Atsuyuki Kojima scite author profile

A series of cyclic imides bearing a omega-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT1A receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,-3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.

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Discovery of a novel potent Na + /Ca 2+ exchanger inhibitor: design, synthesis and structure–activity relationships of 3,4-dihydro-2(1 H )-quinazolinone derivatives

Hasegawa

Muraoka

Matsui

et al. 2003

Bioorganic & Medicinal Chemistry Letters

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Coumarins as novel 17β-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer

Harada¹,

Kubo²,

Tomigahara³

et al. 2010

Bioorganic & Medicinal Chemistry Letters

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A novel class of sodium/calcium exchanger inhibitor: design, synthesis, and structure–activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives

Hasegawa

Muraoka

Ohmori

et al. 2005

Bioorganic & Medicinal Chemistry

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Atsuyuki Kojima

Structure-activity relationship of optically active 2-(3-pyridyl)thiazolidin-4-ones as a PAF antagonists

Synthesis and Anxiolytic Activity of N-Substituted Cyclic Imides(1R,2S,3R,4S)-N-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-2,3-bicyclo(2.2.1)heptanedicarboximide(Tandospirone) and Related Compounds.

Discovery of a novel potent Na + /Ca 2+ exchanger inhibitor: design, synthesis and structure–activity relationships of 3,4-dihydro-2(1 H )-quinazolinone derivatives

Coumarins as novel 17β-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer

A novel class of sodium/calcium exchanger inhibitor: design, synthesis, and structure–activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives

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Atsuyuki Kojima

Structure-activity relationship of optically active 2-(3-pyridyl)thiazolidin-4-ones as a PAF antagonists

Synthesis and Anxiolytic Activity of N-Substituted Cyclic Imides(1R*,2S*,3R*,4S*)-N-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-2,3-bicyclo(2.2.1)heptanedicarboximide(Tandospirone) and Related Compounds.

Discovery of a novel potent Na + /Ca 2+ exchanger inhibitor: design, synthesis and structure–activity relationships of 3,4-dihydro-2(1 H )-quinazolinone derivatives

Coumarins as novel 17β-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer

A novel class of sodium/calcium exchanger inhibitor: design, synthesis, and structure–activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives

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Product

Resources

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Synthesis and Anxiolytic Activity of N-Substituted Cyclic Imides(1R,2S,3R,4S)-N-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-2,3-bicyclo(2.2.1)heptanedicarboximide(Tandospirone) and Related Compounds.