Bihani Manisha, Bora Pranjal P, Bez Ghanashyam, Askari Hassan
Department of Chemistry, North Eastern Hill University, Shillong, 793022, India.
Mol Divers. 2014 Nov;18(4):745-57. doi: 10.1007/s11030-014-9532-8. Epub 2014 Jul 9.
A novel series of unsymmetrically substituted alkyl/benzyl pyrazolyl barbiturates incorporating highly biologically active pyrazolone and barbiturate moieties was synthesized by four-component reactions of a mixture of ethyl acetoacetate, hydrazine hydrate, aldehydes and barbituric acid/thiobarbituric acid in ethanol without using a catalyst. The photophysical properties of the newly designed alkyl/benzyl pyrazolyl barbiturates were studied, and good quantum yield of some products indicated a definitive scope in the field of biochemical applications. Single-crystal X-ray crystallographic studies revealed that the newly synthesized compounds exist in zwitterionic form. The zwitterionic nature of the new chimera makes them interesting candidates for drug delivery as zwitterionic drugs are known to have highly water soluble properties, specific protein absorption, slow recognition by immune system, slow blood clearance from body and can constantly diffuse and deposit throughout the physiological pH.
通过乙酰乙酸乙酯、水合肼、醛与巴比妥酸/硫代巴比妥酸的混合物在乙醇中进行四组分反应,无需使用催化剂,合成了一系列新型的不对称取代烷基/苄基吡唑基巴比妥酸盐,其中包含具有高生物活性的吡唑啉酮和巴比妥酸部分。研究了新设计的烷基/苄基吡唑基巴比妥酸盐的光物理性质,一些产物的良好量子产率表明其在生化应用领域具有明确的应用范围。单晶X射线晶体学研究表明,新合成的化合物以两性离子形式存在。这种新嵌合体的两性离子性质使其成为药物递送的有趣候选物,因为已知两性离子药物具有高度水溶性、特定的蛋白质吸收、免疫系统的缓慢识别、体内血液清除缓慢,并且可以在整个生理pH值下不断扩散和沉积。