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Synthesis, Characterization and Antimicrobial Activities of 1,4- Disubstituted 1,2,3-Triazole Compounds.
Current Topics in Medicinal Chemistry ( IF 3.4 ) Pub Date : 2020-01-01 , DOI: 10.2174/1568026620666200819143029
Seck Insa 1 , Fall Alioune 1 , Ba Lalla Aicha 2 , Ndoye Samba Fama 3 , Ka Seydou 3 , Diop Abdoulaye 4 , Ciss Ismaïla 3 , Ba Abda 3 , Diop Amadou 4 , Boye Cheikh Sadibou 4 , Gomez Generosa 5 , Fall Yagamare 5 , Seck Matar 3
Affiliation  

BACKGROUND 1,2,3-triazoles are five-membered heterocyclic scaffold; their broad-spectrum biological activities are known. Researchers around the world are increasingly being interested in this emerging area, owing to its immense pharmacological scope. OBJECTIVE This work summarizes the synthesis of 1,2,3-triazoles and the significance of this pattern as a lead structure for new drug molecules discovery. METHODS 1,2,3-triazoles can be obtained on a multigram scale through "click chemistry" under ambient conditions. RESULTS Sixteen compounds were synthesized and evaluated on five microbial strains E. coli, E. faecalis, P. aeruginosa, S. aureus and C. albicans. NMR, MS and IR were used to characterize all compounds. They were evaluated with their Minimum Inhibitory Concentrations (MICs) and interesting results were obtained with compounds 12a, 12b, 3, 2a and 2c, with MIC 0.14 μM (P. aeruginosa), 1.08 μM (E. coli), 1.20 μM (E. faecalis and C. albicans), 3.5 μM (E. faecalis) and 4.24 μM (C. albicans), respectively. P. aeruginosa and C. albicans were the most sensitive among all the strains. CONCLUSION The synthesized compounds were found as potential antimicrobial agents against Gram (+), Gram (-) strains and fungi.

中文翻译:

1,4-二取代的 1,2,3-三唑化合物的合成、表征和抗菌活性。

背景 1,2,3-三唑是五元杂环支架;它们的广谱生物活性是已知的。由于其巨大的药理学范围,世界各地的研究人员对这一新兴领域越来越感兴趣。目的 本工作总结了 1,2,3-三唑的合成以及这种模式作为新药物分子发现的先导结构的重要性。方法 1,2,3-三唑可以在环境条件下通过“点击化学”以多克规模获得。结果 在五种微生物菌株大肠杆菌、粪肠球菌、铜绿假单胞菌、金黄色葡萄球菌和白色念珠菌上合成并评估了 16 种化合物。NMR、MS 和 IR 用于表征所有化合物。对它们的最小抑制浓度 (MIC) 进行了评估,化合物 12a、12b、3、2a 和 2c 获得了有趣的结果,MIC 为 0.14 μM(铜绿假单胞菌)、1.08 μM(大肠杆菌)、1.20 μM(大肠杆菌) . faecalis 和 C. albicans),分别为 3.5 μM(E. faecalis)和 4.24 μM(C. albicans)。铜绿假单胞菌和白色念珠菌是所有菌株中最敏感的。结论 合成的化合物被发现是针对革兰氏 (+)、革兰氏 (-) 菌株和真菌的潜在抗菌剂。
更新日期:2020-08-19
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