Studies on Agents with Vasodilator and .BETA.-Blocking Activities. I.

Seki, Toshimi; Takezaki, Takayuki; Ohuchi, Rikio; Ohuyabu, H.; Ishimori, Tsutomu; Yasuda, Kikuo

doi:10.1248/cpb.42.1609

Cited by 12 publications

(2 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The introduction of various secondary amines was uneventfully realized in near-quantitative yield producing compounds of very high purity. Unsaturated or deactivated amines (entries 27 and 28) could, however, not be introduced under these conditions.…”

Section: Resultsmentioning

confidence: 99%

Stereocontrolled Synthesis of Key Advanced Intermediates toward Simplified Acetogenin Analogues

1999

View full text Add to dashboard Cite

The stereo- and enantiocontrolled synthesis of substituted beta-hydroxy ethers based on glycol and catechol bearing an alkyne group and a series of substituents is reported. These substrates were designed to mimic the bis-THF array of annonaceous acetogenins and to provide an access to simplified and modified analogues. The key steps of the synthesis involve the condensation of the nonracemic mesylate of solketal with ethylene glycol and catechol, followed by an alkylation with a glycidyl derivative. Under appropriate conditions, the reaction is completely stereoselective and allows the synthesis of all the diastereomers. After the epoxide was opened with triethylsilylacetylene, the second epoxide was unmasked and reacted with a series of alkyl, aryl, amine, and alcohol reagents. A series of 28 analogues was prepared having a glycol or a catechol core, a stereodefined configuration of the flanking hydroxyl groups, and an acetylenic appendage suitable for a coupling to a lactone-bearing fragment.

show abstract

Section: Resultsmentioning

confidence: 99%

Stereocontrolled Synthesis of Key Advanced Intermediates toward Simplified Acetogenin Analogues

1999

View full text Add to dashboard Cite

show abstract

“…A substantial number of pyridazinones in the recent past have been reported to possess antimicrobial (Kassab, 2002;Mojahidul et al, 2008;Sayed et al, 2002), antitubercular (Sayed et al, 2002), analgesic (Piaz et al, 1996;Giovannoni et al, 2003;Gokce et al, 2001;Dogruer et al, 2000;Biancalani et al, 2009a, b;Pieretti et al, 1999;Rubat et al, 1992), anti-inflammatory (Hallas, 1995;Takaya et al, 1979;Dogruer et al, 2003;Flouzat et al, 1993;Gökce et al, 2009;Santagati et al, 1985a, b;Sato et al, 1981;Raskin, 1999;Cignarella et al, 1978;Deniz and Fethi, 2003;Banoglu et al, 2004;Ayla et al, 2003), cyclooxygenase inhibitor (Okcelik et al, 2003;Chintakunta et al, 2002), antidiabetic (Rathish et al, 2009), antihypertensive (Barbaro et al, 2001;Seki et al, 1996;Siddiqui and Wani, 2004;Bansal et al, 2009;Verdouw et al, 1986;Korvald et al, 2002;Rüegg et al, 1984;Schneider et al, 1979;Schudt et al, 1991;Ranju et al, 2008;Kubo, 1997;Kumar et al, 2008;Wang et al, 2008;Uhlmann et al, 1995;…”

Section: Introductionmentioning

confidence: 99%

Pyridazinone: an important element of pharmacophore possessing broad spectrum of activity

Dubey¹,

Bhosle

2015

Med Chem Res

View full text Add to dashboard Cite

In the last few years, the pyridazine derivatives have been found to exhibit a wide range of pharmacological activities. A large number of research articles and patents described them, and several drugs based on its nucleus have come into light. Pyridazinone, a derivative of pyridazine, was initially exploited in search of cardiovascular drugs and for its use in agrochemicals, but later on this nucleus was found to be associated with plethora of activities. In this article, we have reviewed the influence of structural changes on the pharmacodynamic profile of the pyridazinone moiety.

show abstract

References

2000

Chemistry of Heterocyclic Compounds: A Series of Monographs

View full text Add to dashboard Cite

Studies on Agents with Vasodilator and .BETA.-Blocking Activities. I.

Cited by 12 publications

References 0 publications

Stereocontrolled Synthesis of Key Advanced Intermediates toward Simplified Acetogenin Analogues

Stereocontrolled Synthesis of Key Advanced Intermediates toward Simplified Acetogenin Analogues

Pyridazinone: an important element of pharmacophore possessing broad spectrum of activity

References

Contact Info

Product

Resources

About