Synthesis of new 2-[1(2H)-phthalazinon-2-yl]-acetamide and 3-[1(2H)-phthalazinon-2-yl]-propanamide derivatives as antinociceptive and anti-inflammatory agents

被引：56
作者：
Dogruer, DS
Kupeli, E
Yesilada, E
Sahin, MF [1 ]
机构：
[1] Gazi Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06330 Ankara, Turkey
[2] Gazi Univ, Fac Pharm, Dept Pharmacognosy, TR-06330 Ankara, Turkey
来源：
ARCHIV DER PHARMAZIE | 2004年 / 337卷 / 06期
关键词：
1(2H); phthalazinone; antinociceptive; anti-inflammatory;
D O I：
10.1002/ardp.200200719
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
As a consequence of our ongoing studies on heterocyclic compounds for new antinociceptive and anti-inflammatory agents bearing lactam functional group, new 2-[1(2H)-phthalazinon-2-yl]acetamide and 3-[1(2H)-phthalazinon-2-yl]propanamide derivatives have been synthesized. Among the compounds synthesized, compound 4e was found the most active derivative in terms of antinociceptive and anti-inflammatory activities, without gastric lesions and bleeding at the given dose.
引用
收藏
页码：303 / 310
页数：8
相关论文
共 18 条
  • [11] Önkol T, 2001, ARCH PHARM, V334, P17
  • [12] Önkol T, 2000, ARCH PHARM, V333, P337
  • [13] Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, Celecoxib)
    Penning, TD
    Talley, JJ
    Bertenshaw, SR
    Carter, JS
    Collins, PW
    Docter, S
    Graneto, MJ
    Lee, LF
    Malecha, JW
    Miyashiro, JM
    Rogers, RS
    Rogier, DJ
    Yu, SS
    Anderson, GD
    Burton, EG
    Cogburn, JN
    Gregory, SA
    Koboldt, CM
    Perkins, WE
    Seibert, K
    Veenhuizen, AW
    Zhang, YY
    Isakson, PC
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (09) : 1347 - 1365
  • [14] ANNULATION TO THE PHTHALAZINE RING-SYSTEM UTILIZING MESOIONIC RING-SYSTEMS
    POTTS, KT
    BORDEAUX, KG
    KUEHNLING, WR
    SALSBURY, RL
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1985, 50 (10) : 1677 - 1681
  • [15] The discovery of rofecoxib, [MK 966, Vioxx®, 4-(4′-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2 inhibitor
    Prasit, P
    Wang, Z
    Brideau, C
    Chan, CC
    Charleson, S
    Cromlish, W
    Ethier, D
    Evans, JF
    Ford-Hutchinson, AW
    Gauthier, JY
    Gordon, R
    Guay, J
    Gresser, M
    Kargman, S
    Kennedy, B
    Leblanc, Y
    Léger, S
    Mancini, J
    O'Neill, GP
    Ouellet, M
    Percival, MD
    Perrier, H
    Riendeau, D
    Rodger, I
    Tagari, P
    Thérien, M
    Vickers, P
    Wong, E
    Xu, LJ
    Young, RN
    Zamboni, R
    Boyce, S
    Rupniak, N
    Forrest, N
    Visco, D
    Patrick, D
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (13) : 1773 - 1778
  • [16] NEW NON-STEROIDAL ANALGESIC ANTI-INFLAMMATORY AGENT - SYNTHESIS AND ACTIVITY OF 4-ETHOXY-2-METHYL-5-MORPHOLINO-3(2H)-PYRIDAZINONE AND RELATED COMPOUNDS
    TAKAYA, M
    SATO, M
    TERASHIMA, K
    TANIZAWA, H
    MAKI, Y
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1979, 22 (01) : 53 - 58
  • [17] STUDIES ON PYRIDAZINONE DERIVATIVES .16. ANALGESIC-ANTIINFLAMMATORY ACTIVITIES OF 3(2H)-PYRIDAZINONE DERIVATIVES
    TAKAYA, M
    SATO, M
    [J]. YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 1994, 114 (02): : 94 - 110
  • [18] VINEGAR R, 1987, FASEB J, V46, P118
12