Synthesis, Characterization, Cytotoxicity Analysis and Evaluation of Novel Heterocyclic Derivatives of Benzamidine against Periodontal Disease Triggering Bacteria.

Autor: Kavitha R; Department of Biotechnology, Faculty of Applied Science, AIMST University, Bedong 08100, Kedah, Malaysia., Sa'ad MA; Department of Biotechnology, Faculty of Applied Science, AIMST University, Bedong 08100, Kedah, Malaysia.; Centre of Excellence for Vaccine Development (CoEVD), Faculty of Applied Science, AIMST University, Bedong 08100, Kedah, Malaysia., Fuloria S; Centre of Excellence for Biomaterials Engineering, Faculty of Pharmacy, AIMST University, Bedong 08100, Kedah, Malaysia., Fuloria NK; Centre of Excellence for Biomaterials Engineering, Faculty of Pharmacy, AIMST University, Bedong 08100, Kedah, Malaysia.; Center for Transdisciplinary Research, Department of Pharmacology, Saveetha Institute of Medical and Technical Sciences, Saveetha Dental College and Hospital, Saveetha University, Chennai 600077, Tamil Nadu, India., Ravichandran M; Department of Biotechnology, Faculty of Applied Science, AIMST University, Bedong 08100, Kedah, Malaysia.; Centre of Excellence for Vaccine Development (CoEVD), Faculty of Applied Science, AIMST University, Bedong 08100, Kedah, Malaysia.; Mygenome, ALPS Global Holding, Kuala Lumpur 50400, Malaysia., Lalitha P; Department of Biochemistry, Faculty of Medicine, AIMST University, Bedong 08100, Kedah, Malaysia.
Jazyk: angličtina
Zdroj: Antibiotics (Basel, Switzerland) [Antibiotics (Basel)] 2023 Feb 02; Vol. 12 (2). Date of Electronic Publication: 2023 Feb 02.
DOI: 10.3390/antibiotics12020306
Abstrakt: Periodontal disease (PD) is multifactorial oral disease that damages tooth-supporting tissue. PD treatment includes proper oral hygiene, deep cleaning, antibiotics therapy, and surgery. Despite the availability of basic treatments, some of these are rendered undesirable in PD treatment due to side effects and expense. Therefore, the aim of the present study is to develop novel molecules to combat the PD triggering pathogens. The study involved the synthesis of 4-((5-(substituted-phenyl)-1,3,4-oxadiazol-2-yl)methoxy)benzamidine ( 5a-e ), by condensation of 2-(4-carbamimidoylphenoxy)acetohydrazide ( 3 ) with different aromatic acids; and synthesis of 4-((4-(substituted benzylideneamino)-4H-1,2,4-triazol-3-yl)methoxy)benzamidine ( 6a-b ) by treatment of compound 3 with CS 2 followed by hydrazination and a Schiff reaction with different aromatic aldehydes. Synthesized compounds were characterized based on the NMR, FTIR, and mass spectrometric data. To assess the effectiveness of the newly synthesized compound in PD, new compounds were subjected to antimicrobial evaluation against P. gingivalis and E. coli using the micro-broth dilution method. Synthesized compounds were also subjected to cytotoxicity evaluation against HEK-293 cells using an MTT assay. The present study revealed the successful synthesis of heterocyclic derivatives of benzamidine with significant inhibitory potential against P. gingivalis and E. coli . Synthesized compounds exhibited minimal to the absence of cytotoxicity. Significant antimicrobial potential and least/no cytotoxicity of new heterocyclic analogs of benzamidine against PD-triggering bacteria supports their potential application in PD treatment.
Databáze: MEDLINE