“Design, Synthesis, And Characterization Of Novel Benzimidazole Derivatives And Their Biological Evaluation”

Main Article Content

Chandanshive S. N.
Pathade K.S
Mulla S.S.
Chate N.G
Kamble P.I.

Abstract

Because of their various biological functions and possible therapeutic uses, benzimidazole derivatives have drawn a lot of interest in medicinal chemistry. Our goal was to create, manufacture, and assess a number of new benzimidazole derivatives with improved pharmacological properties in this work. In order to maximize target interactions with particular biological targets, the benzimidazole scaffold was logically modified during the design process. A multistep synthetic process was used to create the novel derivatives, allowing for the integration of various functional groups. The effective synthesis of the intended chemicals was confirmed by characterizing techniques such nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry, and infrared spectroscopy. The produced compounds were then evaluated using an in vitro techniques. Human cell lines were used in preliminary cytotoxicity tests to get knowledge about the derivatives' possible safety characteristics. This study's findings identified a number of benzimidazole compounds with significant biological properties and possible medicinal uses. In conclusion, a number of substances with remarkable therapeutic potential have been produced as a result of the design, synthesis, and assessment of novel benzimidazole derivatives.

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How to Cite
Chandanshive S. N., Pathade K.S, Mulla S.S., Chate N.G, & Kamble P.I. (2024). “Design, Synthesis, And Characterization Of Novel Benzimidazole Derivatives And Their Biological Evaluation”. Journal of Advanced Zoology, 44(5), 676–688. https://doi.org/10.53555/jaz.v44i5.3140
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Articles
Author Biographies

Chandanshive S. N.

Department of Pharmaceutical Chemistry, Appaseheb Birnale Collage of Pharmacy, Sangli, 416416, Maharashtra, India

Pathade K.S

Department of Pharmaceutical Chemistry, Appaseheb Birnale Collage of Pharmacy, Sangli, 416416, Maharashtra, India

Mulla S.S.

Department of Pharmaceutical Chemistry, Appaseheb Birnale Collage of Pharmacy, Sangli, 416416, Maharashtra, India

Chate N.G

Department of Pharmaceutical Chemistry, Appaseheb Birnale Collage of Pharmacy, Sangli, 416416, Maharashtra, India

Kamble P.I.

Department of Pharmaceutical Chemistry, Appaseheb Birnale Collage of Pharmacy, Sangli, 416416, Maharashtra, India

References

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6864827/#:~:text=The%20applicatioa%20of%20heterocycles%20provides,of%20drugs%20or%20drug%20candidates

Al-Mulla A. A review: biological importance of heterocyclic compounds. Der Pharma Chemica. 2017;9(13):141-7.

Roman G. Mannich bases in medicinal chemistry and drug design. European journal of medicinal chemistry. 2015 Jan 7;89:743-816.

Bala S, Sharma N, Kajal A, Kamboj S, Saini V. Mannich bases: an important pharmacophore in present scenario. International journal of medicinal chemistry. 2014;2014.

Keri RS, Hiremathad A, Budagumpi S, Nagaraja BM. Comprehensive review in current developments of benzimidazole‐based medicinal chemistry. Chemical biology & drug design. 2015 Jul;86(1):19-65.

Bansal Y, Silakari O. The therapeutic journey of benzimidazoles: A review. Bioorganic & medicinal chemistry. 2012 Nov 1;20(21):6208-36.

Sharma S, Abuzar S. The benzimidazole anthelmintics—chemistry and biological activity. Progress in Drug Research/Fortschritte der Arzneimittelforschung/Progrèsdes recherches pharmaceutiques. 1983 Jan 1:85-161.

Yadav G, Ganguly S. Structure activity relationship (SAR) study of benzimidazole scaffold for different biological activities: A mini-review. European journal of medicinal chemistry. 2015 Jun 5;97:419-43.

https://encyclopedia.pub/entry/31419#:~:text=Among%20the%20BZs%2C%20benzimidazole%20(BI,because%20of%20the%20annular%20tautomerism.

Srestha N, Banerjee J, Srivastava S. A review on chemistry and biological significance of benzimidazole nucleus. IOSR J Pharm. 2014 Dec;4(12):28-41

Padhy GK, Panda J, Raul SK, Behera AK. 2-Acetylbenzimidazole: a Valuable Synthon for the Synthesis of Biologically Active Molecules.

Wu L, Yang Y, Wang Z, Wu X, Su F, Li M, Jing X, Han C. Design, Synthesis, and Biological Evaluation of Aromatic Amide-Substituted Benzimidazole-Derived Chalcones. The Effect of Upregulating TP53 Protein Expression. Molecules. 2020 Mar 5;25(5):1162.

Chawla A, Kaur G, Sharma AK. Green Chemistry as a Versatile Technique for the Synthesis of Benzimidazole Derivatives. Int. J. Pharm. Phytopharmacol. Res.. 2012;2:148-59.

Kalirajan R, Rathore L, Jubie S, Gowramma B, Gomathy S, Sankar S. Microwave assisted synthesis of some novel pyrazole substituted benzimidazoles and evaluation of their biological activities.

Eswayah A, Khaliel S, Saad S, Shebani N, Fhid O, Belaid A, Alsharif T, Elforjane H, Saadalla Y, Baga E. Synthesis and analgesic activity evaluation of some new benzimidazole derivatives. American Journal of Chemistry and Application. 2017;4(5):30-5.

Hashem HE, El Bakri Y. An overview on novel synthetic approaches and medicinal applications of benzimidazole compounds. Arabian Journal of Chemistry. 2021 Nov 1;14(11):103418.

Rathee PS, Dhankar R, Bhardwaj S, Gupta M, Kumar R. Synthesis and antimicrobial studies of novel benzimidazole derivatives. Journal of Applied pharmaceutical science. 2011 Jun 30(Issue):127-30.

Lai Z, Wu R, Li J, Chen X, Zeng L, Wang X, Guo J, Zhao Z, Sajiki H, Cui S. Multicomponent double Mannich alkylamination involving C (sp2)–H and benzylic C (sp3)–H bonds. Nature Communications. 2022 Jan 21;13(1):435.

Gul HI, Tugrak M, Gul M, Mazlumoglu S, Sakagami H, Gulcin I, Supuran CT. New phenolic Mannich bases with piperazines and their bioactivities. Bioorganic chemistry. 2019 Sep 1;90:103057.

Saranya S, Harry NA, Krishnan KK, Anilkumar G. Recent developments and perspectives in the asymmetric Mannich reaction. Asian Journal of Organic Chemistry. 2018 Apr;7(4):613-33.

Sujith KV, Rao JN, Shetty P, Kalluraya B. Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety. European journal of medicinal chemistry. 2009 Sep 1;44(9):3697-702

LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Antineoplastic Agents. [Updated 2023 Feb 13]. Available from: https://www.ncbi.nlm.nih.gov/books/NBK548022/

Strober W. Trypan Blue Exclusion Test of Cell Viability. Curr Protoc Immunol. 2015 Nov 2;111:A3.B.1-A3.B.3. doi: 10.1002/0471142735.ima03bs111. PMID: 26529666; PMCID: PMC6716531.

https://www.testing.com/tests/lactatedehydrogenaseldh/#:~:text=Lactate%20dehydrogenase%20(LDH)%20is%20a,evaluate%20certain%20types%20of%20cancer.

https://www.sigmaaldrich.com/IN/en/technical-documents/protocol/cell-culture-andcell-culture-analysis /cell-counting-and-health-analysis/cell-proliferation-kit-i-mtt

https://www.sigmaaldrich.com/IN/en/technical-documents/protocol/cell-culture-andcell-culture-analysis/ cell-counting-and-health-analysis/cell-proliferation-kit-xtt-assay

Orellana EA, Kasinski AL. Sulforhodamine B (SRB) Assay in Cell Culture to Investigate Cell Proliferation. Bio Protoc. 2016 Nov 5;6(21):e1984. doi: 10.21769/BioProtoc.1984. PMID: 28573164; PMCID: PMC5448418.

Sawant VJ, Bamane SR, Shejwal RV, Patil SB. Comparison of drug delivery potentials of surface functionalized cobalt and zinc ferrite nanohybrids for curcumin in to MCF7 breast cancer cells. Journal of Magnetism and Magnetic Materials. 2016 Nov 1;417:222-9.

https://www.yourgenome.org/facts/what-are-helminths/

Shahare MB, Kadam VJ, Jagdale DM, Gandhi PS, Gaikwad PL. Synthesis and evaluation of novel anthelmentic benzimidazole derivatives. Int. J. Res. Pharm. Chem. 2012;2(1):132-6.

Aswar M, Aswar U, Watkar B, Vyas M, Wagh A, Gujar KN. Anthelmintic activity of Ficus benghalensis. International Journal of Green Pharmacy (IJGP). 2008;2(3).

Islam, S., Fahad, F.I., Sultana, A., Sayem, S.A.J., Roy, S.B., Islam, M.N., Roy, A. and Sayeed, M.A., 2022. Evaluation of antioxidant, cytotoxic, anti-inflammatory, antiarthritic, thrombolytic, and anthelmintic activity of methanol extract of Lepidagathis hyalina Nees root. Evidence-Based Complementary and Alternative Medicine, 202