ChemInform Abstract: Investigations on the Synthesis and Properties of N‐Aryl(heteroaryl) piperazinylalkyl Derivatives of Imide of 6‐Methyl‐2‐(1‐piperidino)‐3,4‐ pyridinedicarboxylic Acid.

Abstract

Investigations on the Synthesis and Properties of N-Aryl(heteroaryl) piperazinylalkyl Derivatives of Imide of 6-Methyl-2-(1-piperidino)-3,4-pyridinedicarboxylic Acid.-In the search for new chemical compounds with analgesic and antidepressant activities the title compounds are synthesized and tested. -(SLADOWSKA, H.; SIEKLUCKA-DZIUBA, M.; MISZTAL, M.; KLEINROK, Z.; Farmaco, Ed. Sci. 49 (1994) 7-8, 493-498; Dep. Chem. Drugs, Sch. Med., PL-50-137 Wroclaw, Pol.; EN)

Synthesis and thermal study of new N-substituted 1H-pyrrolo[3,4-c]pyridine-1,3(2H)diones of Mannich base type

“…1). A 0.5 g (0.002 mol) of 4-methoxy or 4-ethoxy-2,3-dihydro-6-methyl-1,3-dioxo-1H-pyrrolo [3,4-c]pyridine was dissolved in 40 cm 3 of tetrahydrofurane and to this solution 1 cm 3 of 33% formaline was added. The mixture was refluxed for 0.5 h. After the time 0.0022 mol of the suitable amine (4-benzylpiperazine or 4-(2-phenylethyl)piperazine) were added, again refluxed for 10 h. Then the solvents were evaporated completely under reduced pressure.…”

“…It was reported previously that the derivatives of 3,4-pyridinedicarboximide cause in animal tests significant analgesic activity and do not display any noticeable toxic effects (LD 50 [ 2000 mg/kg) [1][2][3]. Over the last decade, many similar compounds with structural modifications have been synthesised.…”

An Overview of the Biological Activity of Pyrrolo[3,4-c]pyridine Derivatives

“…While conducting studies on pyrrolo[3,4- c ]pyridines to obtain new anxiolytic derivatives of the buspirone type, Śladowska’s team noticed that these compounds are often not active in this regard. Instead, they show other pharmacological effects, in particular, sedative [ 27 ] and analgesic activity [ 27 , 28 , 29 ]. The analgesic activity of the new pyrrolo[3,4- c ]pyridines is described in the following section.…”

“…Taking into account the results of previous work [ 28 , 29 ], in 1994, the above researchers obtained a series of nine new N-substituted piperazinalkyl derivatives of 6-methyl-2-(1-piperidine)-pyridine-1,3-dione ( Figure 20 ) [ 27 ].…”

Synthesis and DSC study a new pyridinedicarboximide diones derivatives, obtained under various conditions

“…Some of them were tested in the pharmacological screening test, and they have showed both the analgesic and antidepressant activities, but not the anxiolytic ones [8]. Some of these derivatives significantly suppress spontaneous locomotor activity in mice, cause hypothermia in normothermic mice, significantly decrease their amphetamine-induced hyperactivity as well as display weak analgesic action [9]. During the further research on these derivates, the structure of 1H-pyrrolo [3,4-c]pyridine-1,3(2H)-diones have been modified.…”