2-(6-取代喹啉-4-基)-1-烷氧基丙-2-醇作为潜在抗分枝杆菌剂的合成
Synthesis of 2-(6-substituted quinolin-4-yl)-1-alkoxypropan-2-ol as potential antimycobacterial agents.
作者信息
Shinde Abhijit, Thakare Prashant P, Nandurkar Yogesh, Chavan Abhijit, Shaikh Abdul Latif N, Mhaske Pravin C
机构信息
Department of Chemistry, S. P. Mandali's Sir Parashurambhau College (Affiliated to, Savitribai Phule Pune University), Tilak Road, Pune, 411030 India.
Department of Chemistry, N. Wadia College (Affiliated to Savitribai Phule Pune University), Pune, India.
出版信息
Chem Zvesti. 2023;77(7):3791-3802. doi: 10.1007/s11696-023-02741-3. Epub 2023 Feb 25.
UNLABELLED
Resistance to antibiotic drugs has directed global health security to a life-threatening situation due to mycobacterial infections. In search of a new potent antimycobacterial, a series of (±) 2-(6-substituted quinolin-4-yl)-1-alkoxypropan-2-ol () have been synthesized. The structures of the newly synthesized derivatives were characterized by spectrometric analysis. Derivatives were evaluated for antitubercular activity against H37Rv (ATCC 25177), antibacterial activity against (NCIM2388), (NCIM 2065), (NCIM2063) (NCIM 2178) and antifungal activity against (NCIM 3100), (ATCC 504). Thirteen 2-(6-substituted quinolin-4-yl)-1-alkoxypropan-2-ol ( derivatives reported moderate to good antitubercular activity against H37Rv with MIC 9.2-106.4 μM. Compounds and showed comparable activity with respect to the standard drug pyrazinamide. The active compounds screened for cytotoxicity activity against L929 mouse fibroblast cells showed no significant cytotoxic activity. Compounds , , , , , and displayed good activity against . Compounds and showed good activity against and , respectively. The potential antimycobacterial activities imposed that the 2-(6-substituted quinolin-4-yl)-1-alkoxypropan-2-ol derivatives could lead to compounds that could treat tuberculosis.
SUPPLEMENTARY INFORMATION
The online version contains supplementary material available at 10.1007/s11696-023-02741-3.
未标注
由于分枝杆菌感染，对抗生素药物的耐药性已将全球卫生安全导向了危及生命的境地。为寻找新型强效抗分枝杆菌药物，已合成了一系列（±）2-（6-取代喹啉-4-基）-1-烷氧基丙烷-2-醇（）。通过光谱分析对新合成衍生物的结构进行了表征。对衍生物进行了针对结核分枝杆菌H37Rv（ATCC 25177）的抗结核活性、针对（NCIM2388）、（NCIM 2065）、（NCIM2063）、（NCIM 2178）的抗菌活性以及针对（NCIM 3100）、（ATCC 504）的抗真菌活性评估。13种2-（6-取代喹啉-4-基）-1-烷氧基丙烷-2-醇（衍生物对结核分枝杆菌H37Rv表现出中度至良好的抗结核活性，MIC为9.2 - 106.4 μM。化合物和与标准药物吡嗪酰胺表现出相当的活性。筛选出的对L929小鼠成纤维细胞具有细胞毒性活性的活性化合物未显示出显著的细胞毒性活性。化合物、、、、、和对表现出良好活性。化合物和分别对和表现出良好活性。潜在的抗分枝杆菌活性表明2-（6-取代喹啉-4-基）-1-烷氧基丙烷-2-醇衍生物可能会产生可治疗结核病的化合物。
补充信息
在线版本包含可在10.1007/s11696-023-02741-3获取的补充材料。
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