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

被引：9

作者：

Reddy, Seelam Venkata ^{[1
]}

Rao, Gangula Mohan ^{[1
]}

Kumar, Baru Vijaya ^{[1
]}

Meda, Chandana L. T. ^{[2
]}

Deora, Girdhar Singh ^{[2
]}

Kumar, K. Shiva ^{[2
]}

Parsa, Kishore V. L. ^{[2
]}

Pal, Manojit ^{[2
]}

机构：

[1] CKM Arts & Sci Coll, Med Chem Lab, Res Ctr, Warangal 506006, Andhra Pradesh, India

[2] Univ Hyderabad Campus, Inst Life Sci, Hyderabad 500046, Andhra Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 07期

关键词：

Imidazophenoxazine; Sulfonamide; PDE4; Docking; PHOSPHODIESTERASE-4; INHIBITORS; ANTIPROLIFERATIVE ACTIVITY; PHENOXAZINES; DERIVATIVES; PHENOTHIAZINES; STRATEGY; AGENTS; RING;

D O I：

10.1016/j.bmc.2013.01.023

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu M. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：1952 / 1963

页数：12

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