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Synthesis of New Benzoxazole Derivatives and Evaluation of their Antifungal and Antibacterial Activities
UTTAR PRADESH JOURNAL OF ZOOLOGY Pub Date : 2024-01-25 , DOI: 10.56557/upjoz/2024/v45i33872 Vaishali Bhardwaj , Anurag Sharma
UTTAR PRADESH JOURNAL OF ZOOLOGY Pub Date : 2024-01-25 , DOI: 10.56557/upjoz/2024/v45i33872 Vaishali Bhardwaj , Anurag Sharma
Analytical chemistry aims to synthesize some novel benzoxazole derivatives with lower side effects and more efficacy. In this research, we synthesized the target compound’s reaction of 2- aminophenol in methanol and added carbon disulfide to obtain benzo[d] oxazole-2-thiol. This obtained compound again reacts with 4-chlorobenzoic acid to form 4-(benzo [d]oxazol-2-ylthio) benzoic acid. 4-(benzo[d]oxazol-2-ylthio) benzoic acid was further treated with substituted esters to give the crude product (4a-4e). The structures of derivatives are characterized with the help of IR, 1H NMR, TLC Spectroscopy, and melting point. The derivatives of the compounds were tested for antibacterial & antifungal activities. Antimicrobial evaluation was performed individually with gram-positive and gram-negative bacteria S. aureus and Pseudomonas aeruginosa. Aspergillus niger and Candida albicans were the two types of fungi on which antifungal activities were conducted. The outcomes were compared to those of the common medications Amphotericin B and Ciprofloxacin. It was discovered that the produced compounds have considerable antibacterial and antifungal activity. Four synthesized derivatives are named as 4 (d, b, e, c). The 4 d showed a good antimicrobial activity against the S. aureus. The 4 c showed good antifungal activities against the Candida albicans MTCC3541. The order of antifungal activity of these synthesized compounds is 4c >4e > 4b >4d. The standard. The 4 c showed a good antifungal activity against the C. albicans.
中文翻译:
新型苯并恶唑衍生物的合成及其抗真菌、抗菌活性评价
分析化学旨在合成一些副作用更低、功效更强的新型苯并恶唑衍生物。本研究合成了目标化合物2-氨基苯酚在甲醇中加入二硫化碳反应得到苯并[d]恶唑-2-硫醇。所得化合物再次与4-氯苯甲酸反应形成4-(苯并[d]恶唑-2-基硫基)苯甲酸。将4-(苯并[d]恶唑-2-基硫基)苯甲酸进一步用取代的酯处理,得到粗产物(4a-4e)。衍生物的结构通过IR、1H NMR、TLC光谱和熔点进行表征。测试了这些化合物的衍生物的抗菌和抗真菌活性。对革兰氏阳性菌和革兰氏阴性菌金黄色葡萄球菌和铜绿假单胞菌分别进行抗菌评价。黑曲霉和白色念珠菌是对其进行抗真菌活性的两种真菌。结果与常用药物两性霉素 B 和环丙沙星的结果进行了比较。发现所产生的化合物具有相当大的抗菌和抗真菌活性。四种合成的衍生物被命名为4(d、b、e、c)。4 d 对金黄色葡萄球菌表现出良好的抗菌活性。4c对白色念珠菌MTCC3541表现出良好的抗真菌活性。这些合成化合物的抗真菌活性顺序为4c>4e>4b>4d。标准。4c 对白色念珠菌表现出良好的抗真菌活性。
更新日期:2024-01-25
中文翻译:
新型苯并恶唑衍生物的合成及其抗真菌、抗菌活性评价
分析化学旨在合成一些副作用更低、功效更强的新型苯并恶唑衍生物。本研究合成了目标化合物2-氨基苯酚在甲醇中加入二硫化碳反应得到苯并[d]恶唑-2-硫醇。所得化合物再次与4-氯苯甲酸反应形成4-(苯并[d]恶唑-2-基硫基)苯甲酸。将4-(苯并[d]恶唑-2-基硫基)苯甲酸进一步用取代的酯处理,得到粗产物(4a-4e)。衍生物的结构通过IR、1H NMR、TLC光谱和熔点进行表征。测试了这些化合物的衍生物的抗菌和抗真菌活性。对革兰氏阳性菌和革兰氏阴性菌金黄色葡萄球菌和铜绿假单胞菌分别进行抗菌评价。黑曲霉和白色念珠菌是对其进行抗真菌活性的两种真菌。结果与常用药物两性霉素 B 和环丙沙星的结果进行了比较。发现所产生的化合物具有相当大的抗菌和抗真菌活性。四种合成的衍生物被命名为4(d、b、e、c)。4 d 对金黄色葡萄球菌表现出良好的抗菌活性。4c对白色念珠菌MTCC3541表现出良好的抗真菌活性。这些合成化合物的抗真菌活性顺序为4c>4e>4b>4d。标准。4c 对白色念珠菌表现出良好的抗真菌活性。