Novel adenosine-derived inhibitors of Cryptosporidium parvum inosine 5 '-monophosphate dehydrogenase

Shigetomi, Kengo; Sarwono, Albertus Eka Yudistira; Ichikawa, Satoshi et al.

Journal of antibiotics, 2019, 72(12), 934-942

Permalink : https://hdl.handle.net/2115/78287

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アクセス権
open access
URI
https://hdl.handle.net/2115/78287
タイトル
Novel adenosine-derived inhibitors of Cryptosporidium parvum inosine 5 '-monophosphate dehydrogenase
著者
Shigetomi, Kengo ; Sarwono, Albertus Eka Yudistira ; Ichikawa, Satoshi ; Ubukata, Makoto
e-Rad_Researcher
20547202
著者名
Shigetomi, Kengo
著者名
Sarwono, Albertus Eka Yudistira
e-Rad_Researcher
60333621
著者名
Ichikawa, Satoshi
e-Rad_Researcher
60168739
著者名
Ubukata, Makoto
言語
英語
発行日
2019-12
出版者
Nature Publishing Group
収録物名
Journal of antibiotics
巻(号)
72(12)
ページ
934-942
抄録
We have found cyclophane-type adenosine derivatives having p-quinone amide moieties (1 and 2) as weak inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase (CpIMPDH) from the Hokkaido University Chemical Library via the luciferase-based high-throughput screening. To obtain more potent inhibitors, we synthesized four new derivatives free from cyclophane rings (3-6). The N-H derivatives 3 and 5 showed more potent activities (24.4 and 11.1 mu M, respectively) in the presence of dithiothreitol (DTT), whereas the N-methyl derivative 4 indicated more potent activity (2.1 mu M) without DTT. Conformational analysis of compounds 3 and 4 suggested that N-H amide 3 binds to IMP-binding site in the DTT mediated manner.
資源タイプ
学術雑誌論文
出版タイプ
Accepted Manuscript
PISSN
0021-8820
EISSN
1881-1469
NCID
AA0069330X
関連情報
PMID
31296916
関連情報 (isVersionOf)
出版社版DOI
https://doi.org/10.1038/s41429-019-0199-3