Synthesis and structure-activity analysis of 2-(4-chlorophenyl)-5,6-dihydrothieno[2′,3′:2,3]thiepino[4,5-c]pyridazin-3(2H)-ones as ligands for benzodiazepine receptors

doi:10.1016/0223-5234(96)88305-X

Paper

DOI: 10.1016/0223-5234(96)88305-X

Synthesis and structure-activity analysis of 2-(4-chlorophenyl)-5,6-dihydrothieno[2′,3′:2,3]thiepino[4,5-c]pyridazin-3(2H)-ones as ligands for benzodiazepine receptors

Published 1995 · Hiroshi Tanaka, S. Kirihara, H. Yasumatsu

European Journal of Medicinal Chemistry

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Abstract

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In Vitro Study

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2-(4-chlorophenyl)-5,6-dihydrothieno[2′,3′:2,3]thiepino[4,5-c]pyridazin-3(2H)-ones show partial and full agonistic activities toward benzodiazepine receptor

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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References

DOI: 10.1111/j.1476-5381.1994.tb14868.x

The pharmacological properties of Y‐23684, a benzodiazepine receptor partial agonist

Y-23684 is a potent and selective anxiolytic agent with less side-effects than conventional BZ-anxiolytics, showing high affinity for the benzodiazepine receptor.

1994·33citations·H. Yasumatsu et al.·British Journal of Pharmacology

British Journal of Pharmacology

DOI: 10.1021/JM00032A007

Synthesis of benzo-fused benzodiazepines employed as probes of the agonist pharmacophore of benzodiazepine receptors.

Benzo-fused benzodiazepines 1-6 show moderate affinity for benzodiazepine receptors and exhibit both anticonvulsant and muscle relaxant activity, with full occupation of L2 resulting in increased muscle relaxant effects at the expense of anticonvulsant/anxiolytic effects.

1994·50citations·W. Zhang et al.·Journal of medicinal chemistry

Journal of medicinal chemistry

DOI: 10.1248/CPB.39.2556

Studies on the synthesis of condensed pyridazine derivatives. IV. Synthesis and anxiolytic activity of 2-aryl-5,6-dihydro-(1)benzothiepino[5,4- c]pyridazin-3(2H)-ones and related compound.

Compound 37 (Y-23684) shows potential as a potent anxiolytic agent with twice the potency of diazepam in anticonflict tests, but less muscle relaxation and augmentation of gamma-aminobutyric acid-induced chloride current than diazep

1991·7citations·T. Nakao et al.·Chemical & pharmaceutical bulletin

Chemical & pharmaceutical bulletin

DOI: 10.1248/CPB.39.524

Synthesis of 2-aryl-5,6-dihydro-(1)benzothiepino[5,4-c]pyridazin-3(2H)-one by a novel dehydrogenation reaction

This novel dehydrogenation reaction enables the synthesis of 2-aryl-5,6-dihydro-(1)benzothiepino[5,4-c]pyridazin-3(2H)-one in 80% yield, with potential applications in organic synthesis.

1991·5citations·T. Nakao et al.·Chemical & Pharmaceutical Bulletin

Chemical & Pharmaceutical Bulletin

DOI: 10.1248/YAKUSHI1947.110.12_922

[Studies on the synthesis of condensed pyridazine derivatives. III. Synthesis and benzodiazepine receptor binding studies of condensed triazolopyridazine derivatives].

Condensed triazolopyridazine derivatives with a planar shape show high affinity to the benzodiazepine receptor, with 11-aryl compounds showing potent affinity comparable to diazepam.

1990·2citations·T. Nakao et al.·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan

DOI: 10.1016/0165-6147(90)90126-S

Novel anxiolytics that act as partial agonists at benzodiazepine receptors.

Partial agonists at benzodiazepine receptors show potential in reducing unwanted side effects and enhancing anticonvulsant and anti-anxiety effects.

1990·229citations·W. Haefely et al.·Trends in pharmacological sciences

Trends in pharmacological sciences

DOI: 10.1248/YAKUSHI1947.110.8_561

[Studies on the synthesis of condensed pyridazine derivatives. I. Synthesis and benzodiazepine receptor binding studies of 2-substituted-4,4a,5,6-tetrahydrobenzo[h]cinnolin-3(2H)-ones and related compounds].

2-substituted-4,4a,5,6-tetrahydrobenzo[h]cinnolin-3(2H)-ones with 4-methoxyphenyl, 4-chlorophenyl, or 4-methylphenyl groups at position-2 show high affinity to the benz

1990·5citations·T. Nakao et al.·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan

DOI: 10.1248/YAKUSHI1947.110.8_573

[Studies on the synthesis of condensed pyridazine derivatives. II. Synthesis and anxiolytic activities of 2-aryl-4,4a,5,6-tetrahydropyridazino[4,3-c]quinolin-3(2H)-ones, 2-aryl-4a,5-dihydro-2H-(1)benzothiopyrano[4,3-c]pyridazin-3(4H)-ones, and related compounds].

The trans sulfoxide of 2-aryl-4,4a,5,6-tetrahydropyridazino[4,3-c]quinolin-3(4H)-one (16b) shows remarkable anxiolytic activities and may be useful in treating anxiety and narcotic pot

1990·4citations·T. Nakao et al.·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan

DOI: 10.1021/JM00165A028

Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester.

The pharmacophore for the agonist site of the benzodiazepine receptor requires interaction of two electron density sites, a third at E+, and two lipophilicity sites.

1990·86citations·S. Hollinshead et al.·Journal of medicinal chemistry

Journal of medicinal chemistry

Citations

DOI: 10.1007/s00044-011-9579-3

Benzoxepin derivatives: design, synthesis, and pharmacological evaluation with sedative–hypnotic effect

Novel benzoxepin-derived compounds, including compound 6, show a sedative-hypnotic effect when incorporated with a Phenobarbital moiety in the nucleus.

2012·7citations·Nagwa M. Abdel Gawad et al.·Medicinal Chemistry Research

Medicinal Chemistry Research

DOI: 10.1016/S0223-5234(97)83286-2

Synthesis and evaluation of novel 2-aryl-2,5,6,7-tetrahydro-3H-thieno [2′,3′:6,7]cyclohepta[1,2-c]pyridazin-3-ones and 2-aryl-5, 6-dihydrothieno[2,3-h]cinnolin-3(2H)-ones as anxiolytics

Novel 2-aryl-2,5,6,7-tetrahydro-3H-thieno compounds show high affinity for benzodiazepine receptors, with potential as anxiolytics.

1997·7citations·Hiroshi Tanaka et al.·European Journal of Medicinal Chemistry

European Journal of Medicinal Chemistry

DOI: 10.1002/JHET.5570340332

Synthesis of tricyclic and tetracyclic thieno[3,2-f]-1,4-thiazepines

Tricyclic and tetracyclic thieno[3,2-f]-1,4-thiazepines were synthesized, with potential for studying their affinity for benzodiazepine receptors.

1997·8citations·Hiroshi Tanaka et al.·Journal of Heterocyclic Chemistry

Journal of Heterocyclic Chemistry

DOI: 10.1016/S0079-6468(08)70047-X

New directions in anxiolytic drug research.

Newer, promising anxiolytic agents like RWJ-51204 show promise in reducing side-effects and enhancing efficacy compared to marketed benzodiazepines.

1999·8citations·M. Scott et al.·Progress in medicinal chemistry

Progress in medicinal chemistry