Nazim Urooj, Ahmed Mansoor, Ali Basharat, Khan Khalid Mohammed, Ali Mohsin, Kobarfard Farzad, Arshia -, Ayatollahi S Abdul-Majid, Hassan Amir, Jabeen Almas, Faheem Ayesha
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan.
HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.
Pak J Pharm Sci. 2019 Jan;32(1):15-19.
This research based on the anti-inflammatory and antiplatelet aggregation properties of some new thiazolyl hydrazone derivatives of 1-indanone. In this regard a thiosemicabazone and twelve thiazolyl derivatives of 1-indanone have been synthesized. Out of these synthetic compounds seven derivatives 1-3, 6, 11-13 exhibited varying degree of anti-inflammatory action with IC esteems going from 5.1±1.3 - 78.8±4.6μM/mL. Compound 1 (IC50 =5.1±1.9μM) displayed potent result than standard ibuprofen (IC50 = 11.2±1.9 μM). In antiplatelet aggregation assay, five compounds 1, 5, 6, 8 and 11 were observed to be dynamic with IC50 esteems observed in the range of 38.34-255.7±4.1μM, wher eas, aspirin (IC = 30.3±2.6 μM) was used as standard. However, compound 11 was found to be good active for both anti-inflammatory and antiplatelet aggregation activities (IC = 13.9±4.9μg/mL) (IC = 38.60±3.1μM), respectively.
本研究基于1-茚满酮的一些新型噻唑基腙衍生物的抗炎和抗血小板聚集特性。在此方面，已合成了一种硫代半卡巴腙和1-茚满酮的十二种噻唑基衍生物。在这些合成化合物中，七种衍生物1-3、6、11-13表现出不同程度的抗炎作用，IC值范围为5.1±1.3 - 78.8±4.6μM/mL。化合物1（IC50 =5.1±1.9μM）显示出比标准布洛芬（IC50 = 11.2±1.9 μM）更强的效果。在抗血小板聚集试验中，观察到五种化合物1、5、6、8和11具有活性，IC50值在38.34 - 255.7±4.1μM范围内，而阿司匹林（IC = 30.3±2.6 μM）用作标准。然而，发现化合物11在抗炎和抗血小板聚集活性方面均具有良好活性（分别为IC = 13.9±4.9μg/mL）（IC = 38.60±3.1μM）。
