Download Antiviral Drug Strategies (Methods and Principles in by Erik De Clercq PDF

By Erik De Clercq

ISBN-10: 3527326960

ISBN-13: 9783527326969

By means of concentrating on common molecular mechanisms of antiviral medications instead of cures for person viruses, this prepared reference offers the serious wisdom had to strengthen fullyyt novel therapeutics and to focus on new viruses.It starts off with a common dialogue of antiviral ideas, by means of a vast survey of recognized viral objectives, corresponding to opposite transcriptases, proteases, neuraminidases, RNA polymerases, helicases and primases, in addition to their identified inhibitors. the ultimate part comprises numerous situations stories of modern profitable antiviral drug development.Edited by way of Erik de Clercq, the area authority on small molecule antiviral medications, who has constructed extra new antivirals than somebody else.

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The farthest developed in the clinic (phase II) is a nonimmunosuppressive derivative of cyclosporin A, Debio-025 (structure as shown in Ref. [106]), a cyclophilin binding agent that has potent activity against both HCV [107] and HIV-1 [108]. Debio-025 has shown potent anti-HCV activity in patients coinfected with HCV and HIV-1 [109]. For the treatment of poliovirus, and other enterovirus, and rhinovirus infections, a large variety of antipicornavirus agents have been described [106], the last in the series being a protein 3A inhibitor, TTP-8307 [110].

De Clercq, E. (1980) Antiviral and antitumor activities of 5-substituted 20 - References 40 41 42 43 44 45 46 47 deoxyuridines. Methods and Findings in Experimental and Clinical Pharmacology, 2, 253–267. T. (1979) (E)-5-(2-Bromovinyl)-20 deoxyuridine: a potent and selective antiherpes agent. Proceedings of the National Academy of Sciences of the United States of America, 76, 2947–2951. De Clercq, E. (2004) Discovery and development of BVDU (brivudin) as a therapeutic for the treatment of herpes zoster.

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].

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