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Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives
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...
| Clasificación: | Libro Electrónico |
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| Autor principal: | |
| Autor Corporativo: | |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Tokyo :
Springer Japan : Imprint: Springer,
2013.
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| Edición: | 1st ed. 2013. |
| Colección: | Springer Theses, Recognizing Outstanding Ph.D. Research,
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| Temas: | |
| Acceso en línea: | Texto Completo |
MARC
| LEADER | 00000nam a22000005i 4500 | ||
|---|---|---|---|
| 001 | 978-4-431-54445-6 | ||
| 003 | DE-He213 | ||
| 005 | 20220117032211.0 | ||
| 007 | cr nn 008mamaa | ||
| 008 | 131007s2013 ja | s |||| 0|eng d | ||
| 020 | |a 9784431544456 |9 978-4-431-54445-6 | ||
| 024 | 7 | |a 10.1007/978-4-431-54445-6 |2 doi | |
| 050 | 4 | |a QD241-441 | |
| 072 | 7 | |a PNN |2 bicssc | |
| 072 | 7 | |a SCI013040 |2 bisacsh | |
| 072 | 7 | |a PNN |2 thema | |
| 082 | 0 | 4 | |a 547 |2 23 |
| 100 | 1 | |a Mizuhara, Tsukasa. |e author. |4 aut |4 http://id.loc.gov/vocabulary/relators/aut | |
| 245 | 1 | 0 | |a Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives |h [electronic resource] / |c by Tsukasa Mizuhara. |
| 250 | |a 1st ed. 2013. | ||
| 264 | 1 | |a Tokyo : |b Springer Japan : |b Imprint: Springer, |c 2013. | |
| 300 | |a XI, 151 p. 98 illus., 3 illus. in color. |b online resource. | ||
| 336 | |a text |b txt |2 rdacontent | ||
| 337 | |a computer |b c |2 rdamedia | ||
| 338 | |a online resource |b cr |2 rdacarrier | ||
| 347 | |a text file |b PDF |2 rda | ||
| 490 | 1 | |a Springer Theses, Recognizing Outstanding Ph.D. Research, |x 2190-5061 | |
| 505 | 0 | |a Introduction -- Development of Divergent Synthetic Methods of Pyrimidobenzothiazine and Related Tricyclic Heterocycles -- Structure-Activity Relationship Study of PD 404182 Derivatives for the Highly Potent Anti-HIV Agents.- Design and Synthesis of Photoaffinity Probes and Their Application to Target Identification Study of PD 404182 -- Conclusion. | |
| 520 | |a 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 sp2-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. | ||
| 650 | 0 | |a Chemistry, Organic. | |
| 650 | 0 | |a Pharmaceutical chemistry. | |
| 650 | 0 | |a Medicinal chemistry. | |
| 650 | 0 | |a Virology. | |
| 650 | 1 | 4 | |a Organic Chemistry. |
| 650 | 2 | 4 | |a Pharmaceutics. |
| 650 | 2 | 4 | |a Medicinal Chemistry. |
| 650 | 2 | 4 | |a Virology. |
| 710 | 2 | |a SpringerLink (Online service) | |
| 773 | 0 | |t Springer Nature eBook | |
| 776 | 0 | 8 | |i Printed edition: |z 9784431544463 |
| 776 | 0 | 8 | |i Printed edition: |z 9784431544449 |
| 776 | 0 | 8 | |i Printed edition: |z 9784431561651 |
| 830 | 0 | |a Springer Theses, Recognizing Outstanding Ph.D. Research, |x 2190-5061 | |
| 856 | 4 | 0 | |u https://doi.uam.elogim.com/10.1007/978-4-431-54445-6 |z Texto Completo |
| 912 | |a ZDB-2-CMS | ||
| 912 | |a ZDB-2-SXC | ||
| 950 | |a Chemistry and Materials Science (SpringerNature-11644) | ||
| 950 | |a Chemistry and Material Science (R0) (SpringerNature-43709) | ||