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Balzarini J, Celen S, Karlsson A, de Groot T, Verbruggen A, Bormans G., The effect of a methyl or 2-fluoroethyl substituent at the N-3 position of thymidine, 3'-fluoro-3'-deoxythymidine and 1-beta-D-arabinosylthymine on their antiviral and cytostatic activity in cell culture, Antivir Chem
Chemother.
240:, 3'-fluoro-3'-deoxythymidine (FLT) and 3'-fluorodideoxyguanosine (FLG), and the NNRTI's 1--6-phenylthiothymine (HEPT), tetrahydro-imidazo-benzodiazepine-2(1H)-one and -thione (TIBO) and alpha-anilinophenylacetamide (alpha-APA) were first described at the Rega Institute. The anti-viral drugs
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Rudi
Pauwels, Koen Andries, Jan Desmyter, Dominique Schols, Michael J. Kukla, Henry J. Breslin, Alfons Raeymaeckers, Jozef Van Gelder, Robert Woestenborghs, Jozef Heykants, Karel Schellekens, Marcel A. C. Janssen, Erik De Clercq, Paul A. J. Janssen, Potent and selective inhibition of HIV-1
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binding site. The NNRTIs block the normal enzymatic activity of the RT and thereby interrupt the replication cycle of HIV. As a result of the "Rega-Janssen" cooperation several prototypes of NNRTIs, among which the so-called TIBO ("TetrahydroImidazoBenzodiazepinOne") and alpha-APA
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De Clercq E., Chemotherapy of the acquired immune deficiency syndrome (AIDS): non-nucleoside inhibitors of the human immunodeficiency virus type 1 reverse transcriptase, Int J Immunopharmacol. 1991;13 Suppl
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De Clercq E., Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection, Farmaco. 1999 Jan-Feb;54(1-2):26-45.
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198:(TMC-278). NNRTIs are at the moment considered one of the essential ingredients of so-called anti-HIV cocktails. The best well-known NNRTIs are
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replication in vitro by a novel series of TIBO derivatives, Nature 343, 470 - 474 (1 February 1990).
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1269:Categories
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541:Since 1968
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210:References
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187:allosteric
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