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5-(3-氯苯基)-2-((N-(取代)-2-乙酰基硫基)-1,3,4-恶二唑衍生物的合成、表征、抗菌、溶血和溶栓活性评价。

Synthesis, characterization, antibacterial, hemolytic and thrombolytic activity evaluation of 5-(3-chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives.

机构信息

Department of Chemistry, Government College University, Lahore, Pakistan.

Department of Chemistry, Government College University, Faisalabad, Pakistan.

出版信息

Pak J Pharm Sci. 2020 Mar;33(2(Supplementary)):871-876.

Abstract

A novel series of 5-(3-Chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives was efficiently synthesized and screened for antibacterial, hemolytic and thrombolytic activities. The molecule 7c remained the best inhibitor of all selected bacterial strains and furthermore possessed very low toxicity, 8.52±0.31. Compound 7a 7b and 7f showed very good thrombolytic activity relative to Streptokinase employed as reference drug. In addition to low toxicity and moderately good thrombolytic activity, the synthesized compounds possessed excellent to moderate antibacterial activity, relative to ciprofloxacin. All compounds especially 7b and 7f can be consider for further clinical studies and might be helpful in synthesis of new drugs for treatment of cardiovascular diseases.

摘要

一系列新型的 5-(3-氯苯基)-2-((N-(取代)-2-乙酰基硫代)-1,3,4-恶二唑衍生物被高效合成,并对其进行了抗菌、溶血和溶栓活性筛选。分子 7c 仍然是所有选定的细菌菌株的最佳抑制剂,并且具有非常低的毒性,8.52±0.31。化合物 7a、7b 和 7f 与作为参比药物的链激酶相比,表现出非常好的溶栓活性。除了低毒性和中度良好的溶栓活性外,与环丙沙星相比,合成的化合物具有优异至中度的抗菌活性。所有化合物,特别是 7b 和 7f,可以考虑进一步的临床研究,并可能有助于治疗心血管疾病的新药合成。

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