Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4.
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Reddy SV, Rao GM, Kumar BV, Meda CL, Deora GS, Kumar KS, Parsa KV, Pal M
Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4.
Bioorg Med Chem. 2013 Apr 1;21(7):1952-63. doi: 10.1016/j.bmc.2013.01.023. Epub 2013 Jan 26.
- PubMed ID
- 23415088 [ View in PubMed]
- 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 muM.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) (R)-Rolipram cAMP-specific 3',5'-cyclic phosphodiesterase 4B IC 50 (nM) 941 N/A N/A Details