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

Seelam Venkata Reddy; Gangula Mohan Rao; Baru Vijaya Kumar; Chandana L T Meda; Girdhar Singh Deora; K. Shiva Kumar; Kishore V L Parsa; Manojit Pal

doi:10.1016/j.bmc.2013.01.023

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

Seelam Venkata Reddy, Gangula Mohan Rao, Baru Vijaya Kumar, Chandana L T Meda, Girdhar Singh Deora, K. Shiva Kumar, Kishore V L Parsa, Manojit Pal

Research output: Contribution to journal › Article › Research › peer-review

12 Citations (Scopus)

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
Pages (from-to)	1952-1963
Number of pages	12
Journal	Bioorganic & Medicinal Chemistry
Volume	21
Issue number	7
DOIs	https://doi.org/10.1016/j.bmc.2013.01.023
Publication status	Published - 1 Apr 2013
Externally published	Yes

Keywords

Docking
Imidazophenoxazine
PDE4
Sulfonamide

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10.1016/j.bmc.2013.01.023

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title = "Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4",

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. ",

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AU - Reddy, Seelam Venkata

AU - Rao, Gangula Mohan

AU - Kumar, Baru Vijaya

AU - Meda, Chandana L T

AU - Deora, Girdhar Singh

AU - Kumar, K. Shiva

AU - Parsa, Kishore V L

AU - Pal, Manojit

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KW - Sulfonamide

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

Abstract

Keywords

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