Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship
Shoujun Chen
1
,
Zhiqiang Xia
1
,
Masazumi Nagai
1
,
Rongzhen Lu
1
,
Elena Kostik
1
,
Teresa Przewloka
1
,
Minghu Song
1
,
Dinesh Chimmanamada
1
,
David James
1
,
Shijie Zhang
1
,
Jun Jiang
1
,
Mitsunori ONO
1
,
Keizo Koya
1
,
Lijun Sun
1
1
Synta Pharmaceuticals Corp., 45 Hartwell Ave., Lexington, MA, USA
|
Publication type: Journal Article
Publication date: 2011-01-01
SJR: —
CiteScore: —
Impact factor: —
ISSN: 20402503, 20402511
Organic Chemistry
Drug Discovery
Biochemistry
Pharmacology
Pharmaceutical Science
Molecular Medicine
Abstract
A series of novel indolizine 2-oxoacetamides were designed and synthesized as PDE4 inhibitors. Preliminary SAR of this new class of compounds revealed key structural features required for high potency. Compounds 1ab and 2a are among the most potent inhibitors of PDE4 with low single nM IC50. Cellular activity was demonstrated by the inhibition of TNFα production from human PBMC with IC50 ranging from 14 to 72 nM. Docking analyses suggest the OH group in 1ab enhance the binding via an H-bond interaction with the PDE4 enzyme.
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Metrics
35
Total citations:
35
Citations from 2025:
3
(8.57%)
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MLA
Cite this
GOST
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Chen S. et al. Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship // MedChemComm. 2011. Vol. 2. No. 3. pp. 176-180.
GOST all authors (up to 50)
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Chen S., Xia Z., Nagai M., Lu R., Kostik E., Przewloka T., Song M., Chimmanamada D., James D., Zhang S., Jiang J., ONO M., Koya K., Sun L. Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship // MedChemComm. 2011. Vol. 2. No. 3. pp. 176-180.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1039/c0md00215a
UR - https://doi.org/10.1039/c0md00215a
TI - Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship
T2 - MedChemComm
AU - Chen, Shoujun
AU - Xia, Zhiqiang
AU - Nagai, Masazumi
AU - Lu, Rongzhen
AU - Kostik, Elena
AU - Przewloka, Teresa
AU - Song, Minghu
AU - Chimmanamada, Dinesh
AU - James, David
AU - Zhang, Shijie
AU - Jiang, Jun
AU - ONO, Mitsunori
AU - Koya, Keizo
AU - Sun, Lijun
PY - 2011
DA - 2011/01/01
PB - Royal Society of Chemistry (RSC)
SP - 176-180
IS - 3
VL - 2
SN - 2040-2503
SN - 2040-2511
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2011_Chen,
author = {Shoujun Chen and Zhiqiang Xia and Masazumi Nagai and Rongzhen Lu and Elena Kostik and Teresa Przewloka and Minghu Song and Dinesh Chimmanamada and David James and Shijie Zhang and Jun Jiang and Mitsunori ONO and Keizo Koya and Lijun Sun},
title = {Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship},
journal = {MedChemComm},
year = {2011},
volume = {2},
publisher = {Royal Society of Chemistry (RSC)},
month = {jan},
url = {https://doi.org/10.1039/c0md00215a},
number = {3},
pages = {176--180},
doi = {10.1039/c0md00215a}
}
Cite this
MLA
Copy
Chen, Shoujun, et al. “Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship.” MedChemComm, vol. 2, no. 3, Jan. 2011, pp. 176-180. https://doi.org/10.1039/c0md00215a.