Synthèse et criblage antiplasmodial de quelques benzimidazolyl-chalcones

Ouattara, Mahama; Sissouma, Drissa; Yavo, William; Koné, MW

doi:10.4314/ijbcs.v9i3.48

Cited by 7 publications

(7 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This inversion of efficiency of chalconic derivatives of similar chemical profile had previously been described on field isolates. Indeed, some compounds that had moderate activity on CQ-S isolates were highly effective on CQ-R isolates [33]. However, in our study, this trend was not found with isolates collected from patients.…”

Section: Discussioncontrasting

confidence: 74%

Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates ofPlasmodium falciparum

Dable¹,

Tano²,

Ouattara

et al. 2019

Pathogens and Global Health

View full text Add to dashboard Cite

The extension of Plasmodium falciparum resistance to existing antimalarial drugs is worrying. Faced with this problem, the search for new and effective molecules is necessary. In this context, six chalcone derivatives (B1, B11, B14, B17, SCA02 and SCA03) were tested on field isolates and then reference strains to evaluate their antiplasmodial activity by using the Rieckmann semimicrotest, recommended by WHO, for in vitro and ex vivo activity tests. Compounds B14 and B17 exhibited promising antiplasmodial activities (IC 50s : 14.41-16.40 μM) regardless of the type of isolate. Compounds B1, B11, SCA02 and SCA03 showed a moderate inhibition of field isolates (IC 50S : 25.63-48.29 μM) and very good activity against reference strains (IC50s: 3.82-10.03 μM). Therefore, more structural modulations should improve their efficiency and make these molecules very good candidates for future effective antimalarial drugs.

show abstract

Section: Discussioncontrasting

confidence: 74%

Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates ofPlasmodium falciparum

Dable¹,

Tano²,

Ouattara

et al. 2019

Pathogens and Global Health

View full text Add to dashboard Cite

show abstract

“…As described in our previous work [14,15], the access to 5-substituted-2-acetylbenzimidazole required the prior synthesis of 2-(α-hydroxy) ethyl benzimidazoles. In this perspective, Ophenylenediamine (1a-c) (0.042 mol) suitably chosen, with lactic acid (2) (0.060 mol) in presence of 4N hydrochloric acid (50 mL) were refluxed on the water for 45 min.…”

Section: Synthesis Of 5'-substituted-2acetylbenzimidazolesmentioning

confidence: 99%

“…Based on these observations, in this study, antileishmanial assays against L. donovani promastigotes of 2-arylpropenon-1Hbenzimidazole hybrids have been performed, which have already displayed remarkable anthelmintics, antimalarials, and anticandidosis activities [13][14][15]. Furthermore, the molecules reported as potent anti-leishmanial agents have been selected to investigate their activities against T. brucei.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Profiles of Some Benzimidazolyl-chalcones as Anti-leishmanial and Trypanocidal Agents

N'guessan¹,

Kablan²,

Kacou³

et al. 2021

CSIJ

View full text Add to dashboard Cite

Background: Benzimidazole constitutes a starting point for the development of new antiprotozoal agents since this nucleus exists in several pharmacologically significant molecules, in particular possessing antifungal, antiviral, antibacterial, and antiparasitic properties. Objective: The present study aimed to identify a molecular hit likely to be developed as an anti-leishmanial and antitrypanosomal drug candidate. Methods: Thus, 12 hybrids of chalcone or benzimidazolyl-arylpropenones were synthesized and screened in vitro for anti-leishmanial activity against promastigotes of Leishmania donovani. The microculture tetrazolium assay was used to determine their potential to inhibit 50% of a parasite growth (IC50). Results: Two compounds among 5-chlorobenzimidazole-chalcones (4a and 4c), which exhibited potent activity (IC50<1 μM) against L. donovani and one derivative (4d) poorly effective against L. donovani (IC50>50 μM) were selected to check their trypanocidal activity. Lethal concentration (LC100) values of these compounds were estimated by using observations on the viability of trypomastigotes of Trypanosoma brucei brucei in MEM medium with Earle’s salts and L-glutamine. Seven of the tested compounds (4a, 4b, 4c, 4e, 4g, 4h, and 4j) showed particularly higher inhibitory activity than pentamidine (IC50= 7.6 μM) against L. donovani promastigotes with IC50 values in a range from 0.5 to 1.8 μM. In addition, the 2’-chlorine derivative (4c), displayed potent anti-trypanosomal activity comparable to those of melarsoprol, used as reference drug. Conclusion: These results support this series of benzimidazole holding arylpropenone group in position 2 as a starting point for future optimization to get novel agents active against leishmaniasis and trypanosomiasis.

show abstract

“…Furthermore, the benzimidazole ring also had a panel of biological activities [24] [25] [26]. Among them, the most important which could be quoted are the antiviral [24], antiplasmodial [25] and anthelmintic [26] (Figure 1). Thus, pyrimidines or thiopyrimidines and benzimidazoles play an important role in cellular processes making these molecules valuable to become leads for new drug discoveries.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antibacterial Activities of New 2-(Benzylthio)pyrimidines and 2-(Benzimidazolylmethylthio)pyrimidines Derivatives

Achi¹,

Coulibali²,

Zon³

et al. 2021

OJMC

View full text Add to dashboard Cite

A series of 2-(benzylthio)pyrimidines (6a-l) and 2-(benzimidazolylmethylthio)pyrimidines derivatives (6m and 6n) analogues of ethyl 2-(benzylthio)-6-methyl-4-phenyl-1,4-dihydropyrimidine-5-carboxylates and ethyl 2-(((1H-benzimidazol-2-yl)methyl)thio)-6-methyl-4-phenyl-1,4-dihydropyri-midine-5-carboxylates were prepared and evaluated for antibacterial activity. These compounds were obtained by condensation of 2-thiopyrimidines (4) with benzyl halides or 2-(chloromethyl)-1H-benzimidazole (5) in the presence of a base. All compounds were characterized by 1 H, 13 C and HRMS spectra. Out of fourteen, only eight compounds were screened against multi-resistant strains of Escherichia coli and Staphylococcus aureus. The results revealed that all of them were found to possess significant antibacterial activity against the germs tested. Compounds 6c, 6d, 6h and 6m were more active on S. aureus and compounds 6h and 6m more active on E. coli.

show abstract

Synthèse et criblage antiplasmodial de quelques benzimidazolyl-chalcones

Cited by 7 publications

References 18 publications

Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates ofPlasmodium falciparum

Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates ofPlasmodium falciparum

Synthesis and Biological Profiles of Some Benzimidazolyl-chalcones as Anti-leishmanial and Trypanocidal Agents

Synthesis and Antibacterial Activities of New 2-(Benzylthio)pyrimidines and 2-(Benzimidazolylmethylthio)pyrimidines Derivatives

Contact Info

Product

Resources

About