SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF A NEW CLASS OF 2-OXO-8-AZASPIRO (4,5)DECAN-1-ONES AS ANALOGS OF THE MUSCARINIC AGONIST RS-86

被引：0
|
作者：
CIGNARELLA, G [1 ]
VILLA, S [1 ]
BARLOCCO, D [1 ]
机构：
[1] UNIV MODENA,DIPARTIMENTO SCI FARMACEUT,I-41100 MODENA,ITALY
来源：
FARMACO | 1993年 / 48卷 / 10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 8-substituted-2-oxo-8-azapsiro (4,5)decan-1-ones has been synthesized and compounds tested for their cholinergic properties in comparison with the muscarinic agonist RS-86. Preliminary in vitro and in vivo pharmacological data indicate that none of them is provided with significant cholinergic effects either at central or peripheral level. A possible explanation for the lack of activity is given on the basis of conformational studies.
引用
收藏
页码：1439 / 1445
页数：7
相关论文
共 32 条
  • [21] Synthesis and pharmacological investigation of novel 1-alkyl-4-(4-substituted aryl/heteroaryl)-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents
    Alagarsamy, Veerachamy
    Yadav, Mangae Ram
    Giridhar, Rajani
    ARZNEIMITTELFORSCHUNG-DRUG RESEARCH, 2006, 56 (12): : 834 - 841
  • [22] Synthesis of some new 2′-amino-2-fluoro-5′-oxo-1′-(4-phenylthiazole-2-yl)-1′,4′,5′,6′,7′,8′-hexahydro-3,4′-biquinoline-3′-carbonitrile derivatives and biological evaluation as antimicrobial agents
    Shah, Amish
    Raj, Dilipsinh
    JOURNAL OF SAUDI CHEMICAL SOCIETY, 2015, 19 (01) : 73 - 82
  • [23] Synthesis and pharmacological investigation of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]-quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents (vol 15, pg 1877, 2005)
    Alagarsamy, V
    Giridhar, R
    Yadav, MR
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (13) : 3316 - 3316
  • [24] Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198)
    Chang, Steven D.
    Brieaddy, Lawrence E.
    Harvey, Joseph D.
    Lewin, Anita H.
    Mascarella, S. Wayne
    Seltzman, Herbert H.
    Reddy, P. Anantha
    Decker, Ann M.
    McElhinny, Charles J., Jr.
    Zhong, Desong
    Peterson, Elisha E.
    Navarro, Hernan A.
    Bruchas, Michael R.
    Carroll, F. Ivy
    ACS CHEMICAL NEUROSCIENCE, 2015, 6 (12): : 1956 - 1964
  • [25] New Pyridobenzoxazepine Derivatives Derived from 5-(4-Methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): Chemical Synthesis and Pharmacological Evaluation
    Liegeois, Jean-Francois
    Deville, Marine
    Dilly, Sebastien
    Lamy, Cedric
    Mangin, Floriane
    Resimont, Melissa
    Tarazi, Frank I.
    JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (04) : 1572 - 1582
  • [26] A NEW CLASS OF INOTROPIC AGENTS - SYNTHESIS, SAR AND BIOLOGICAL PROFILE OF 2,4-DIHYDRO-5-[4-(1H-IMIDAZOL-1-YL)PHENYL]-3H-PYRAZOL-3-ONES - RING CONTRACTED ANALOGS OF IMAZODAN (CI-914)
    SIRCAR, I
    MORRISON, GC
    BOBOWSKI, G
    BURKE, SE
    SKEEAN, R
    WEISHAAR, RE
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1987, 194 : 57 - MEDI
  • [27] Synthesis and pharmacological evaluation of 3-(2-furyl)- and 3-(3-furyl)-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides, new 3-heteroaryl substituted benzodiazepine receptor ligands
    Costanzo, A
    Guerrini, G
    Ciciani, G
    Bruni, F
    Costagli, C
    Selleri, S
    Costa, B
    Martini, C
    Malmberg-Aiello, P
    MEDICINAL CHEMISTRY RESEARCH, 2002, 11 (02) : 87 - 101
  • [28] SYNTHESIS OF NOVEL FUSED BETA-LACTAMS BY INTRAMOLECULAR 1,3-DIPOLAR CYCLO-ADDITIONS .7. (9RS,9ARS)-9,9A-DIHYDRO-5-METHYL-8-OXO-9-PHENOXYACETAMIDO-8H-AZETO[1,2-A]-V-TRIAZOLO[5,1-C]PYRAZINE-6-CARBOXYLIC ACIDS AND (3BRS,4RS,7SR)-4,5-DIHYDRO-5-OXO-4-PHENOXYACETAMIDO-3BH-AZETO[1',2'-3,4]-IMIDAZO[1,5-C]-V-TRIAZOLE-7-CARBOXYLIC ACID,
    BRANCH, CL
    FINCH, SC
    PEARSON, MJ
    JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1985, (07): : 1491 - 1498
  • [29] Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-thienylmethoxycarbonyl) derivative: An anxioselective agent in rodents
    Costanzo, A
    Guerrini, G
    Ciciani, G
    Bruni, F
    Costagli, C
    Selleri, S
    Besnard, F
    Costa, B
    Martini, C
    Malmberg-Aiello, P
    JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (26) : 5710 - 5720
  • [30] Convenient synthesis, characterization, evaluation and molecular docking of some new fused pyrazolo[3,4-d]pyrimidine derivatives and 3-methyl-8 phenylpyrazolo[3′,4':4,5]pyrimido[6,1-c][1,2,4]triazines against HeLa cancer cells
    Helmy, Mirna T.
    Teleb, Mohamed A. Mohamed
    Hanna, Demiana H.
    El-Maadawy, Mohamed W.
    Hassaneen, Hamdi M.
    Kamel, Monica G.
    TETRAHEDRON, 2025, 177
1234