Cytotoxic, Thrombolytic and Antibacterial Evaluation of Synthesized Substituted and Un-Substituted Selenium-N-Heterocyclic Carbene Adducts

IF 0.6 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Journal of the chemical society of pakistan Pub Date : 2023-01-01 DOI:10.52568/001198/jcsp/45.01.2023
Amna Kamal Amna Kamal, Muhammad Adnan Iqbal Muhammad Adnan Iqbal, Haq Nawaz Bhatti and Abdul Ghaffar Haq Nawaz Bhatti and Abdul Ghaffar
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引用次数: 1

Abstract

Alkyl-substituted azolium salts (1-8) and their Se-N-heterocyclic carbene (Se-N-Het-C) adducts (9-12) were obtained in very reasonable yields. All synthesized azolium salts and their Se-N-Het-C adducts were characterized by different spectroscopic techniques such as FT-IR, 1HNMR, 13CNMR, and elemental analysis. It was found that all synthesized Se-N-Het-C adducts were stable at room temperature in both air and moisture. In-vitro these compounds (5-12) were assessed for their antimicrobial potential against Bacillus subtilis (B. subtilis), Macrococcus brunensis (M. brunensis), and Bacillus cereus (B. cereus) in vitro. Results of MIC and inhibition zone values revealed that the majority of the Selenium N-Heterocyclic carbene adducts were active against Bacillus subtilis (B. subtilis) than Macrococcus brunensis (M. brunensis) and Bacillus cereus (B. cereus) whereas opposite in the azolium salts (5-8). Compounds 5-8 have an inhibition zone of 16and#177;0.1-26and#177;0.3mm against all tested bacterial strains while selenium-NHC adducts 9-12 have a zone of inhibition (16and#177;0.2 to 25 and#177; 0.4mm). Adduct 12 showed good activity against all tested strains with ZI values 25 and#177; 0.1, 22and#177; 0.5, 17 and#177; 0.3 mm and MIC values 17 and#177; 0.2, 16 and#177; 0.4 and 18 and#177; 0.3 and#181;g/mL against Bacillus subtilis (B. subtilis), Macrococcus brunensis (M. brunensis) and Bacillus cereus (B. cereus) respectively. Adduct 10 showed the highest thrombolysis i-e 86.9% and adduct 12 showed good hemolysis i-e 0.51%. Overall results of thrombolysis and cytotoxicity studies revealed that the compounds are safe for preclinical studies of mouse blood in vitro.
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合成取代和未取代硒- n-杂环卡宾加合物的细胞毒性、溶栓性和抗菌性评价
烷基取代唑盐(1-8)及其se - n -杂环碳(Se-N-Het-C)加合物(9-12)的产率非常合理。所有合成的唑盐及其Se-N-Het-C加合物通过FT-IR、1HNMR、13CNMR和元素分析等不同的光谱技术进行了表征。结果表明,所有合成的Se-N-Het-C加合物在室温下均稳定。这些化合物(5-12)在体外对枯草芽孢杆菌(B. subtilis)、布鲁氏大球菌(M. brunensis)和蜡样芽孢杆菌(B. cereus)的抑菌潜力进行了评估。MIC和抑制带值结果显示,n -杂环碳杂烯硒加合物对枯草芽孢杆菌(B. subtilis)的抑制作用强于褐大球菌(M. brunensis)和蜡样芽孢杆菌(B. cereus),而对唑盐的抑制作用则相反(5-8)。化合物5-8对所有测试菌株的抑制区为16和#177;0.1-26和#177;0.3mm,而硒- nhc加合物9-12对所有测试菌株的抑制区为16和#177;0.2 至25 和#177; 0.4mm。加合物12显示良好的活动对所有测试菌株子值25 # 177; 0.1,22 # 177; 0.5,17个 和# 177;17  0.3毫米和麦克风值# 177; 0.2,16 # 177; 0.4和18 和# 177; 0.3和# 181;g / mL对枯草芽孢杆菌(枯草芽孢杆菌),Macrococcus brunensis (m . brunensis)和蜡样芽胞杆菌(b .仙人掌)。加合物10溶栓率最高,为86.9%;加合物12溶栓率较好,为0.51%。溶栓和细胞毒性研究的总体结果表明,这些化合物在体外小鼠血液的临床前研究中是安全的。
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来源期刊
CiteScore
1.30
自引率
14.30%
发文量
41
审稿时长
3.4 months
期刊介绍: This journal covers different research areas in the field of Chemistry. These include; Analytical Chemistry, Applied Chemistry, Biochemistry, Environmental Chemistry, Industrial Chemistry, Inorganic Chemistry, Organic Chemistry and Physical Chemistry. The journal publishes full length articles and Reviews from researchers in academia in addition to featuring comments. Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry.
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