Synthesis and antifungal activity of novel 7- O -substituted pyridyl-4-methyl coumarin derivatives
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Med Chem Res DOI 10.1007/s00044-013-0470-2
ORIGINAL RESEARCH
Synthesis and antifungal activity of novel 7-O-substituted pyridyl-4-methyl coumarin derivatives Xiaoyun Chai • Shichong Yu • Xiaoyan Wang Nan Wang • Zhanzhou Zhu • Dazhi Zhang • Qiuye Wu • Yongbing Cao • Qingyan Sun
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Received: 3 September 2012 / Accepted: 3 January 2013 Ó Springer Science+Business Media New York 2013
Abstract A new series of 7-O-substituted pyridyl-4methyl coumarin derivatives were synthesized and characterized based on their spectral data. All the target compounds were evaluated for their in vitro antifungal activity against eight important fungal pathogens. This study showed that the introduction of the substituted pyridyl moiety at the 7-hydroxy position of coumarin could enhance the antifungal activities. It also indicated that a bulky substituent was not beneficial to the antifungal activity of those coumarin derivatives. Keywords Coumarin derivatives Synthesis Antifungal activity Pechmann reaction
Xiaoyun Chai and Shichong Yu contributed equally to this study. X. Chai S. Yu D. Zhang Q. Wu Q. Sun (&) Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai 200433, People’s Republic of China e-mail: [email protected] X. Wang Center for Laboratory Teaching, School of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai 200433, People’s Republic of China N. Wang Z. Zhu Pharmacy Team, Administrative Brigade of Postgraduate, Second Military Medical University, Zhengtong Road 41, Shanghai 200433, People’s Republic of China Y. Cao Drug Research Center, School of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai 200433, People’s Republic of China
Introduction Fungi are widely distributed in nature and frequently appear as pathogens in the animal and plant kingdoms. In recent decades, the incidence of systemic fungal infections has been increasing dramatically due to an increasing number of immunocompromised hosts, such as patients undergoing organ transplants or anticancer chemotherapy and patients with AIDS (Fridkin and Jarvis, 1996; Wingard and Leather, 2004). However, resistance to a number of antifungal agents among a variety of clinically significant species of fungi is becoming an increasingly major global problem and is reaching an alarming level on a global scale. These issues pose a serious challenge to the scientific community, and hence emphasis has been laid on the development of new antifungal agents, including natural compounds (Jeu et al., 2003; Lepesheva et al., 2006). A large number of naturally occurring compounds appear as interesting sources for antifungal compounds and are also considered a valuable source of knowledge for the discovery of new antifungal drugs. Among them, coumarins and their derivatives have gained great therapeutic importance in the field of medicinal chemistry because they display a fascinating array of pharmacological properties, such as antibacterial (Chopra et al., 2008), antifung
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