Anti-influenza drug

Anti-Influenza Drugs The Development of Sialidase Inhibitors... 

The Discovery of Zanamivir, the First Potent Designer Anti-Influenza Drug.. 119... 

An overview of the role of the virus-associated glycoprotein sialidase (neuraminidase) and some of the most recent developments towards the discovery of anti-influenza drugs based on the inhibition of influenza virus sialidase is provided in this chapter. 

As a result of the emergence of the extremely aggressive avian H5N1 influenza virus, the likelihood of a human influenza pandemic and the possible socioeconomic impact is now of major concern. In the absence of strain-independent anti-influenza drugs, there has been significant effort worldwide over the years in the quest for the discovery of novel therapeutic agents against all types of influenza. 

The development of sialidase-based inhibitors as anti-influenza drugs has provided a first line-of-defence to safeguard humanity against a potential pandemic and most importantly to buy time for vaccine and further anti-influenza drug development. Most exciting is that new opportunities exist for next generation sialidase inhibitor development. 

Islam T, von Itzstein M (2007) Anti-influenza drug discovery are we ready for the next pandemic Adv Carbohydr Chem Biochem 61 293-352... 

Klumpp K (2004) Recent advances in the discovery and development of anti-influenza drugs. Exp Opin Ther Patents 14 1153-1168... 

This type of analysis is now well established and has been used in many drug discovery projects over the past fifteen years. Examples include HIV protease inhibitors [13], anti-influenza drugs [14], isoform-selective ligands for the estrogen receptor [15], and many more. 

A highly useful and important regioselective reduction of substrate 84 leads to a mixture of 3-hydroxy ethers 85 and 86 in a 32 1 ratio (Eq. 306). Compound 85 is further converted to the anti-influenza drug oseltamivir phosphate, better known as Tamiflu .498... 

Much more interesting, in terms of applications, is the case in which the anomeric oxygen is replaced by a double bound. This is the case of Zanamivir (Fig. 3)2 an anti-influenza drug approved by the US Food... 

Fig. 1.4 Hemagglutination assay results from the active fraction of the red alga Gigartina skottsbergii. a Red blood cells (RBCs) hemagglutinate in the presence of influenza virus top row) and with extract A4 -t- virus or extract A4 alone. The bottom two rows present the back titration of the virus used in this experiment, b In contrast to the other anti-influenza drugs (ribavirin, amantadine, rimantadine, and zanamivir) that do not induce hemagglutination of human as well as chicken RBCs, extract A4 does it in a dose-dependent manner...

Dimethylbiguanide has been said (232) to be analgesic, antipyretic, non-toxic and possibly of value as an anti-influenza drug, but its antipyretic properties have not been confirmed (675) The compound inhibits the course of cowpox, influenza A, pneumonia and measles (676). 

The third major difficulty in developing cold cures arises from the fact that the HRVs are RNA viruses. When presented with any selective pressure, including chemotherapeutic or antibody challenge, RNA viruses mutate rapidly [9]. This ability to mutate is most clearly illustrated in influenza viruses (RNA viruses), where new strains continuously arise to circumvent immunity in a population. Influenza A viruses have been shown to mutate around the anti-influenza drug Amantadine, after a single passage through a susceptible human host. The mutated viruses shed from a host treated with Amantadine are now resistant to Amantadine. These mutated viruses appear to be as virulent as the parent strain of virus [10]. 

Ketamine also shares a close chemical kinship to prescription drugs Tiletamine and Memantine. Tileta-mine is used in combination with zolazepam as a veterinary anesthetic under the brand names Zoletic and Tela-zol. Memantine is derived from the anti-influenza drug amantadine, and also works to block NDMA receptors. Memantine has been approved for use in Parkinson s disease and dementia in the elderly. It is also being used experimentally with AIDS patients for the treatment of HIV encephalopathy. 

ANTI-INFLUENZA DRUG DISCOVERY ARE WE READY FOR THE NEXT PANDEMIC ... 

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