Design, synthesis and antihypertensive screening of novel pyridazine substituted s-triazin-2-imine/one/thione derivatives

Mishra, Ravinesh; Siddiqui, Anees A.; Husain, Asif; Rashid, Mohd; Goda, Chirag

doi:10.3109/14756366.2012.656623

Cited by 8 publications

(3 citation statements)

References 19 publications

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“…The pyridazine ring is an important structural feature in a number of pharmaceutical compounds, such as hydralazine (brand name Apresoline, vasodilator, US, FDA), cefozopran (anti-bacterial agent, Japan), and pipofezine (brand name Azafen or Azaphen, antidepressant, STADA, Nizhny Novgorod, Russia). Pyridazine derivatives have been reported to possess various pharmacological activities and intermediates for drugs synthesis, including antimicrobial, analgesic, anticancer, antitubercular, antidiabetic, antifungal, antihypertensive, anticonvulsant, anti-HIV, antiasthma, anti-inflammatory, phosphodiesterase (PDE) inhibitors, cyclooxygenase (COX) inhibitors, antipyretic, insecticidal, and neurological [66,67,68,69,70,71,72,73]. The reaction of arylazo 10d and ethylacetoacetate 11b in either acetic acid or ethanolic KOH, followed by reflux to afford pyridazinones 15d , has been reported.…”

Section: Resultsmentioning

confidence: 99%

Glycerol and Q-Tubes: Green Catalyst and Technique for Synthesis of Polyfunctionally Substituted Heteroaromatics and Anilines

AlMarzouq

Elnagdi

2019

Molecules

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The role of glycerol as a green bio-based solvent, reactant, and/or a catalyst in the synthesis of novel heterocycles, under pressure, is studied. Synthesis of novel quinolines in good yields using a new modified Skraup synthesis, utilizing glycerol and pressure Q-tubes, is demonstrated. Novel aniline trimers are prepared using glycerol, and substituted anilines under pressure, in acidic medium and water. Glycerol was employed as a catalyst and a green solvent in the synthesis of novel pyridazines 13a–c. The mechanisms of the reactions and the catalytic effect of glycerol in protic and aprotic media are fully discussed. The structures of the synthesized compounds were determined via X-ray crystallography and spectroscopic methods.

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Section: Resultsmentioning

confidence: 99%

Glycerol and Q-Tubes: Green Catalyst and Technique for Synthesis of Polyfunctionally Substituted Heteroaromatics and Anilines

AlMarzouq

Elnagdi

2019

Molecules

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“…as the minaprine, hydralazine, pipofezine, cefozopran, and so on. The derivatives of the Pyridazine were found to be having a variety of pharmacological activities, which include the antibacterial [13][14][15][16] anti-fungal, anti-tubercular [17][18][19] anticonvulsant, 20,21 antihypertensive, 22 anti-inflammatory, and analgesic. 23,24…”

Section: Research Articlementioning

confidence: 99%

Synthesis, Characterization and Evaluation of the Antibacterial Activity of Some Heterocyclic Compounds

Mohan¹,

Jassim²

2022

IJDDT

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This work includes preparing various heterocyclic compound types, which include the phthalazin, pyridazin, pyrazol, phthalazin-3,8-dione [5] and pyridazin-3,6-dione [6] derivatives which derived from hydrazide compound [3]. The structures of those compounds have been identified by the fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR) spectroscopy and checked with the use of the TLC technique, and evaluated the antibacterial activities for some of the synthesized compounds. Those activities have been characterized in vitro using the well diffusion approach against three types of the pathogenic strains of the bacteria Escherichia coli and Pseudomonas (G-) and S. aureus (G+). Results have shown that some of those compounds have shown good activity.

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“…Pyrazole and their derivatives possess a wide range of bioactivities. − Pyridazine and their analogues were thought worthwhile to study because they are available as a number of marketed drugs such as Hydralazine, Minaprine, and Cefozopran . It has also been reported that pyridazine derivatives display anticancer, anti-HIV, antihypertensive, antimicrobial, and antifungal activities. − …”

Section: Introductionmentioning

confidence: 99%

Serendipitous Formation of 2H-Pyrazolo[3,4-d]pyridazin-7(6H)-ones from 3-Arylsydnones

et al. 2019

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Fused nitrogen heterocyclesnamely, pyrazolo[3,4- d ]pyridazin-7(6 H )-ones have been obtained by exploiting the 1,3-dipolar nature of N -arylsydnones, from hydrazones of 3-aryl-4-acetylsydnones via the Vilsmeier–Haack strategy. Facile intramolecular nucleophilic addition followed by CO 2 elimination under reflux or upon microwave irradiation was presented. Plausible mechanisms for the formation of the title compounds are proffered. Structure confirmatory evidence came from single-crystal X-ray crystallography.

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Design, synthesis and antihypertensive screening of novel pyridazine substituted s-triazin-2-imine/one/thione derivatives

Cited by 8 publications

References 19 publications

Glycerol and Q-Tubes: Green Catalyst and Technique for Synthesis of Polyfunctionally Substituted Heteroaromatics and Anilines

Glycerol and Q-Tubes: Green Catalyst and Technique for Synthesis of Polyfunctionally Substituted Heteroaromatics and Anilines

Synthesis, Characterization and Evaluation of the Antibacterial Activity of Some Heterocyclic Compounds

Serendipitous Formation of 2H-Pyrazolo[3,4-d]pyridazin-7(6H)-ones from 3-Arylsydnones

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