Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives

Hyper-inflammation aggravates the symptoms of both communicable and non-communicable diseases. Therefore, anti-inflammatory compounds may have wide therapeutic application. Benzimidazole is a privileged scaffold and its success in drug development is evident from the long list of benzimidazole-based...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2022-11, Vol.56 (8), p.1070-1074
Main Authors: Moharana, Alok Kumar, Dash, Rudra Narayan, Mahanandia, Nimai Charan, Subudhi, Bharat Bhusan
Format: Article
Language:English
Subjects:
Analysis
Anti-inflammatory drugs
Communicable diseases
Health aspects
Inflammation
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Telmisartan
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Summary:Hyper-inflammation aggravates the symptoms of both communicable and non-communicable diseases. Therefore, anti-inflammatory compounds may have wide therapeutic application. Benzimidazole is a privileged scaffold and its success in drug development is evident from the long list of benzimidazole-based drugs with wide range of applications. This study was undertaken to develop new small molecules with anti-inflammatory properties. Compounds MBPHYD, MBNHYD and MBHYDX were synthesised, purified, characterised and found to be non-toxic both in vitro (in 100 ÎĽMconcentration for 24 h vs. 3000 Vero cells/well) and in vivo (at a dose of 100 mg/kg in female Wistar rats with animals observed for 48 h for any mortality). Compounds MBPHYD and MBNHYD were found to possess significant anti-inflammatory properties. Further, in silico analysis suggested their compliance with drug-likeness. While no toxicity was predicted, both compounds were suggested to have good oral bioavailability. Thus, results of this study may encourage further investigation to establish new anti-inflammatory benzimidazoles for application against various disease conditions.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-022-02755-3