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

6 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

Access to Document

10.1016/j.bmc.2013.01.023

Link to publication in Scopus

Cite this

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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. ",

keywords = "Docking, Imidazophenoxazine, PDE4, Sulfonamide",

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

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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; Pal, Manojit.

In: Bioorganic & Medicinal Chemistry, Vol. 21, No. 7, 01.04.2013, p. 1952-1963.

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

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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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