2012 Fiscal Year Final Research Report
Study on betulin and betulinic acid derivatives aimed at developing anti-HIV agents effective against resistant virus
| Project/Area Number |
22510233
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 一般 |
|---|
| Research Field |
Living organism molecular science
|
|---|
| Research Institution | The University of Tokushima |
|---|
Principal Investigator |
KASHIWADA Yoshiki 徳島大学, 大学院・ヘルスバイオサイエンス研究部, 准教授 (30169429)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
TAKAISHI Yoshihisa 徳島大学, 大学院・ヘルスバイオサイエンス研究部, 教授 (60035558)
|
|---|
| Research Collaborator |
LEE Kuo-hsiung ノースカロライナ大学チャペルヒル校, エシェルマン薬学部, 教授
QIAN Keduo ノースカロライナ大学チャペルヒル校, エシェルマン薬学部, 助教
CHEN Chin-ho デューク大学, 医学部, 教授
|
|---|
| Project Period (FY) |
2010 – 2012
|
| Keywords | AIDS / 薬剤耐性 / トリテルペン / ベツリン |
|---|
| Research Abstract |
Based on our finding of a first-in-class drug candidate as a viral maturation inhibitor, bevirimat [3-O-(3',3'-dimethylsuccinyl)-betulinic acid], and potent anti-HIV active 3-O-acyl-(dihidro)betulin derivatives (e.g. 3-O-glutarydihydrobetulin and 3,28-di-O-dimethylsuccinylbetulin), a series of conjugates of 3,28-di-O-acylbetulin derivatives and HIV-reverse transcriptase inhibitor, AZT, as well as conjugates of 28-leucinyl-bevirimat and acyl-betulin derivatives were prepared and evaluated their anti-HIV activity. Several derivatives showed more potent anti-HIV activity than bevirimat.
|
