Department of Chemistry, Kurukshetra University, Kurukshetra-136 119, Haryana, India.
Eur J Med Chem. 2010 Jun;45(6):2650-5. doi: 10.1016/j.ejmech.2010.01.059. Epub 2010 Jan 29.
A new series of pyrazolylpyrazolines (5a-k) was synthesized by the reaction of appropriate chalcones (3a-k) with 4-hydrazinobenzenesulfonamide hydrochloride (4) in ethanol. All the newly synthesized target compounds (5a-k) were screened for their anti-inflammatory activity using carrageenan-induced rat paw edema assay. Compounds 5g and 5j showed pronounced anti-inflammatory activity comparable to the reference standard nimesulide, whereas, compounds 5b, 5d and 5h displayed good anti-inflammatory activity. Additionally, the synthesized compounds were evaluated for their in vitro antimicrobial activity against two Gram-positive bacteria and two Gram-negative bacteria. Four compounds 5c, 5h-5j showed good broad spectrum activity against all the tested Gram-positive and Gram-negative bacterial strains. Compound 5j could be identified as the most biologically active member within this study with an interesting dual anti-inflammatory and antibacterial profile.
通过将适当的查耳酮(3a-k)与 4-肼苯磺酰胺盐酸盐(4)在乙醇中反应,合成了一系列新的吡唑并吡唑啉(5a-k)。所有新合成的目标化合物(5a-k)都通过角叉菜胶诱导的大鼠足肿胀试验进行了抗炎活性筛选。化合物 5g 和 5j 表现出明显的抗炎活性,可与参比标准尼美舒利相媲美,而化合物 5b、5d 和 5h 则表现出良好的抗炎活性。此外,还评估了合成化合物对两种革兰氏阳性菌和两种革兰氏阴性菌的体外抗菌活性。四种化合物 5c、5h-5j 对所有测试的革兰氏阳性和革兰氏阴性菌均表现出良好的广谱活性。化合物 5j 可以被确定为该研究中最具生物活性的成员,具有有趣的抗炎和抗菌双重特性。