Synthesis and properties of novel alkoxy- and phenoxyalkyl ethers of secondary and tertiary ethynylpiperidin-4-ols possessing unusual analgesic, anti-bacterial, anti-spasmotic, and anti-allergic properties as well as low toxicity
Joint Authors
Yu, Valentina K.
Kabdraissova, Aissulu Zh.
Praliyev, Kaldybay D.
Shin, Svetlana N.
Berlin, K. Darrell
Source
Journal of Saudi Chemical Society
Issue
Vol. 13, Issue 2 (31 Aug. 2009), pp.209-217, 9 p.
Publisher
Publication Date
2009-08-31
Country of Publication
Saudi Arabia
No. of Pages
9
Main Subjects
Topics
Abstract EN
Methodology was developed to obtain a series of unusual alkoxy-and phenoxyalkyl ethers of secondary and tertiary ethynylpiperidin-4-ols representative examples of which were evaluated for analgesic, anti-bacterial, anti-spasmodic, and anti-allergic activity.
Twenty-two new compounds were prepared and identified by elemental and spectra analyses.
Etherification of 4-hydroxypiperidin-4-ols was accomplished via Williamson ether-type syntheses in dry DMF.
Side reactions of the bromides used appeared to involve complex processes with DMF under a variety of conditions employed which led to modest yields of products.
Since all target molecules were oils at room temperature, conversions to P-cyclodextrins were accomplished and served as vehicles for pharmacological screening.
Several ethyl-substituted agents displayed deep analgesic activity in the "tail flick" model although some alkoxy- and phenoxy ethers from secondary alcohols were less effective as analgesics (Table 1).
Interestingly, LD50 values for the agents.
American Psychological Association (APA)
Yu, Valentina K.& Kabdraissova, Aissulu Zh.& Praliyev, Kaldybay D.& Shin, Svetlana N.& Berlin, K. Darrell. 2009. Synthesis and properties of novel alkoxy- and phenoxyalkyl ethers of secondary and tertiary ethynylpiperidin-4-ols possessing unusual analgesic, anti-bacterial, anti-spasmotic, and anti-allergic properties as well as low toxicity. Journal of Saudi Chemical Society،Vol. 13, no. 2, pp.209-217.
https://search.emarefa.net/detail/BIM-250899
Modern Language Association (MLA)
Yu, Valentina K.…[et al.]. Synthesis and properties of novel alkoxy- and phenoxyalkyl ethers of secondary and tertiary ethynylpiperidin-4-ols possessing unusual analgesic, anti-bacterial, anti-spasmotic, and anti-allergic properties as well as low toxicity. Journal of Saudi Chemical Society (Aug. 2009), pp.209-217.
https://search.emarefa.net/detail/BIM-250899
American Medical Association (AMA)
Yu, Valentina K.& Kabdraissova, Aissulu Zh.& Praliyev, Kaldybay D.& Shin, Svetlana N.& Berlin, K. Darrell. Synthesis and properties of novel alkoxy- and phenoxyalkyl ethers of secondary and tertiary ethynylpiperidin-4-ols possessing unusual analgesic, anti-bacterial, anti-spasmotic, and anti-allergic properties as well as low toxicity. Journal of Saudi Chemical Society. 2009. Vol. 13, no. 2, pp.209-217.
https://search.emarefa.net/detail/BIM-250899
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references : p. 217
Record ID
BIM-250899