Design, synthesis and in vitro PDE4 inhibition activity of certain quinazolinone derivatives for treatment of asthma

被引：11

作者：

Elansary, Afaf K. ^{[1
]}

Kadry, Hanan H. ^{[1
]}

Ahmed, Eman M. ^{[1
]}

Sonousi, Amr Sayed Motawi ^{[1
]}

机构：

[1] Cairo Univ, Fac Pharm, Dept Organ Chem, Cairo 11562, Egypt

来源：

MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 11期

关键词：

Phosphodiesterase 4 (PDE4) inhibitors; Quinazolinone; Asthma; Synthesis; PHOSPHODIESTERASE; AMINES;

D O I：

10.1007/s00044-011-9846-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this study, a novel series of quinazolinone derivatives analogue to nitraquazone structure were synthesized. The compounds tested for their inhibitory activity against phosphodiesterase 4B revealed that compound 6d shows promising inhibitory activity comparable to that of Rolipram, whereas compounds 6a and 6c exhibited moderate inhibitory activity.

引用

页码：3327 / 3335

页数：9

共 23 条

[1]

ADELROTH E, 1990, AM REV RESPIR DIS, V142, P91

[2] NEW ASPECTS OF ASTHMA [J].

BARNES, PJ .

JOURNAL OF INTERNAL MEDICINE, 1992, 231 (05) :453-461

[3]

BUTCHER RW, 1962, J BIOL CHEM, V237, P1244

[4] Gallium(III) triflate-catalyzed one-pot selective synthesis of 2 3-dihydroquinazolin-4(1H)-ones and quinazolin-4(3H)-ones [J].

Chen, Jiuxi ;

Wu, Dengze ;

He, Fei ;

Liu, Miaochang ;

Wu, Huayue ;

Ding, Jinchang ;

Su, Weike .

TETRAHEDRON LETTERS, 2008, 49 (23) :3814-3818

[5] Isatoic anhydride I Reactions with primary and secondary amines and with some amides [J].

Clark, RH ;

Wagner, EC .

JOURNAL OF ORGANIC CHEMISTRY, 1944, 9 (01) :55-67

[6] Design, synthesis, and biological activities of new thieno[3,2-d]pyrimidines as selective type 4 phosphodiesterase inhibitors [J].

Crespo, MI ;

Pagès, L ;

Vega, A ;

Segarra, V ;

López, M ;

Doménech, T ;

Miralpeix, M ;

Beleta, J ;

Ryder, H ;

Palacios, JM .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (21) :4021-4035

[7] Therapeutic potential of phosphodiesterase 4 inhibitors in allergic diseases [J].

Crocker, IC ;

Townley, RG .

DRUGS OF TODAY, 1999, 35 (07) :519-535

[8] Phosphodiesterase 4 inhibitors, structurally unrelated to Rolipram, as promising agents for the treatment of asthma and other pathologies [J].

Dal Piaz, V ;

Giovannoni, MP .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2000, 35 (05) :463-480

[9] MUCOSAL INFLAMMATION IN ASTHMA [J].

DJUKANOVIC, R ;

ROCHE, WR ;

WILSON, JW ;

BEASLEY, CRW ;

TWENTYMAN, OP ;

HOWARTH, PH ;

HOLGATE, ST .

AMERICAN REVIEW OF RESPIRATORY DISEASE, 1990, 142 (02) :434-457

[10] Chromate oxidation of α-nitro alcohols to α-nitro ketones:: Significant improvements to a classic method [J].

Elmaaty, TA ;

Castle, LW .

MOLECULES, 2005, 10 (12) :1458-1461

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