Antiviral compounds coumarins

Several reviews have been published dealing with natural products-derived antiviral compounds [11,12,16-23]. Presently, there are only two plant-derived compounds under clinical development [2]. (+)-Calanolide A (12) is a C22 coumarin isolated from the Malaysian rainforest tree, Calophyllum langigerum by the U.S. National Cancer Institute [2]. It shows a potent HIV-RT inhibitory activity [2]. In vitro studies of 12 demonstrated activity against HIV-1 including AZT and other nonnucleoside RT inhibitors-resistant strains. It also shows synergistic anti-HIV activity in combination with nucleoside RT inhibitors 7, 8 and 9 [2]. To overcome the difficulty of supply of 12, its total chemical synthesis was accomplished [2]. In June 1997, clinical development of 12 was started as a potential drug for treatment of AIDS. A single -center 7-month U.S. phase la clinical trial of 12 was started to assess its safety and... 

Mass screening of our compound collection, utilizing the Amersham SPA technology, afforded pyrone and coumarin non-peptide templates as initial lead structures. X-ray cocrystallization and structure-based design were utilized to assist in the design of more potent inhibitors. These efforts resulted in the design of the 5,6-dihydropyrones, which afforded a more flexible template from which to fill the internal pockets of the enzyme. Optimization of the dihydropyrone series afforded a potent antiviral agent,... 

These include the SSA-catalyzed synthesis of heterocyclic compounds such as xanthenes, coumarins, oxazoles, and so on. Xanthenes are of great therapeutic and biological interest on account of their many biological activities such as anti-inflanunatory, antiviral, antibacterial properties, and so on. Seyyed Hamzeh et al. (2008) carried out the SSA-catalyzed synthesis of aryl-14 f-dibenzo[fl,y]xanthenes from aldehydes and P-naphthol and 1,8-dioxo-octahydro-xanthenes from aldehydes and 1,3-dicarbonyl componnd such as dimedone under solvent-free conditions (Schemes 5.25, 5.26). Reactions were carried out at 80°C. Nazeruddin et al. (2011) documented an effective method for 9,10-dihydro-12-aryl-8 f-benzo[a]xanthenes-ll(12 f)-one derivatives in excellent yield and short reaction time using SSA under solvent-free conditions (Scheme 5.27). 

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