Thiosemicarbazone and Thiazolylhydrazones of 1-indanone: as a New Class of Nonacidic Anti-inflammatory and Antiplatelet Aggregation Agents. | [Pakistan Journal of Pharmaceutical Sciences • 2019]

Author(s):

1. Urooj Nazim: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan

2. Mansoor Ahmed: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan

3. Basharat Ali: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan

4. Khalid Mohammed Khan: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan

5. Mohsin Ali: Department of Chemistry, Faculty of Science, University of Karachi, Karachi, Pakistan

6. Farzad Kobarfard: Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences; Phytochemistry Research Centre, Shahid Beheshti University of Medical Sciences; Vali Asr Ave. Niayesh Junction,Tehran, Iran

7. S Abdul Majid Ayatollahi: Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences; Phytochemistry Research Centre, Shahid Beheshti University of Medical Sciences; Vali Asr Ave. Niayesh Junction,Tehran, Iran

8. Amir Hassan: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan

9. Almas Jabeen: Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan

10. Ayesha Faheem: Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan

11. Arshia: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan

Abstract:

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 IC50 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, whereas, aspirin (IC50 = 30.3±2.6 µM) was used as standard. However, compound 11 was found to be good active for both antiinflammatory and antiplatelet aggregation activities (IC50 = 13.9±4.9µg/mL) (IC50 = 38.60±3.1µM),, respectively.

Page(s): 15-19

DOI: DOI not available

Published: Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 32, Issue: 1, Year: 2019

Keywords:

thiosemicarbazone , 1Indanone , thiazole , Antiinflammatory , antiplatelet aggregation

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