Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis

Design, synthesis, bio-evaluation, and in silico studies of some N-substituted 6-(chloro/nitro)-1H-benzimidazole derivatives as antimicrobial and anticancer agents

“…38 Especially, the 6-fluoro-1 H -benzimidazole derivative showed potent antibacterial activities against the Gram-positive strains MSSA and MRSA with MIC of 4 and 2–8 μg mL −1 , respectively. 7 Some of our synthesized compounds ( 3s and 4k ) also exhibited potential antibacterial activity with MICs of 2–4 μg mL −1 against MSSA and MSRA when compared with compounds of Tunçbilek et al (2009) and Malasala et al (2021). 5,7 This may be due to the structure of compound 3s and 4k with the presence of N , N -dimethylamino group at position 4 on the phenyl ring of the 1 H -benzimidazole nucleus has shown a similar role to the 4-chloro/4-nitro group that of Tunçbilek et al (2009) and Morcoss et al (2020).…”

“…It is a cyclic ring that has two nitrogens as heteroatoms and is called a heterocyclic aromatic compound. In addition, benzimidazole is a remarkable scaffold of medicinal importance possessing promising pharmacological activities like anticancer, 1–4 antimicrobial, 5–7 anti-inflammation, 8 antiviral, 9 anti-hypertensive, 10 antihistamine, 11 antitubercular, 12 antiulcer, 13 analgesic, 14 anthelmintic, 15 antiprotozoal, 16 antiamoebic, 17 anticonvulsant, 18 and antiparasitic. 19…”

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

“…The derivatives with 4-nitro, 4-chloro, 4-fluoro, 4-bromo, and unsubstituted exerted good to moderate inhibitory actions against S. aureus and M. tuberculosis H37Rv. Similarly, the analogues with phenyl, 3,4-dimethoxy, and 4-chloro exhibited moderate to good inhibitory property S. aureus and M. tuberculosis H37Rv ( Malasala et al, 2021 ). Furthermore, compounds 91–94 inhibited C. albicans and C. neoformans var.…”

“…Besides, co-treatment of compound 81 with colistin exhibited a promising synergistic effect against wild strains E. coli , K. pneumoniae , A. baumannii , and P. aeruginosa with MIC range = 8–16 μg/ml ( Dokla et al, 2020 ). Malasala et al ( Malasala et al, 2021 ) reported nine more potent antibacterial agents 82–90 with MIC range 4–64 μg/ml against several resistant organisms, including methicillin and vancomycin-resistant S. aureus . The derivatives with 4-nitro, 4-chloro, 4-fluoro, 4-bromo, and unsubstituted exerted good to moderate inhibitory actions against S. aureus and M. tuberculosis H37Rv.…”

Cyclocondensation of Anthranilamide with Aldehydes on Gallium-Containing MCM-22 Zeolite Materials

“…In this regard, this study reports that 2,3-dihydroquinazolin-4­(1 H )-ones are an important class of heterocyclic compounds, which has been applied in agrochemicals and medicinal and organic chemistry . Consequently, the central structural motifs of biological interest coupled with another heterocyclic ring have exhibited therapeutic potential in different domains such as antileishmanial, anticancer, antimicrobial, and antituberculosis . Numerous methods have been reported for the synthesis of 2,3-dihydroquinazolin-4­(1 H )-ones, which include the multicomponent reaction of isatoic anhydride, ammonium chloride, and aldehydes using indium chloride, condensation of 2-aminobenzamide with aldehydes using zirconium­(IV) chloride (2 mol­(M)%) in ethanol, and palladium-catalyzed cyclocarbonylation of o -iodoanilines .…”