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Bücher Englische Bücher Wissen & Bildung Naturwissenschaft, Medizin, Informatik, Technik Chemie Organische Chemie Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives
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Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives
Tsukasa Mizuhara (Gebundene Ausgabe, Englisch)
Optischer Zustand
Beschreibung
The author successfully developed novel anti-HIV PD 404182 derivatives that exhibited submicromolar inhibitory activity against both HIV-1 and HIV-2. His thesis is in three parts. The first part expounds efficient methods for the synthesis of tricyclic heterocycles related to PD 404182 based on the sp 2 -carbon−heteroatom bond formations. Starting from arene or haloarene, C-O, C-N, or C-S bonds… were formed by simply changing the reactants. These synthetic methods provide powerful approaches for the divergent preparation of pyrimido-benzoxazine, -quinazoline, or -benzothiazine derivatives. The second part explains SAR studies of PD 404182 for the development of anti-HIV agents. Through optimization studies of the central 1,3-thiazin-2-imine core, the benzene and cyclic amidine ring parts, 3-fold more potent inhibitors were obtained compared with the lead compound. The author also reveals by a time-of-drug-addition experiment that PD 404182 derivatives impaired HIV replication at the binding or fusion stage. The third part of the thesis elucidates the development of photoaffinity probes for the target identification of PD 404182. By the photolabeling experiment of HIV-1-infected H9 cells using these probes, the author detected proteins specifically bound to PD 404182. These new anti-HIV agents may be promising agents for anti-HIV therapy because their mechanisms of action differ from those of the currently approved anti-HIV agents. Dieses Produkt haben wir gerade leider nicht auf Lager.
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Technische Daten
Erscheinungsdatum
17.10.2013
Sprache
Englisch
EAN
9784431544449
Herausgeber
Springer Tokyo
Serien- oder Bandtitel
Springer Theses
Sonderedition
Nein
Autor
Tsukasa Mizuhara
Seitenanzahl
151
Einbandart
Gebundene Ausgabe
Autorenporträt
Department of ChemistryUniversity of Massachusetts Amherst, USAPh. D. in Pharmaceutical Sciences Graduate School of Pharmaceutical Sciences, Kyoto University, Japan
Schlagwörter
Anti-HIV Agents, Aromatic Nucleophilic Substitution, C−H Functionalization, PD 404182, Photoaffinity Labeling, Pyrimidobenzothiazine, Structure−activity Relationship
Thema-Inhalt
PNN - Organische Chemie
PNB - Medizinische Chemie, Pharmazeutische Chemie
PSG - Mikrobiologie (nicht-medizinisch)
Höhe
235 mm
Breite
15.5 cm
Transparenz & Sicherheit
Hersteller: Springer, Europaplatz 3, Heidelberg, Deutschland, 69115, ProductSafety@springernature.com, Springer Nature Customer Service Center GmbH
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