Synthesis and Anticonvulsant Activity of Novel 1-Substituted-1,2-dihydro-pyridazine-3,6-diones

Abstract

The synthesis and pharmacological evaluation of novel 1-substituted-1,2-dihydro-pyridazine-3,6-diones (4a-l, 5a-j) as potential anticonvulsant agents are described. The compounds were tested in vivo for the anticonvulsant activity. The compound which have maximum protection against MES induced seizures is 1-[3-(2-aminophenylamino)-2-hydroxypropyl)-1,2-dihydro-pyridazine-3,6-dione 4h (ED 50 ‫7.44؍‬ mg · kg ؊1 i.p.) 1-[2-hydroxy-3-piperazin1-yl-propyl)-1,2-dihydro-pyridazine-3,6-dione 4c (ED 50 ‫27؍‬ mg · kg ؊1 i.p.) and 1-[2-hydroxy-3-imidazol-1-yl-propyl)-1,2-dihydro-pyridazine-3,6-dione 4d (ED 50 ‫97؍‬ mg · kg ؊1 i.p.) were also found to have maximum protection against MES induced seizures. Whereas all these compounds failed to protect the animals from subcutaneous pentylenetetrazole (Metrozol) seizure threshold test (sc-Met).

Synthesis, Anticonvulsant and Antihypertensive Activities of 8-Substituted Quinoline Derivatives

“…The increase in the carbon atom number at the 4th position of piperazine influenced the activity remarkably. In the propanol series (12)(13)(14)(15)(16)(17)(18)(19)(20), only compounds 13, 14, 19 and 20 were found to have a high degree of protection against MES-induced convulsions. 4-phenylpiperazino substituted compounds at the 3Ј position showed higher protection than the other substitutions at piperazine compounds.…”

“…We have already reported the potential anticonvulsant activity and the b-blocking activity of propanolamine, aminopropane and aminoethane from our laboratory. [14][15][16][17][18][19][20] To explore the heteroaryl and propanolamine/aminoethane combination, it was envisaged that chemical entities with both quinoline and aryloxypropanolamine/aminoethane moieties would result in compounds with interesting biological activities.…”

Current Research on Antiepileptic Compounds

“…The compound which have maximum protection against MES-induced seizures was compound 195 with ED 50 = 44.7 mg/kg i.p. 4 h (Table 10) [157]. value of 8.3 mg/kg and PI value of 5.5, but compound 216 exhibited better PI value of 9.3 ( Figure 12), which was much greater than PI value of the prototype drug phenytoin [168].…”

Synthesis and Antitubercular Activity of Pyridazinone Derivatives

“…The compounds, 1 and 2, were synthesized according to the reported method [14]. (3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18). Compounds (3-18) were synthesized from 3-(4-chloro/methyl benozyl) propionic acid (1,2) following literature method [14].…”

“…Differently substituted pyridazinones have been found to have potential antibacterial, antifungal and antiviral including anti-HIV activities [1][2][3][4]. Various 3-(2H)-pyridazinone derivatives have shown anticancer [4], analgesic & anti-inflammatory [4][5][6], anticonvulsant [7], cardiotonic & hypotensive [8,9] and antiulcer activities [10].…”