Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad, India.
Arch Pharm (Weinheim). 2013 Sep;346(9):645-53. doi: 10.1002/ardp.201300118. Epub 2013 Aug 1.
A novel series of Biginelli 2-3 (a and b) and Biginelli-like compounds 4-7 (a and b) were synthesized from 3-aryl-4-formylsydnone 1 (a and b). Since the crystal structure of hyaluronidase was unavailable, the human hyaluronidase protein structure was used as template and homology modeling was performed, validated by Ramachandran plots and subjected to docking studies along with in vitro anti-inflammatory activity assessment against hyaluronidase. Compounds 2-3 (a and b) exhibited potent enzyme inhibition.
新型系列比格利尼 2-3（a 和 b）和比格利尼类似物 4-7（a 和 b）由 3-芳基-4-甲酰基-2-吡咯啉 1（a 和 b）合成。由于透明质酸酶的晶体结构不可用，因此使用人透明质酸酶蛋白结构作为模板进行同源建模，通过 Ramachandran 图谱进行验证，并与体外透明质酸酶抗炎活性评估一起进行对接研究。化合物 2-3（a 和 b）表现出较强的酶抑制作用。
