The Resource Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives, by Tsukasa Mizuhara, (electronic resource)

Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives, by Tsukasa Mizuhara, (electronic resource)

Label
Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives
Title
Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives
Statement of responsibility
by Tsukasa Mizuhara
Creator
Contributor
Author
Provider
Subject
Language
eng
Summary
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
Member of
http://library.link/vocab/creatorName
Mizuhara, Tsukasa
Image bit depth
0
LC call number
QD415-436
Literary form
non fiction
http://library.link/vocab/relatedWorkOrContributorName
SpringerLink
Series statement
Springer Theses, Recognizing Outstanding Ph.D. Research,
http://library.link/vocab/subjectName
  • Chemistry
  • Pharmaceutical technology
  • Medical virology
  • Chemistry, Organic
  • Biochemistry
  • Chemistry
  • Organic Chemistry
  • Pharmaceutical Sciences/Technology
  • Medicinal Chemistry
  • Virology
Label
Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives, by Tsukasa Mizuhara, (electronic resource)
Instantiates
Publication
Antecedent source
mixed
Carrier category
online resource
Carrier category code
cr
Carrier MARC source
rdacarrier
Color
not applicable
Content category
text
Content type code
txt
Content type MARC source
rdacontent
Contents
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
Dimensions
unknown
Extent
XI, 151 p. 98 illus., 3 illus. in color.
File format
multiple file formats
Form of item
electronic
Isbn
9784431544456
Level of compression
uncompressed
Media category
computer
Media MARC source
rdamedia
Media type code
c
Other control number
10.1007/978-4-431-54445-6
Other physical details
online resource.
Quality assurance targets
absent
Reformatting quality
access
Specific material designation
remote
System control number
(DE-He213)978-4-431-54445-6
Label
Development of Novel Anti-HIV Pyrimidobenzothiazine Derivatives, by Tsukasa Mizuhara, (electronic resource)
Publication
Antecedent source
mixed
Carrier category
online resource
Carrier category code
cr
Carrier MARC source
rdacarrier
Color
not applicable
Content category
text
Content type code
txt
Content type MARC source
rdacontent
Contents
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
Dimensions
unknown
Extent
XI, 151 p. 98 illus., 3 illus. in color.
File format
multiple file formats
Form of item
electronic
Isbn
9784431544456
Level of compression
uncompressed
Media category
computer
Media MARC source
rdamedia
Media type code
c
Other control number
10.1007/978-4-431-54445-6
Other physical details
online resource.
Quality assurance targets
absent
Reformatting quality
access
Specific material designation
remote
System control number
(DE-He213)978-4-431-54445-6

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