2-Aryl benzimidazoles: Synthesis, In vitro α-amylase inhibitory activity, and molecular docking study

Akande, Akinsola; Khan, Khalid Mohammed; Salar, Uzma; Aboaba, Sherifat A.; Kanwal,; Chigurupati, Sridevi; Fatima, Itrat; Taha, Muhammad; Wadood, Abdul; Mohammad, Jahidul Isalm; Khan, Huma; Perveen, Shahnaz

doi:10.1016/j.ejmech.2018.03.011

Cited by 51 publications

(23 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…[6] In addition, the benzimidazole-substituted compounds possesses anti-fungal, antiviral, anthelmintic, antiproliferative, anti-hypertensive, H-3 antagonistic, human glucagon receptor antagonistic, male contraceptive and anti-infective activities. [6][7][8][9][10] Benzimidazole derivatives also exhibit significant cytotoxic activity towards leukemia, lung, prostate, melanoma, kidneys, breast and colon human cancer cell lines. [11][12][13][14][15][16] Yadav and group prepared a series of benzimidazole derivatives and determined their anticancer activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of benzimidazole pendant cyanopyrimidine derivatives as anticancer agents

Wang

Akhtar

Nainwal

et al. 2020

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

Thirteen new benzimidazole pendant cyanopyrimidine derivatives were synthesized. The compounds were synthesized through multistep reaction protocol. The structures of synthesized derivatives were studied by EI‐MS, 1H NMR, FT‐IR and elemental analysis. All the compounds were studied for their anticancer activity at National Cancer Institute. Except compound 7j, all the compounds unveiled cytotoxicity against cancer cells. The most active compound 7a had shown highest value of growth inhibition of 88.44% and 84.19% against HOP‐92 and T‐47D cancer cell lines.

show abstract

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of benzimidazole pendant cyanopyrimidine derivatives as anticancer agents

Wang

Akhtar

Nainwal

et al. 2020

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

show abstract

“…Some of them show anticancer potency [9,15] or neuroprotective properties [8]. Benzimidazole derivatives are also known as β-glucuronidase [16,17], α-glucosidase [18,19], urease [20], and α-amylase enzymes inhibitors [21]. Molecular modeling studies for 5-aryl-4-(1,3,4-thiadiazol-2-yl)benzene-1,3-diols obtained by us indicated a network of essential bonds between the -OH groups of the benzenediol ring and the residues of amino acid AChE in the active site which results in a significant inhibitory effect against AChE [22,23].…”

Section: Introductionmentioning

confidence: 99%

Biological Evaluation, Molecular Docking, and SAR Studies of Novel 2-(2,4-Dihydroxyphenyl)-1H- Benzimidazole Analogues

et al. 2019

View full text Add to dashboard Cite

In the present study, new 4-(1H-benzimidazol-2-yl)-benzene-1,3-diols, modified in both rings, have been synthesized and their efficacies as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors have been determined.The modified Ellman's spectrophotometric method was applied for the biological evaluation. The compounds showed strong (IC 50 80-90 nM) AChE and moderate (IC 50 5-0.2 µM) BuChE inhibition in vitro. Some compounds were effective toward AChE/BuChE, exhibiting high selectivity ratios versus BuChE, while the other compounds were active against both enzymes. The structure-activity relationships were discussed. The compounds inhibited also in vitro self-induced Aβ(1-42) aggregation and exhibited antioxidant properties. The docking simulations showed that the benzimidazoles under consideration interact mainly with the catalytic site of AChE and mimic the binding mode of tacrine.

show abstract

“…Benzimidazole derivatives were synthesized by protocol described previously [36]. Briefly, o-phenylene diamine derivative (1 mmol) and substituted benzaldehyde (1 mmol) were taken in N,N-dimethylformamide (10 mL) into a 100 mL round-bottomed flask.…”

Section: Overall Technique For the Synthesis Of Benzimidazoles (A1 Anmentioning

confidence: 99%

Novel Azoles as Antiparasitic Remedies against Brain-Eating Amoebae

et al. 2020

Self Cite

View full text Add to dashboard Cite

Balamuthia mandrillaris and Naegleria fowleri are opportunistic protozoan pathogens capable of producing infection of the central nervous system with more than 95% mortality rate. Previously, we have synthesized several compounds with antiamoebic properties; however, synthesis of compounds that are analogues of clinically used drugs is a highly desirable approach that can lead to effective drug development against these devastating infections. In this regard, compounds belonging to the azole class possess wide range of antimicrobial properties and used clinically. In this study, six novel benzimidazole, indazole, and tetrazole derivatives were synthesized and tested against brain-eating amoebae. These compounds were tested for their amoebicidal and static properties against N. fowleri and B. mandrillaris. Furthermore, the compounds were conjugated with silver nanoparticles and characterized. The synthetic heterocyclic compounds showed up to 72% and 65% amoebicidal activities against N. fowleri and B. mandrillaris respectively, while expressing up to 75% and 70% amoebistatic activities, respectively. Following conjugation with silver nanoparticles, amoebicidal activities of the drugs increased by up to 46 and 36% versus B. mandrillaris and N. fowleri. Minimal effects were observed when the compounds were evaluated against human cells using cytotoxicity assays. In summary, azole compounds exhibited potent activity against N. fowleri and B. mandrillaris. Moreover, conjugation of the azole compounds with silver nanoparticles further augmented the capabilities of the compounds against amoebae.

show abstract

2-Aryl benzimidazoles: Synthesis, In vitro α-amylase inhibitory activity, and molecular docking study

Cited by 51 publications

References 27 publications

Synthesis and biological evaluation of benzimidazole pendant cyanopyrimidine derivatives as anticancer agents

Synthesis and biological evaluation of benzimidazole pendant cyanopyrimidine derivatives as anticancer agents

Biological Evaluation, Molecular Docking, and SAR Studies of Novel 2-(2,4-Dihydroxyphenyl)-1H- Benzimidazole Analogues

Novel Azoles as Antiparasitic Remedies against Brain-Eating Amoebae

Contact Info

Product

Resources

About