Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4

Reddy, Seelam Venkata, Rao, Gangula Mohan, Kumar, Baru Vijaya, Meda, Chandana L. T., Deora, Girdhar Singh, Kumar, K. Shiva, Parsa, Kishore V. L. and Pal, Manojit (2013) Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4. Bioorganic and Medicinal Chemistry, 21 7: 1952-1963. doi:10.1016/j.bmc.2013.01.023


Author Reddy, Seelam Venkata
Rao, Gangula Mohan
Kumar, Baru Vijaya
Meda, Chandana L. T.
Deora, Girdhar Singh
Kumar, K. Shiva
Parsa, Kishore V. L.
Pal, Manojit
Title Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4
Journal name Bioorganic and Medicinal Chemistry   Check publisher's open access policy
ISSN 0968-0896
1464-3391
Publication date 2013-04-01
Year available 2013
Sub-type Article (original research)
DOI 10.1016/j.bmc.2013.01.023
Volume 21
Issue 7
Start page 1952
End page 1963
Total pages 12
Place of publication Kidlington, Oxford, United Kingdom
Publisher Pergamon
Collection year 2014
Language eng
Formatted abstract
A number of novel imidazophenoxazine-4-sulfonamides have been designed as potential inhibitors of PDE4. All these compounds were readily prepared via an elegant multi-step method involving the initial construction of 1-nitro 10H-phenoxazine ring and then fused imidazole ring as key steps. Some of these compounds showed promising PDE4B and D inhibition when tested in vitro and good interactions with these proteins in silico. Three of these compounds showed dose dependent inhibition of PDE4B with IC50 value of 3.31 ± 0.62, 1.23 ± 0.18 and 0.53 ± 0.18 μM.
Keyword Imidazophenoxazine
Sulfonamide
PDE4
Docking
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Non HERDC
School of Pharmacy Publications
 
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