Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors

Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors Publisher

Mirfazli SS¹ ; Khoshneviszadeh M² ; Jeiroudi M¹ ; Foroumadi A¹ ; Kobarfard F^{3, 4} ; Shafiee A¹

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1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
2. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
3. Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
4. Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Vali Asr Ave. Niayesh Junction, Tehran, Iran

Source: Medicinal Chemistry Research Published:2016

Abstract

A series of novel substituted indole carbohydrazide was synthesized and evaluated for anti-platelet aggregation activity. The structures of the synthesized compounds were confirmed by spectral data and elemental analysis and were evaluated for their ability to inhibit platelet aggregation induced by adenosine diphosphate, arachidonic acid (AA) and collagen. Compounds 3e and 3b exhibited the highest activities against the platelet aggregation induced by collagen with IC50 values of 12.7 and 13.3 μM, respectively, and 2h with IC50 value of 51.88 μM and 2i with IC50 of 44.38 μM efficiently inhibited platelet aggregation induced by AA. The QSAR investigation indicated the importance of the topological, constitutional and geometrical parameters (PW3, PW4, LP1 and GATS6v) in describing the anti-platelet aggregation activity of the synthesized hydrazides. Evaluation of cytotoxic activity of the compounds against L929 cell line and three cancer cell lines revealed that none of the compounds have significant cytotoxicity. Graphical Abstract: [Figure not available: see fulltext.] © 2015 Springer Science+Business Media New York.

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Massoud Amanlou (1)

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Style	Citing Format
MLA	Mirfazli SS, et al.. "Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors." Medicinal Chemistry Research, vol. 25, no. 1, 2016, pp. 1-18.
APA	Mirfazli SS, Khoshneviszadeh M, Jeiroudi M, Foroumadi A, Kobarfard F, Shafiee A (2016). Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors. Medicinal Chemistry Research, 25(1), 1-18.
Chicago	Mirfazli SS, Khoshneviszadeh M, Jeiroudi M, Foroumadi A, Kobarfard F, Shafiee A. "Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors." Medicinal Chemistry Research 25, no. 1 (2016): 1-18.
Harvard	Mirfazli SS et al. (2016) 'Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors', Medicinal Chemistry Research, 25(1), pp. 1-18.
Vancouver	Mirfazli SS, Khoshneviszadeh M, Jeiroudi M, Foroumadi A, Kobarfard F, Shafiee A. Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors. Medicinal Chemistry Research. 2016;25(1):1-18.
BibTex	@article{ author = {Mirfazli SS and Khoshneviszadeh M and Jeiroudi M and Foroumadi A and Kobarfard F and Shafiee A}, title = {Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors}, journal = {Medicinal Chemistry Research}, volume = {25}, number = {1}, pages = {1-18}, year = {2016} }
RIS	TY - JOUR AU - Mirfazli SS AU - Khoshneviszadeh M AU - Jeiroudi M AU - Foroumadi A AU - Kobarfard F AU - Shafiee A TI - Design, Synthesis and Qsar Study of Arylidene Indoles As Anti-Platelet Aggregation Inhibitors JO - Medicinal Chemistry Research VL - 25 IS - 1 SP - 1 EP - 18 PY - 2016 ER -

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