Novel Quinolizidinyl Derivatives as Antiarrhythmic Agents: 2. Further Investigation

被引：15

作者：

Tasso, Bruno ^{[1
]}

Budriesi, Roberta ^{[2
]}

Vazzana, Iana ^{[1
]}

Ioan, Pierfranco ^{[2
]}

Micucci, Matteo ^{[2
]}

Novelli, Federica ^{[1
]}

Tonelli, Michele ^{[1
]}

Sparatore, Anna ^{[3
]}

Chiarini, Alberto ^{[2
]}

Sparatore, Fabio ^{[1
]}

机构：

[1] Univ Genoa, Dipartimento Sci Farmaceut, I-16132 Genoa, Italy

[2] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

[3] Univ Milan, Dipartimento Sci Farmaceut, I-20133 Milan, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 12期

关键词：

PHARMACOLOGICAL INTEREST; ATRIAL-FIBRILLATION; RECEPTOR ANTAGONISTS; 1-LUPINYLQUINOXALIN-2(1H)-ONES; METOCLOPRAMIDE; ARRHYTHMIAS; LUPININE; LIGANDS; DRUGS; 5-HT3;

D O I：

10.1021/jm100298d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Fifteen quinolizidine derivatives have been tested for antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig (gp) heart tissues and to assess calcium antagonist activity. All compounds exhibited from moderate to high antiarrhythmic activity, and five of them (3, 4, 6, 13, and 15) were more active and potent than the reference drugs (amiodarone, lidocaine, procainamide, and quinidine). These compounds were studied on spontaneously beating Langendorff-perfuse gp heart; even at concentration 17-67 times higher than the Corresponding EC50 for antiarrhythmic activity, they prolonged the QT intervals only moderately, comparing favorably with amiodarone and quinidine. Compounds 3 and 15 deserve further investigation due to their interesting cardiovascular profiles.

引用

页码：4668 / 4677

页数：10

共 50 条

[21] STUDIES ON CARDIOTONIC AGENTS .2. SYNTHESIS OF NOVEL PHTHALAZINE AND 1,2,3-BENZOTRIAZINE DERIVATIVES
NOMOTO, Y
OBASE, H
TAKAI, H
TERANISHI, M
NAKAMURA, J
KUBO, K
CHEMICAL & PHARMACEUTICAL BULLETIN, 1990, 38 (08) : 2179 - 2183
[22] INTERCALATING AGENTS WITH COVALENT BOND FORMING CAPABILITY - A NOVEL TYPE OF POTENTIAL ANTICANCER AGENTS .2. DERIVATIVES OF CHRYSOPHANOL AND EMODIN
KOYAMA, M
TAKAHASHI, K
CHOU, TC
DARZYNKIEWICZ, Z
KAPUSCINSKI, J
KELLY, TR
WATANABE, KA
JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (07) : 1594 - 1599
[23] 2-AMINOBENZENETHIOL DERIVATIVES AS POTENTIAL PSYCHOTHERAPEUTIC AGENTS .2.
NIEFORTH, KA
ROBICHAUD, RC
JOURNAL OF PHARMACEUTICAL SCIENCES, 1964, 53 (05) : 529 - +
[24] Antirheumatic agents .2. Novel methotrexate derivatives bearing an alkyl-substituted benzene ring
Matsuoka, H
Maruyama, N
Suzuki, H
Kuroki, T
Tsuji, K
Kato, N
Ohi, N
Mihara, M
Takeda, Y
Yano, K
CHEMICAL & PHARMACEUTICAL BULLETIN, 1996, 44 (12) : 2287 - 2293
[25] ENDORIBONUCLEASE-IV .2. FURTHER INVESTIGATION ON SPECIFICITY
MULLER, WEG
SEIBERT, G
STEFFEN, R
ZAHN, RK
EUROPEAN JOURNAL OF BIOCHEMISTRY, 1976, 70 (01): : 249 - 258
[26] SYNTHESIS OF INDAN DERIVATIVES AS POSSIBLE ANTIHYPERTENSIVE AGENTS .2.
GHOSHAL, PN
PATHAK, B
JOURNAL OF THE INDIAN CHEMICAL SOCIETY, 1978, 55 (09) : 897 - 901
[27] SOME DERIVATIVES OF TETRAHYDROPYRAN AS POTENTIAL PHARMACODYNAMIC AGENTS .2.
BURGER, A
TURNBULL, LB
DINWIDDIE, JG
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1950, 72 (12) : 5512 - 5515
[28] SYNTHESIS OF POTENTIAL ANTIVIRAL AGENTS .2. PYRIDINE DERIVATIVES
SADLER, PW
JOURNAL OF ORGANIC CHEMISTRY, 1961, 26 (04): : 1315 - +
[29] Antiarrhythmic activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
Jacek Sapa
Barbara Filipek
Małgorzata Zygmunt
Katarzyna Kulig
Barbara Malawska
Pharmacological Reports, 2010, 62 : 98 - 98
[30] Investigation of Novel Isatinylhydantoin Derivatives as Potential Anti-Kinetoplastid Agents
Sechoaro, Keamogetswe
Aucamp, Janine
Kannigadu, Christina
van Rensburg, Helena D. Janse
Suganuma, Keisuke
N'Da, David D.
CHEMMEDCHEM, 2025, 20 (01)

← 1 2 3 4 5 →