Download e-book for iPad: Antiviral Drug Strategies (Methods and Principles in by Erik De Clercq

By Erik De Clercq

ISBN-10: 3527326960

ISBN-13: 9783527326969

Through concentrating on normal molecular mechanisms of antiviral medications instead of remedies for person viruses, this prepared reference presents the severe wisdom had to boost totally novel therapeutics and to focus on new viruses.It starts off with a common dialogue of antiviral techniques, by way of a huge survey of recognized viral ambitions, corresponding to opposite transcriptases, proteases, neuraminidases, RNA polymerases, helicases and primases, in addition to their recognized inhibitors. the ultimate part includes a number of instances reports of modern winning antiviral drug development.Edited by means of Erik de Clercq, the area authority on small molecule antiviral medicines, who has built extra new antivirals than a person else.

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Extra resources for Antiviral Drug Strategies (Methods and Principles in Medicinal Chemistry, Volume 50)

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2, NRTIs), which through the absence of a 30 hydroxyl group inevitably act as chain terminators at the reverse transcriptase level. 2 Pharmacophores in antiretrovirus agents. 5 Antiviral Drugs Active against Retroviruses (HIV) FTC) [57, 58], correspond to the (À)- or L-enantiomeric form (whereas the first four have the natural D-form). NtRTIs should be clearly distinguished from the NRTIs as they contain a phosphonate group P C O that is isosteric with the phosphate group O P O C of the normal nucleotides.

004 mM in the HCV (genotype 1b) replicon system. GS327073 is based upon the 5-[(4-bromophenyl)methyl]-2-phenyl-5H-imidazo[4,5-c] pyridine BPIP skeleton, which was akin to VP 32947 [33] first identified as a potent j15 j 1 Outlook of the Antiviral Drug Era 16 and selective inhibitor of the replication of pestiviruses such as BVDV [100]. BPIP was from the start recognized as an inhibitor of RdRp, the “finger” domain of the enzyme being its target. Further chemical modifications of the BPIP skeleton led to the identification of GS-327073 as a potent and selective NNRRI of the HCV RdRp, again with the “finger” domain being the target site [101].

In fact, some of the first attempts to block virus replication in vitro and in vivo aimed at blocking virus entry by targeting virus interaction with its principal cellular receptor CD4. It was not until 2003 when enfuvirtide (T-20, FuzeonÒ ) and later, in 2005, maraviroc (SelzentryÒ ), a coreceptor inhibitor, were approved by the US Food and Drug Administration (FDA), thus becoming the firsts of their class. Human Antiviral Drug Strategies, First Edition. Edited by Erik De Clercq. Ó 2011 Wiley-VCH Verlag GmbH & Co.

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Antiviral Drug Strategies (Methods and Principles in Medicinal Chemistry, Volume 50) by Erik De Clercq


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