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.
Original language | English |
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Pages (from-to) | 1952-1963 |
Number of pages | 12 |
Journal | Bioorganic & Medicinal Chemistry |
Volume | 21 |
Issue number | 7 |
DOIs | |
Publication status | Published - 1 Apr 2013 |
Externally published | Yes |
Keywords
- Docking
- Imidazophenoxazine
- PDE4
- Sulfonamide