STUDIES ON CARDIOTONIC AGENTS .6. SYNTHESIS OF NOVEL 4,5-DIHYDRO-3(2H)-PYRIDAZINONE DERIVATIVES CARRYING SOME BENZOHETEROCYCLES AT THE 6-POSITION

被引:0
|
作者
NOMOTO, Y
TAKAI, H
OHNO, T
KUBO, K
机构
关键词
CARDIOTONIC AGENT; STRUCTURE ACTIVITY RELATIONSHIP; PYRIDAZINONE; QUINAZOLINE; BENZOTHIAZOLE; IMIDAZOBENZOTHIAZOLE; BENZOTHIOPHENE; BENZOTHIENOPYRIMIDINE;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several benzothiazolyl, imidazobenzothiazolyl, benzothienyl, benzothienopyrimidinyl and quinazolinyl 4,5-dihydro-3(2H)-pyridazinones were synthesized and examined for cardiotonic activity in anesthetized dogs after i.v. administration. Among them, 4-methylamino-7-(2,3,4,5-tetrahydro-5-methyl-3-oxo-6-pyridazinyl)quinazoline (36) showed potent and long-lasting inotropic activity (relative potency = 2.11, milrinone = 1). The activity of 36 was more potent that indolidan (2) (relative potency = 1.53) which is one of the most potent inotropic agents to date.
引用
收藏
页码:352 / 357
页数:6
相关论文
共 50 条
  • [31] EFFECTS OF 6-[PARA-(4-PHENYLACETYLPIPERAZIN-1-YL)PHENYL]-4,5-DIHYDRO-3(2H)PYRIDAZINONE (CCI-17810) AND ASPIRIN ON PLATELET-AGGREGATION AND ADHESIVENESS
    GRIFFETT, EM
    KINNON, SM
    KUMAR, A
    LECKER, D
    SMITH, GM
    TOMICH, EG
    BRITISH JOURNAL OF PHARMACOLOGY, 1981, 72 (04) : 697 - 705
  • [32] SYNTHESIS AND EVALUATION OF SOME 4,5-DISUBSTITUTED 6-PHENYL-3(2H)-PYRIDAZINONES AS HYPOTENSIVE AGENTS
    DALPIAZ, V
    GIOVANNONI, MP
    LAGUNA, R
    CANO, E
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1994, 29 (03) : 249 - 252
  • [33] SYNTHESIS AND REACTIONS OF 6-ARYL-4-(3,5-DIMETHYLPYRAZOL-1-YL)-4,5-DIHYDRO-3(2H)-PYRIDAZINONES AND THE STUDY OF THEIR ANTIBACTERIAL AND MOLLUSCICIDAL ACTIVITIES
    SAYED, GH
    YOUSIF, NM
    SHIBA, SA
    MOHAMED, SM
    FLEFEL, IM
    JOURNAL OF THE CHEMICAL SOCIETY OF PAKISTAN, 1992, 14 (02): : 125 - 132
  • [34] SYNTHESIS OF SOME 2-(2-BENZOTHIAZOLYL) AND 2-(2-BENZIMIDAZOLYL)-6-ARYL-4, 5-DIHYDRO-3(2H)-PYRIDAZINONES AS POTENTIAL ANTIINFLAMMATORY AGENTS
    SAWHNEY, SN
    BHUTANI, S
    VIR, D
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 1987, 26 (04): : 348 - 350
  • [35] ANTIHYPERTENSIVE AND ANTITHROMBOTIC ACTIVITIES OF 6-(SUBSTITUTED PHENYL)-5-HYDROXYMETHYL-4,5-DIHYDRO-3(2H)PYRIDAZINONES
    BARLOCCO, D
    MARTINI, A
    PINNA, GA
    CURZU, MM
    SALA, F
    GERMINI, M
    FARMACO-EDIZIONE SCIENTIFICA, 1987, 42 (08): : 585 - 594
  • [36] Synthesis of 11H-indolo[3,2-c]quinoline derivatives carrying a substituent at the 6-position
    Kobayashi, K. (kkoba@chem.tottori-u.ac.jp), 1600, Chemical Society of Japan (78):
  • [37] CRYSTAL-STRUCTURE OF 4,5-DIHYDRO-6-(2-THIENYL)-3(2H)PYRIDAZINONE AZINE, C16H16N6S2
    WILL, G
    FARAG, ISA
    ELKORDY, M
    ACTA CRYSTALLOGRAPHICA SECTION A, 1984, 40 : C285 - C285
  • [38] SYNTHESIS AND REACTION OF 6(9'-ANTHRACENYL)-3(2H)-PYRIDAZINONE DERIVATIVES AND STUDY OF THEIR MICROBIOLOGICAL ACTIVITY
    YASSIN, FA
    ELFARARGY, AF
    ELMOBAYED, MM
    ELKADY, MY
    ELMAKSOUD, MRA
    JOURNAL OF THE CHEMICAL SOCIETY OF PAKISTAN, 1991, 13 (04): : 267 - 272
  • [39] 2-Methyl-6-(4-aminophenyl)-4,5-dihydro-3(2H)-pyridazinone Synthon for Some New Annelated 1,2,3-Selena/Thiadiazoles and 2H-Diazaphospholes with Anticipated Biological Activity and Quantum Chemical Calculations
    El-Shamy, I. E.
    Hleli, E.
    El-Hashash, M. A.
    Kelnar, I.
    Abdel-Mohsen, A. M.
    MOLECULES, 2023, 28 (03):
  • [40] 6-(SUBSTITUTED PHENYL)-5-SUBSTITUTED-4,5-DIHYDRO-3(H-2)-PYRIDAZINONES - ANTIHYPERTENSIVE AGENTS
    MCEVOY, FJ
    ALLEN, GR
    JOURNAL OF MEDICINAL CHEMISTRY, 1974, 17 (03) : 281 - 286