Synthesis and vasorelaxant activity of new 1,4-benzoxazine derivatives potassium channel openers

被引:36
作者
Caliendo, G
Perissutti, E
Santagada, V
Fiorino, F
Severino, B
Bianca, RDD
Lippolis, L
Pinto, A
Sorrentino, R
机构
[1] Univ Naples, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy
[2] Univ Naples Federico II, Dipartimento Sperimentale, I-80131 Naples, Italy
[3] Univ Salerno, Dipartimento Sci Farmaceut, Fisciano, SA, Italy
关键词
D O I
10.1016/S0968-0896(02)00091-3
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
As part of a search for new potassium channel openers, the synthesis and vasorelaxant activity of new 1,4-benzoxazilic derivatives derived from transformation of the benzopyran skeleton of cromakalim were described. Several new 1,4-benzoxazine derivatives were provided with significant vasorelaxant activity with an overall pharmacological behavior similar to CRK (1f, 1i, 2d, 2e, 2f and 2i). (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2663 / 2669
页数:7
相关论文
共 14 条
[1]  
ASHOOD VA, 1986, J MED CHEM, V29, P2194
[2]  
Atwal KS, 1996, CURR MED CHEM, V3, P227
[3]   SYNTHESIS AND BIOLOGICAL-ACTIVITY OF TRANS-(+/-)-N-METHYL-2-(3-PYRIDYL)-2-TETRAHYDROTHIOPYRANCARBOTHIOAMIDE 1-OXIDE (RP 49356) AND ANALOGS - A NEW CLASS OF POTASSIUM CHANNEL OPENER [J].
BROWN, TJ ;
CHAPMAN, RF ;
COOK, DC ;
HART, TW ;
MCLAY, IM ;
JORDAN, R ;
MASON, JS ;
PALFREYMAN, MN ;
WALSH, RJA ;
WITHNALL, MT ;
ALOUP, JC ;
CAVERO, I ;
FARGE, D ;
JAMES, C ;
MONDOT, S .
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (20) :3613-3624
[4]   Synthesis, biological activity and conformational study of 1,4-benzoxazine derivatives as potassium channel modulators [J].
Caliendo, G ;
Grieco, P ;
Perissutti, E ;
Santagada, V ;
Santini, A ;
Albrizio, S ;
Fattorusso, C ;
Pinto, A ;
Sorrentino, R .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1998, 33 (12) :957-967
[5]  
Empfield J. R., 1995, Annu. Rep. Med. Chem., V30, P81
[6]   K+ CHANNEL OPENERS AND NATURAL CARDIOPROTECTION [J].
ESCANDE, D ;
CAVERO, I .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1992, 13 (07) :269-272
[7]  
Garcia M L, 1997, Adv Pharmacol, V39, P425, DOI 10.1016/S1054-3589(08)60078-2
[8]   LEVCROMAKALIM [J].
HAMILTON, TC ;
BEERAHEE, A ;
MOEN, JS ;
PRICE, RK ;
RAMJI, JV ;
CLAPHAM, JC .
CARDIOVASCULAR DRUG REVIEWS, 1993, 11 (02) :199-222
[9]  
KAJINO M, 1991, CHEM PHARM BULL, V39, P2896
[10]   Potassium channel activation: A potential therapeutic approach? [J].
Lawson, K .
PHARMACOLOGY & THERAPEUTICS, 1996, 70 (01) :39-63