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

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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.

DrugBank Data that Cites this Article

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