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INVESTIGATIONS ON THE SYNTHESIS AND PROPERTIES OF 2-(ALKYL,ARYL)-1,4,5-TRI- OXO-1,2,3,4,5,6-HEXAHYDROPYRIDO- [3,4-D]- PYRIDAZINES DERIVATIVES WITH POTENTIAL BIOLOGOCAL ACTIVITY.

Jakub Stanasiuk 

Wroclaw Medical University, Department of Chemistry of Drugs, Tamka 1, Wrocław 50-137, Poland

Abstract

The studies of pyrido[3,4-d]pyridazine derivatives are a continuation of the former investigations of N-arylpiperazinylalkyl 1,4-dioxo(1,4,5-trioxo)-1,2,3,4-tetra( and 1,2,3,4,5,6-hexa)hydropyrido[3,4-d]pyridazines, which in pharmacological screening turned out to reduce spontaneous and amphetamine induced motility and display analgesic and antiserotonic activity. The continuation of the research in this field was due to the positive results of preliminary tests, in which some of the derivatives acquired through condensation of pyrido[3,4-d]pyridazine with 1,2,3-triazepine ring, and resulting formation of the triheterocyclic pyrido[2,3,4-ef]pyridazine[3,4-e]1,2,4-triazepine, appeared to have strong analgesic activity and no toxic effects (LD 50>2000 mg/kg). Our hitherto studies (chemical and biological) proved that many derivatives developed from bicyclic arrangements possess hipotensic, analgesic, anxiolytic and tuberculostatic activities. Exceptionally interesting and significant were the results of the tests for their antimycobacterial activity (TAACF) conducted at Colorado State University. These studies were based mainly on the chemical substances obtained in our department and encourage us to continue the synthesis of drugs from this group.

VMKNOL_1.GIF

References:

1. H. Śladowska, J. Stanasiuk, T. Saran, Z. Kleinrok, Farmako, 1998, 53 no 7
2. H. Śladowska, B. Filipek, Boll. Chim., 2004, 143, no 5.

This investigation was supported by grand No 1521.

 

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Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Jakub Stanasiuk
See On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2006-03-03 20:22
Revised:   2009-06-07 00:44