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03360nam a22004695i 4500 |
| 003 - CONTROL NUMBER IDENTIFIER |
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OSt |
| 005 - DATE AND TIME OF LATEST TRANSACTION |
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| control field |
20140310153335.0 |
| 007 - PHYSICAL DESCRIPTION FIXED FIELD--GENERAL INFORMATION |
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cr nn 008mamaa |
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131007s2013 ja | s |||| 0|eng d |
| 020 ## - INTERNATIONAL STANDARD BOOK NUMBER |
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| International Standard Book Number |
9784431544456 |
|
978-4-431-54445-6 |
| 050 #4 - LIBRARY OF CONGRESS CALL NUMBER |
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| Classification number |
QD415-436 |
| 082 04 - DEWEY DECIMAL CLASSIFICATION NUMBER |
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| Classification number |
547 |
| Edition number |
23 |
| 264 #1 - |
|---|
| -- |
Tokyo : |
| -- |
Springer Japan : |
| -- |
Imprint: Springer, |
| -- |
2013. |
| 912 ## - |
|---|
| -- |
ZDB-2-CMS |
| 100 1# - MAIN ENTRY--PERSONAL NAME |
|---|
| Personal name |
Mizuhara, Tsukasa. |
| Relator term |
author. |
| 245 10 - IMMEDIATE SOURCE OF ACQUISITION NOTE |
|---|
| Title |
Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives |
| Medium |
[electronic resource] / |
| Statement of responsibility, etc |
by Tsukasa Mizuhara. |
| 300 ## - PHYSICAL DESCRIPTION |
|---|
| Extent |
XI, 151 p. 98 illus., 3 illus. in color. |
| Other physical details |
online resource. |
| 440 1# - SERIES STATEMENT/ADDED ENTRY--TITLE |
|---|
| Title |
Springer Theses, Recognizing Outstanding Ph.D. Research, |
| International Standard Serial Number |
2190-5053 |
| 505 0# - FORMATTED CONTENTS NOTE |
|---|
| Formatted contents note |
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 ## - SUMMARY, ETC. |
|---|
| Summary, etc |
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 - SUBJECT ADDED ENTRY--TOPICAL TERM |
|---|
| Topical term or geographic name as entry element |
Chemistry. |
|
|---|
| Topical term or geographic name as entry element |
Pharmaceutical technology. |
|
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| Topical term or geographic name as entry element |
Medical virology. |
|
|---|
| Topical term or geographic name as entry element |
Chemistry, Organic. |
|
|---|
| Topical term or geographic name as entry element |
Biochemistry. |
|
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| Topical term or geographic name as entry element |
Chemistry. |
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| Topical term or geographic name as entry element |
Organic Chemistry. |
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|---|
| Topical term or geographic name as entry element |
Pharmaceutical Sciences/Technology. |
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| Topical term or geographic name as entry element |
Medicinal Chemistry. |
|
|---|
| Topical term or geographic name as entry element |
Virology. |
| 710 2# - ADDED ENTRY--CORPORATE NAME |
|---|
| Corporate name or jurisdiction name as entry element |
SpringerLink (Online service) |
| 773 0# - HOST ITEM ENTRY |
|---|
| Title |
Springer eBooks |
| 776 08 - ADDITIONAL PHYSICAL FORM ENTRY |
|---|
| Display text |
Printed edition: |
| International Standard Book Number |
9784431544449 |
| 856 40 - ELECTRONIC LOCATION AND ACCESS |
|---|
| Uniform Resource Identifier |
http://dx.doi.org/10.1007/978-4-431-54445-6 |
| 942 ## - ADDED ENTRY ELEMENTS (KOHA) |
|---|
| Source of classification or shelving scheme |
|
| Item type |
E-Book |
