Kumari Mukesh, Tahlan Sumit, Narasimhan Balasubramanian, Ramasamy Kalavathy, Lim Siong Meng, Shah Syed Adnan Ali, Mani Vasudevan, Kakkar Saloni
Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India.
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia.
BMC Chem. 2021 Jan 21;15(1):5. doi: 10.1186/s13065-020-00717-y.
Triazole is an important heterocyclic moiety that occupies a unique position in heterocyclic chemistry, due to its large number of biological activities. It exists in two isomeric forms i.e. 1,2,4-triazole and 1,2,3-triazole and is used as core molecule for the design and synthesis of many medicinal compounds. 1,2,4-Triazole possess broad spectrum of therapeutically interesting drug candidates such as analgesic, antiseptic, antimicrobial, antioxidant, anti-urease, anti-inflammatory, diuretics, anticancer, anticonvulsant, antidiabetic and antimigraine agents.
The structures of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR). The synthesized compounds were evaluated for their in vitro antimicrobial activity against Gram-positive (B. subtilis), Gram-negative (P. aeruginosa and E. coli) bacterial and fungal (C. albicans and A. niger) strains by tube dilution method using ciprofloxacin, amoxicillin and fluconazole as standards. In-vitro antioxidant and anti-urease screening was done by DPPH assay and indophenol method, respectively. The in-vitro anticancer evaluation was carried out against MCF-7 and HCT116 cancer cell lines using 5-FU as standards.
RESULTS, DISCUSSION AND CONCLUSION: The biological screening results reveal that the compounds T (MIC = 24.7 µM, MIC, = 12.3 µM) and T (MIC = 27.1 µM) exhibited potent antimicrobial activity as comparable to standards ciprofloxacin, amoxicillin (MIC = 18.1 µM, MIC = 17.1 µM) and fluconazole (MIC = 20.4 µM), respectively. The antioxidant evaluation showed that compounds T (IC = 34.83 µg/ml) and T (IC = 34.38 µg/ml) showed significant antioxidant activity and comparable to ascorbic acid (IC = 35.44 µg/ml). Compounds T (IC = 54.01 µg/ml) was the most potent urease inhibitor amongst the synthesized compounds and compared to standard thiourea (IC = 54.25 µg/ml). The most potent anticancer activity was shown by compounds T (IC = 3.84 μM) and T (IC = 3.25 μM) against HCT116 cell lines as compared to standard 5-FU (IC = 25.36 μM).
三唑是一种重要的杂环部分，由于其具有大量的生物活性，在杂环化学中占据独特的地位。它以两种异构体形式存在，即1,2,4 - 三唑和1,2,3 - 三唑，并用作许多药用化合物设计和合成的核心分子。1,2,4 - 三唑具有广泛的具有治疗意义的候选药物，如止痛剂、防腐剂、抗菌剂、抗氧化剂、抗脲酶剂、抗炎剂、利尿剂、抗癌剂、抗惊厥剂、抗糖尿病剂和抗偏头痛剂。
所有合成化合物的结构通过物理化学性质和光谱手段（红外光谱和核磁共振）进行表征。使用环丙沙星、阿莫西林和氟康唑作为标准品，通过试管稀释法对合成化合物针对革兰氏阳性菌（枯草芽孢杆菌）、革兰氏阴性菌（铜绿假单胞菌和大肠杆菌）以及真菌（白色念珠菌和黑曲霉）菌株进行体外抗菌活性评估。体外抗氧化和抗脲酶筛选分别通过DPPH法和吲哚酚法进行。使用5 - 氟尿嘧啶作为标准品，对MCF - 7和HCT116癌细胞系进行体外抗癌评估。
结果、讨论与结论：生物筛选结果表明，化合物T（MIC = 24.7 μM，MIC = 12.3 μM）和T（MIC = 27.1 μM）分别表现出与标准品环丙沙星、阿莫西林（MIC = 18.1 μM，MIC = 17.1 μM）和氟康唑（MIC = 20.4 μM）相当的强效抗菌活性。抗氧化评估显示，化合物T（IC = 34.83 μg/ml）和T（IC = 34.38 μg/ml）表现出显著的抗氧化活性，与抗坏血酸（IC = 35.44 μg/ml）相当。化合物T（IC = 54.01 μg/ml）是合成化合物中最有效的脲酶抑制剂，与标准品硫脲（IC = 54.25 μg/ml）相当。与标准品5 - 氟尿嘧啶（IC = 25.36 μM）相比，化合物T（IC = 3.84 μM）和T（IC = 3.25 μM）对HCT116细胞系表现出最有效的抗癌活性。
