127806-52-4Relevant articles and documents
Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents
Partap, Sangh,Yar, Mohammad Shahar,Hassan, Md. Zaheen,Akhtar, Md. Jawaid,Siddiqui, Anees A.
, (2017/10/06)
A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models. Among the compounds tested, SS-4F showed significant anticonvulsant activity in both the screens with ED50 values of 25.10 and 85.33 mg/kg in the MES and scPTZ screens, respectively. Compound SS-4F emerged as safer and effective anticonvulsant due to its several-fold higher protective indices. Further, the gamma-aminobutyric acid (GABA) estimation result showed a marked increase in the GABA level (1.7-fold) as compared to the control, which was further confirmed by good binding properties with the GABAA receptor.
Synthesis and antimicrobial activity of some novel oxadiazole derivatives
Islam, Mojahidul,Siddiqui, Anees A.,Rajesh, Ramadoss,Bakht, Afroz,Goyal, Sunil
experimental part, p. 441 - 447 (2009/04/07)
A series of 5-{3′-oxo-6′-(substituted aryl)-2′,3′, 4′,5′-tetrahydropyridazin-2′-ylmethyl}-2-substituted 1,3,4-oxadiazole has been synthesized. Appropriate aromatic hydrocarbon reacts with succinic anhydride in the presence of AlCl3 to yield β-aroyl propionic acid (1a). The corresponding acid is cyclized with hydrazine hydrate to give 6-(substituted aryl)-2,3,4,5-tetrahydro-3-pyridazinone (1b).This ntermediate after reaction with ethyl bromoacetate, was hydrazinolyzed into 3-oxo-6-(substituted aryl)-2, 3, 4, 5-tetrahydropyridazinyl acetohydrazide (1c).The resulting product was converted into 5-{3′-oxo-6′-(substituted aryl)-2′,3′,4′,5′- tetrahydropyridazin-2′-ylmethyl]-2-substituted 1,3,4-oxadiazole (Scheme 1). All the final compounds were structurally elucidated on the basis of IR, 1H-NMR, MS data and elemental analysis and screened for antibacterial, antifungal and antitubercular activity. All the compounds are evaluated for their antibacterial activity against E. coli, S. aureus, Miavcoccus luteus and Klebsiella pneumoniae by using cup plate technique in the nutrient agar at 100 μg/mL concentration. Antitubercular activity was determined using the BACTEC 460 system. Stock solutions of test compounds were prepared in DMSO. MIC of rifampin was calculated by established procedures.All the synthesized compounds were screened at 6.25 μg/mL against M. tuberculosis H37 Rv comparable with that of standard rifampicin and isoniazid. All the final compounds were evaluated for antifungal activity against C. albicans and C. neoformans by using cup-plate method in the Sabouraud agar media The zone of inhibition (mm) of each compound was determined and compared with standard drug fluconazole.
Synthesis and pharmacology of 3-aryl-5,6-dihydro-6-oxo-1(4H)-pyridazineacetic acid derivatives
Kane,Huber,Miller,Kehne
, p. 249 - 251 (2007/10/02)
The title compounds were prepared by alkylation of 6-aryl-4,5-dihydro-3(2H)-pyridazinones with esters of α-bromoacetic acid. Hydrolysis of these esters afforded the corresponding carboxylic acids which were coupled with various amines yielding 6-oxo-1(4H)
