Synthesis, Characterization, and Exploring the Antibacterial and Antifungal Potential of 1,4-Dihydropyrimido[1,2-a]benzimidazole Derivatives

IF 1.1 4区 化学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Dharmesh Katariya, Kailash Pancholi, Mahendra Borisagar
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引用次数: 0

Abstract

Objective: This study aims to synthesize and evaluate the antimicrobial efficacy of a series of 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives (IVa–IVo) as potential therapeutic agents against antibiotic-resistant bacteria and fungi. The increasing prevalence of drug-resistant pathogens necessitates the discovery of novel antimicrobial compounds. Methods: The 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives (IVa–IVo) were synthesized and characterized using various spectroscopic techniques. Their antimicrobial activity was assessed through the minimum inhibitory concentration (MIC) method against a spectrum of Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and fungal strains (Candida albicans, Aspergillus niger, Aspergillus clavatus). Results and Discussion: Among the synthesized compounds, derivatives (IVj), (IVb), and (IVl) demonstrated significant antimicrobial activity, particularly against Staphylococcus aureus, Streptococcus pyogenes, and Escherichia coli, with MIC values comparable to those of standard antibiotics. While the overall activity of the 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives was lower than that of the standard drugs, these compounds show promise as lead structures for further optimization and development in the quest to combat drug-resistant pathogens. Conclusions: The study successfully synthesized and identified 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives with notable antimicrobial properties, especially against specific bacterial strains. These findings suggest that with further development, these compounds could contribute to the discovery of new antimicrobial agents to address the growing challenge of drug-resistant infections.

Abstract Image

1,4-二氢嘧啶[1,2-a]苯并咪唑衍生物的合成、表征及抑菌抑菌潜力的探索
目的:合成并评价一系列1,4-二氢嘧啶[1,2-a]苯并咪唑衍生物(ivo - ivo)对耐药细菌和真菌的抑菌效果。耐药病原体的日益流行要求发现新的抗微生物化合物。方法:合成1,4-二氢嘧啶[1,2-a]苯并咪唑衍生物(IVa-IVo),并利用各种光谱技术对其进行表征。通过最低抑菌浓度(MIC)法对革兰氏阳性菌(金黄色葡萄球菌、化脓性链球菌)、革兰氏阴性菌(大肠杆菌、铜绿假单胞菌)和真菌菌株(白色念珠菌、黑曲霉、棒曲霉)的光谱进行抑菌活性评估。结果和讨论:在合成的化合物中,衍生物(IVj)、(IVb)和(IVl)表现出显著的抗菌活性,特别是对金黄色葡萄球菌、化脓性链球菌和大肠杆菌,其MIC值与标准抗生素相当。虽然1,4-二氢嘧啶[1,2-a]苯并咪唑衍生物的总体活性低于标准药物,但这些化合物有望作为进一步优化和开发的先导结构,以对抗耐药病原体。结论:本研究成功合成并鉴定了1,4-二氢嘧啶[1,2-a]苯并咪唑衍生物,该衍生物具有显著的抗菌性能,特别是对特定菌株的抗菌性能。这些发现表明,随着进一步发展,这些化合物可能有助于发现新的抗微生物药物,以应对日益严峻的耐药感染挑战。
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来源期刊
Russian Journal of Bioorganic Chemistry
Russian Journal of Bioorganic Chemistry 生物-生化与分子生物学
CiteScore
1.80
自引率
10.00%
发文量
118
审稿时长
3 months
期刊介绍: Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.
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