Synthesis and Anti-platelet Activity of 3-phenyl-4(1H)-quinolones

DOI:

https://doi.org/10.37285/ijpsn.2010.3.1.12

Authors

  • Achaiah Garlapati
  • Aruna G
  • Saritha Jyostna T

Abstract

A series of substituted 3-phenyl-4(1H)-quinolones and their 4-alkoxy derivatives have been prepared and evaluated for antiplatelet activity. Among the series compound IVb1 with 5-ethyl substituent and 4-methoxy group showed greater potency (IC50 = 13.29 µM) when compared to Aspirin (IC50 = 28.10 µM).

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Published

2010-05-31

How to Cite

1.
Garlapati A, G A, T SJ. Synthesis and Anti-platelet Activity of 3-phenyl-4(1H)-quinolones. Scopus Indexed [Internet]. 2010 May 31 [cited 2024 Dec. 21];3(1):877-80. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/480

Issue

Section

Research Articles

References

Chemistry (ITCHMC2005) Modena Italy, ARKIVOC.200, 1. Sep 12–1 (2005).

Covic L, Gresser AL, Kuliopulos A. Biphasic kinetic of activation and signaling for PAR1 and PAR4 thrombin receptors in platelets. Biochemistry. 39: 5458-567 (2000).

Eriksson AC, Whiss PA. Measurement of adhesion of human platelets in plasma to protein surfaces in microplates. Pharmacol. Toxicol. 52: 356-365 (2005).

Fujioka T, Teramoto S, Mori T, Hosokawa T, Sumida T, Tominaga M, Yabuuchi Y. Novel positive inotropic agents : Synthesis and biological activity of 6-(3-amino-2-hydroxypropoxy)-2(1H0-quinoline derivatives. J. Med. Chem., 35: 3607-3612 (1992).

Huang W, Zhang P, Zuckett JF, Wang L, Woolfrey J, Song Y, Jia, ZJ’ Clizbe L A, Su T, Tran K, Huang B, Wong P, Sinha U, Park G, Reed A, Malinowski J, Hollenbach SJ, Scarborough RM, Zhu BY. “Design, Synthesis and Structure-Activity Relationships of Benzoxazinone-Based Factor Xa Inhibitors” Bioorg. Med. Chem. Lett. 13: 561-586 (2003).

Jakobsen P, Ritsmar Pedersen B, Persson E. Inhibitors of the tissue factor/factor VIIa-induced coagulation: synthesis and in vitro evaluation of novel specific 2-aryl substituted 4H-3,1-benzoxazin-4-ones. Bioorg. Med. Chem. 8: 2095-2103 (2000).

Li-Jiau Huang, Ming-Chieh Hsieh, Che-Ming Teng, Kuo-Hsiung Lee and Sheng-Chu Kuo. Synthesis and antiplatelet activity of phenyl quinolones. Bioorg. Med. Chem. 10: 1657-1662 (1998).

O’ Brien JR. Some effects of Adrenaline anti-adrenaline compounds on platelets in-vitro and in-vivo. Nature. 200: 763-764 (1963).

Ruggeri ZM. Platelets in aterothrombosis. Nat. Med. 8: 1227-1234 (2002).

Tominaga M, Ogawa H, Yo E, Yamashita S, Yabuuchi Y, Nakagawa K. Studies on positive inotropic agents.IV. Synthesis of 5-(3-amino-2-hydroxypropoxy)-3,4-dihydro-8-hydroxy-2(1H)-quinolinederivatives. Chem. Pharm. Bull., 35: 3699-3704 (1987).

Tominaga M, Yo E, Ogawa H, Yamashita S, Yabuuchi Y, Nakagawa K. Synthesis of 3,4-dihydro-6-[4-(3,4-dimethoxybenzoyl)-1-piperizinyl]-2(1H)-quinolone and related compounds. Chem. Pharm. Bull., 32: 2100-2110 (1984).

Tzeng CC, Chen IL, Chen YL, Wang TC, Chang YL, Teng CM. synthesis and Cytototoxic activities of –Methylidene-r-butyrolactones Bearing a Quinolin-4(1H)-one moiety. Helv. Chim. Acta., 83: 349- (2000).