Synthesis and Anthelmintic Evaluation of Novel Valerolactam- Benzimidazole Hybrids

Munguía, Beatriz; Mendina, Pablo; Espinosa, Romina; Lanz, Andrea; Saldaña, Jenny; Andina, María J.; Ures, X.; López, Andrés; Manta, Eduardo; Domínguez, Laura

doi:10.2174/15701808113109990028

Cited by 15 publications

(12 citation statements)

References 7 publications

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“…8, 8.7, 15.8, 17.4 and 20.3 min, respectively. A mobile phase of acetonitrile:water (20:80) in isocratic mode, at a flow rate of 1 ml/min, with detection at 210 nm, was conducted for compound 2 (valerolactam derivative), as reported (Munguía et al, 2013). Under these chromatographic conditions, the retention times for compound 2 and IS were 6.06 and 10.84 min respectively.…”

Section: Hplc Analysis and Methods Validationmentioning

confidence: 99%

“…Quantification of drugs was done according to what we have previously described (Munguía et al, 2013) with minor modifications, by spiking known amounts in parasite material and repeating the whole process described earlier (by quintuplicate).…”

Section: Hplc Analysis and Methods Validationmentioning

confidence: 99%

“…Phenacetin was used as internal standard (IS) as previously reported (Domínguez et al, 1995). The new series of hybrid compounds valerolactam-benzimidazole (compounds 8, 9 and 10) and valerolactam compound 2 were synthesized according to our recent findings (Munguía et al, 2013). Sulphoxide metabolites of ABZ, FEB, and hybrid compounds 8 and 10 (ABZ SX, FEB SX, 11, and 12, respectively) were synthesized and characterized as described in the Supplementary data.…”

Section: Chemicalsmentioning

confidence: 99%

“…In this context, we have recently reported (Munguía et al, 2013) the design and preparation of hybrid molecules with a dual mode of action (Meunier, 2008) to create efficient new anthelmintic drugs. Novel valerolactam-benzimidazole hybrids were synthesized based on the fusion of two active fragments (Fig.…”

Section: Introductionmentioning

confidence: 99%

“…1). This strategy was used to improve physicochemical properties regarding in vitro bioactive valerolactam moiety (compound 2, Munguía et al, 2013), together with the ex vivo ability of compounds to diffuse into the target parasite studied (the rat parasitic nematode Nippostrongylus brasiliensis four-stage). In that report we have showed the usefulness of diffusion studies jointly with in vitro physiology-based assays to search for anthelmintics.…”

Section: Introductionmentioning

confidence: 99%

See 4 more Smart Citations

Development of novel valerolactam-benzimidazole hybrids anthelmintic derivatives: Diffusion and biotransformation studies in helminth parasites

Munguía

Michelena

Melian

et al. 2015

Experimental Parasitology

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Section: Hplc Analysis and Methods Validationmentioning

confidence: 99%

Section: Hplc Analysis and Methods Validationmentioning

confidence: 99%

Section: Chemicalsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Development of novel valerolactam-benzimidazole hybrids anthelmintic derivatives: Diffusion and biotransformation studies in helminth parasites

Munguía

Michelena

Melian

et al. 2015

Experimental Parasitology

Self Cite

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Microwave assisted synthesis, biological activities, and in silico investigation of some benzimidazole derivatives

Bhavsar

Acharya

Jethava

et al. 2020

Journal of Heterocyclic Chem

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Some derivatives of 2-substituted benzimidazole were prepared via coupling of N-methyl-o-phenylenediamine or o-phenylenediamine with different aromatic aldehydes catalyzed by Ni(OAc) 2 in the presence of chloroform under microwave-assisted conditions. Structural confirmation of all synthesized molecules was investigated by FT-IR, 13 C NMR, 1 H NMR, ESI-MS, and Elemental analysis. All prepared molecules were examined for in-vitro pharmaceutical activities like antibacterial, antifungal, antimalarial, antituberculosis, and antioxidant. Additionally, in silico study was also carried out. We also evaluated the steadiness and molecular interaction of docked complex, that is, complex of molecule (7s) with PDB: 5ZNI and complex of derivative (7l) with PDB: 3VLN, we have established a molecular dynamics model on the best dock molecules. All newly prepared molecules were authenticated to have excellent pharmacokinetics stuffs via calculated ADME-Tox descriptors, which signifying that these derivatives could be utilized as hit for the expansion of the some innovative active compounds.

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Synthetic Clubbing of 2-Methyl-5-Nitroimidazole with 5(6)-Substituted-1H-Benzimidazole as Potential Antimicrobial and Anthelmintic Agents

Pattanayak

Behera

2023

Pharm Chem J

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Synthesis and Anthelmintic Evaluation of Novel Valerolactam- Benzimidazole Hybrids

Cited by 15 publications

References 7 publications

Development of novel valerolactam-benzimidazole hybrids anthelmintic derivatives: Diffusion and biotransformation studies in helminth parasites

Development of novel valerolactam-benzimidazole hybrids anthelmintic derivatives: Diffusion and biotransformation studies in helminth parasites

Microwave assisted synthesis, biological activities, and in silico investigation of some benzimidazole derivatives

Synthetic Clubbing of 2-Methyl-5-Nitroimidazole with 5(6)-Substituted-1H-Benzimidazole as Potential Antimicrobial and Anthelmintic Agents

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