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Multi-Component One-Pot Assisted Synthesis, Anti-bacterial Capabilities, and Scanning Electron Microscopy of Novel Corticosteroid Thiopyran
Current Organic Synthesis ( IF 1.7 ) Pub Date : 2021-05-31 , DOI: 10.2174/1570179417666201218164112
Sultanat 1 , Anam Ansari 1 , Mohd Qamar 1 , Shafiullah 1 , Sartaj Tabassum 1 , Firoz A Ansari 2
Affiliation  

Background: Corticosteroids are an important group of polycyclic compounds having a wide range of pharmacological and physiological properties. Thiopyran derivatives are important building blocks of many biologically active compounds.

Objective: Keeping in mind the wide range of applications of corticosteroids and thiopyran, herein we intend to develop a simple and efficient strategy to synthesize steroidal thiopyran derivatives starting with different commercially available corticosteroids and study their biological properties.

Materials and Methods: To achieve our aim, we employed a one-pot multi-component synthesis of steroidal thiopyran derivatives by the reaction of corticosteroids, malononitrile, and carbon disulphide in the presence of triethylamine as a catalyst.

Results and Discussion: An array of novel thiopyran compounds was obtained with the highest product yield using Et3N. Scanning electron microscopy analysis manifested agglomeration pertaining to brick-shaped crystals of corticosteroid thiopyran. Synthesized compounds were also found to be active as anti-bacterial agents.

Conclusion: We describe a facile one-pot multi-component synthesis of corticosteroid thiopyran derivatives, which are found to possess anti-bacterial activity. Excellent yields of the products, simple work-up, easily available starting materials, and non-chromatographic purification are some of the main advantages of this protocol.



中文翻译:

新型皮质类固醇硫吡喃的多组分一锅辅助合成、抗菌能力和扫描电子显微镜

背景:皮质类固醇是一组重要的多环化合物,具有广泛的药理和生理特性。硫吡喃衍生物是许多生物活性化合物的重要组成部分。

目的:考虑到皮质类固醇和噻喃的广泛应用,我们打算开发一种简单有效的策略,以不同的市售皮质类固醇为原料合成甾体噻喃衍生物并研究其生物学特性。

材料和方法:为了实现我们的目标,我们通过皮质类固醇、丙二腈和二硫化碳在三乙胺作为催化剂的存在下反应,采用一锅多组分合成甾体噻喃衍生物。

结果和讨论:使用 Et 3 N获得了一系列具有最高产率的新型噻喃化合物。扫描电子显微镜分析表明与皮质类固醇噻喃砖状晶体有关的团聚。还发现合成的化合物具有抗菌活性。

结论:我们描述了一种简便的一锅多组分合成皮质类固醇噻喃衍生物,发现其具有抗菌活性。该协议的一些主要优点是产品产量高、处理简单、起始材料易于获得和非色谱纯化。

更新日期:2021-06-08
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