Synthesis, Pharmacological Properties and SAR of New 1,4-Disubstituted Pierazine Derivatives with Hypnotic-Sedative Activity

• Autorzy: Chilmonczyk Z. , Mazgajska M. , Chojnacka-Wójcik E. , Tatarczyńska E. , Kłodzińska A. , Ulman M.
• Języki publikacji: EN

Abstrakty

EN

Synthesis, chromatographic behaviour, pharmacological data and structure activity relationship (SAR) studies of some 1-(pyrimidin-2-yl)piperazine derivatives 1-13 are reported. The hydrophobic indices and chromatographic retention factors of the compounds exhibited statistically significant linear correlation with the calculated lipophilicities. The highest hypnotic-sedative activity as measured in loss of the righting reflex, rota-rod and spontaneous locomotor activity tests exhibited compound6 possessing n-hexyl R substituent. The hypnotic activity of compounds 1-13 measured in loss of the righting reflex test could be described with the aid of hydrophobic indices in terms of Hansch parabolic relationship for structurally related group of compounds (separately for compounds withR= alkyl orR= cycloalkyl). The necessity to describe the pharmacological activity for aliphatic and alicyclic series with 2 different equations corresponded well to the observed difference in the pharmacological properties between the both

Słowa kluczowe

EN

hypnotic-sedative agents; synthesis; SAR

• Wydawca: Polskie Towarzystwo Chemiczne
• Czasopismo: Polish Journal of Chemistry
• Rocznik: 2004
• Tom: Vol. 78 / nr 8
• Strony: 1027--1037
• Opis fizyczny: Bibliogr. 27 poz., rys.

Twórcy

autor

Chilmonczyk Z.

• Insitute of Chemistry, University of Białystok, 15-443 Białystok, Piłsudskiego 11/4, Poland
• National Institute of Public Health, 00-725 Warszawa, Chełmska 30/34, Poland

autor

Mazgajska M.

• Pharmaceutical Research Institute, 01-793 Warszawa, Rydygiera 8, Poland

autor

Chojnacka-Wójcik E.

• Institute of Pharmacology, Polish Academy of Sciences, 31-343 Krakow, Smêtna 12, Poland

autor

Tatarczyńska E.

• Institute of Pharmacology, Polish Academy of Sciences, 31-343 Krakow, Smêtna 12, Poland

autor

Kłodzińska A.

• Institute of Pharmacology, Polish Academy of Sciences, 31-343 Krakow, Smętna 12, Poland

autor

Ulman M.

• Insitute of Chemistry, University of Białystok, 15-443 Białystok, Piłsudskiego 11/4, Poland

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