SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF 4-CARBAMOYL-6-BETA-THIENYL-4,5-DIHYDROPYRIDAZIN-3-(2H)ONES

被引:0
|
作者
PINNA, GA
CURZU, MM
GAVINI, E
MULE, A
PIRISINO, G
SATTA, M
PEANA, A
机构
[1] UNIV SASSARI,CATTEDRA FARMACOGNOSIA,VIA MURONI 23,I-07100 SASSARI,ITALY
[2] UNIV SASSARI,IST CHIM FARMACEUT,I-07100 SASSARI,ITALY
[3] UNIV SASSARI,IST TECN FARMACEUT,I-07100 SASSARI,ITALY
来源
FARMACO | 1993年 / 48卷 / 09期
关键词
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A new series of 4-carbamoyl-6-beta-thienyl-4,5-dihydropyridazin-3-(2H)ones 4a-g have been synthesized and tested for their anti-inflammatory and analgesic properties. Among the tested compounds, only 4f at 1 mmole/Kg showed antiinflammatory activity that was comparable with that of indomethacin (5 mg/Kg) though of shorter duration. Compounds 4a, 4e and especially 4g at 0.2 mmoles/Kg displayed relevant analgesic activity, 4g being the most potent derivative in the writhing test. Compounds 4c and 4g were found to possess analgesic activity also in the hot plate test.
引用
收藏
页码:1239 / 1248
页数:10
相关论文
共 50 条
  • [1] SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF 4-CARBAMOYL-5-ARYL-6-METHYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONES
    PINNA, GA
    SARDU, F
    CURZU, MM
    SATTA, M
    PEANA, A
    CIGNARELLA, G
    BARLOCCO, D
    FARMACO, 1992, 47 (04): : 449 - 463
  • [2] PREPARATION AND SOME REACTIONS OF 4-ARYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONES AND 5-ARYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONES
    BREUKELMAN, SP
    MEAKINS, GD
    ROE, AM
    JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1985, (08): : 1627 - 1635
  • [3] Some reactions with 6-(biphenyl)-4-(5-oxo-1,3-diphenyl-2-pyrazolin-4-yl)-4,5-dihydropyridazin-3-(2H)ones
    Kassab, RR
    Sayed, GH
    Radwan, AM
    Abd El-Azzez, N
    REVUE ROUMAINE DE CHIMIE, 2001, 46 (06) : 649 - 655
  • [4] A convenient synthesis of new phosphonomethyl-containing 4,5-dihydropyridazin-3(2H)-ones
    Bejaoui, Oumayma
    Abdelli, Abderrahmen
    M'rabet, Hedi
    Moreau, Xavier
    Efrit, Mohamed Lotfi
    Prim, Damien
    MENDELEEV COMMUNICATIONS, 2023, 33 (05) : 640 - 641
  • [5] Synthesis and evaluation of 2-substituted-6-phenyl-4,5-dihydropyridazin-3(2H)-ones as potent inodilators
    Kumar, Dinesh
    Carron, Rosalia
    De la Calle, Carmen
    Jindal, Dharam Paul
    Bansal, Ranju
    ACTA PHARMACEUTICA, 2008, 58 (04) : 393 - 405
  • [6] SYNTHESIS, COMPUTER AIDED SCREENING AND PHARMACOLOGICAL EVALUATION OF 2/3-SUBSTITUTED-6(4-METHYLPHENYL)-4,5-DIHYDROPYRIDAZIN3(2H)-ONES, AND PYRIDAZINE SUBSTITUTED TRIAZINE
    Khokra, Sukhbir Lal
    Seth, Sonakshi
    Garg, Shama S.
    Kaushik, Pawan
    Ahmad, Aftab
    Khan, Shah Alam
    Husain, Asif
    INDONESIAN JOURNAL OF PHARMACY, 2015, 26 (04): : 200 - 209
  • [7] A new approach to the synthesis of 4-(N-aryl)carbamoylmethyl-4,5-dihydropyridazin-3(2H)-ones
    Stepakov, Alexander V.
    Kinzhalov, Michail A.
    Boitsov, Vitaly M.
    Stepakova, Liubov V.
    Starova, Galina L.
    Vyazmin, Sergey Yu.
    Grinenko, Elena V.
    TETRAHEDRON LETTERS, 2011, 52 (24) : 3146 - 3149
  • [8] SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 3-CARBAMOYL-4-ARYL-ISOQUINOLIN-1(2H)-ONES
    UNVERFERTH, K
    DORRE, R
    KORNER, B
    SCHEIBE, H
    MORGENSTERN, E
    ARCHIV DER PHARMAZIE, 1991, 324 (10) : 809 - 814
  • [9] 6-Phenyl-4,5-dihydropyridazin-3(2H)-one
    Abourichaa, S
    Benchat, N
    Anaflous, A
    Melhaoui, A
    Ben-Hadda, T
    Oussaid, B
    El Bali, B
    Bolte, M
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2003, 59 : O802 - O803
  • [10] Expedient method for the solid-phase synthesis of some 4-substituted-4,5-dihydropyridazin-3(2H)-ones
    Gouault, N
    Cupif, JF
    Amoros, M
    David, M
    JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 2002, (20): : 2234 - 2236