OH group, on α and β positions possess very good antimicrobial properties.…”

Synthesis, spectroscopic characterization and antiproliferative evaluation in vitro of novel Schiff bases related to benzimidazoles

“…The facts that benzimidazole nuclei is very important pharmacophore in modern drug discovery as well as in medicinal chemistry and that benzimidazole residue is a constituent of vitamin B12, support their potential use as therapeutics. Therefore, benzimidazoles display diverse biological activities such as antimicroabial [19,20], antifungal [21], antitumor [22e24], antiviral [25,26], antihistaminic [27] etc. Benzimidazole and its derivatives have additionally found applications in several other areas as optical laser and polymer dyes in optoelectronics [28,29], organic luminophores, fluorescent tags for detection of biological important molecules, as DNA, RNA or proteins and enzymes [24,30] etc.…”