期刊
PROCEEDINGS OF THE JAPAN ACADEMY SERIES B-PHYSICAL AND BIOLOGICAL SCIENCES
卷 86, 期 2, 页码 85-102出版社
JAPAN ACAD
DOI: 10.2183/pjab.86.85
关键词
Argadin; Argifin; chitinase inhibitor; solid-phase synthesis; rational molecular design; in situ click chemistry
资金
- Ministry of Education Culture, Sports, Science and Technology
- Takeda Science Foundation
- Mochida Memorial Foundation for Medical and Pharmaceutical Research, a Kitasato University Research Grant for Young Researchers
- Research Foundation for Pharmaceutical Sciences
- Grants-in-Aid for Scientific Research [22790017] Funding Source: KAKEN
Chitin, the second most abundant polysaccharide in nature, occurs in fungi; some algae and many invertebrates, including insects. Thus, chitin synthesis and degradation could represent specific targets for fungicides and insecticides. Chitinases hydrolyze chitin into oligomers of N-acetyl-D-glucosamine at key points in the life cycles of organisms, consequently, chitinase inhibitors have become subject of increasing interest. This review covers the development of two chitinase inhibitors of natural origin, Argifin and Argadin, isolated from the cultured broth of microorganisms in our laboratory. In particular, the practical total synthesis of these natural products, the synthesis of lead compounds via, computer-aided rational molecular design, and discovery methods that generate only highly-active compounds using a kinetic target (chitinase)guided synthesis approach (termed in situ click chemistry) are described.
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