Synthesis and Antihypertensive Activity of Some Novel Pyridazinones

Imran, Mohd; Nayeem, Naira

doi:10.13005/ojc/320129

Cited by 14 publications

(5 citation statements)

References 17 publications

(23 reference statements)

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“…The derivatives of pyridazinone have been investigated extensively in the control and management of various cardiovascular diseases [1,2]. Some of the pyridazinone derivatives are under various phases of clinical trials while some have been approved for clinical use [3,4,5,6,7].…”

Section: Introductionmentioning

confidence: 99%

“…Various derivatives of PPD have also been investigated as insecticidal [9], cardioprotective [7,10], analgesics [11,12], anti-inflammatory [12,13], antinociceptive [6], antiulcer [14] and antimicrobial agents [15] in the literature. In spite of various therapeutic activities of PPD derivatives, these compounds have a high toxicity and poor solubility in water and aqueous buffers [1,6]. The poor water solubility of PPD could be a major hurdle for its dosage form design.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, Characterization and Solubility Determination of 6-Phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents

et al. 2019

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The current research work proposed the solubility data and solution thermodynamic properties of the cardiovascular agent 6-phenylpyridazin-3(2H)-one [PPD] in twelve pharmaceutical solvents at “T = 298.2 K to 318.2 K” and “p = 0.1 MPa”. The measured solubilities of PPD were regressed well with “van’t Hoff and Apelblat models”. The solid phases of pure and equilibrated PPD were characterized using differential scanning calorimetry and powder X-ray differactometry, and the results suggested no transformation of PPD into solvates/hydrates/polymorphs after equilibrium. The solubilities of PPD in a mole fraction at “T = 318.2 K” were noted at a maximum in dimethyl sulfoxide (DMSO, 4.73 × 10−1), followed by polyethylene glycol-400 (PEG-400, 4.12 × 10−1), Transcutol® (3.46 × 10−1), ethyl acetate (EA, 81 × 10−2), 2-butanol (2.18 × 10−2), 1-butanol (2.11 × 10−2), propylene glycol (PG, 1.50 × 10−2), isopropyl alcohol (IPA, 1.44 × 10−2), ethylene glycol (EG, 1.27 × 10−2), ethanol (8.22 × 10−3), methanol (5.18 × 10−3) and water (1.26 × 10−5). Similar tendencies were also noted at other studied temperatures. The results of the “apparent thermodynamic analysis” showed an endothermic and entropy-driven dissolution of PPD in all pharmaceutical solvents. The results of the activity coefficients suggested a maximum interaction at the molecular level in PPD-DMSO, PPD-PEG-400 and PPD-Transcutol, compared with other combination of the solute and solvents.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Solubility Determination of 6-Phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents

et al. 2019

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“…Results indicated that compounds with structural features of the general formula 32 showed the maximum antihypertensive activity. Indeed, M. Imran et al, [37] synthesized four pyridazinone derivatives and molecular docking studies of these compounds was carried out on human angiotensin converting enzyme (ACE). Compound 33 exhibited the highest scores in docking study and so tested for ACE inhibitory activity using Dojindo ACE Kit-WST test kit and revealed promising activity (IC 50 = 5.78 µg/mL) compared to that of lisinopril (IC 50 = 0.85 µg/mL).…”

Section: Antihypertensive Activitymentioning

confidence: 99%

Pyridazinones and pyrrolones as promising Scaffolds in Medicinal Chemistry

Abdelbaset

Abdel‐Aziz

Abuo‐Rahma

et al. 2018

Journal of advanced Biomedical and Pharmaceutical Sciences

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Pyridazinones and pyrrolones are important building blocks for some important drugs such as the naturally occurring antibacterial pyrrolone, althiomycin; the cardiotonic pyridazinones, pimobendan and levosimendan and the analgesic anti-inflammatory, emorfozan. Therefore, researchers all over the world paid attention to prepare various pyridazinones and pyrroolones derivatives. The variability in the biological response and ease of preparation from the corresponding furanones attracted attention of researchers to explore these two nuclei in the design and synthesis of different analogues. This review article focuses on different biological activities, structure activity relationship and mechanism of action of pyridazinones and pyrrolones derivatives.

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“…Pyridazine-based compounds demonstrate diverse biological activities [6][7][8][9][10][11][12] , including COX-2 inhibitory activity 1,2 . Emorfazone (Pentoil) Fig.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Cyclooxygenase-2 Inhibitory Activity Evaluation of Some Pyridazine Derivatives

Imran,

Mohd,

Nayeem

et al. 2023

Orient. J. Chem

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This work aimed to discover safe and effective pyridazine-based cyclooxygenase-2 (COX-2) inhibitors. Thirty-three pyridazine-based compounds (compounds 1 to 33) were designed. The in silico studies were conducted to predict their toxicity, docking scores (DS), pharmacokinetic parameters, and drug-likeliness properties compared to celecoxib. Based on the safety and efficacy data obtained by in silico studies, four compounds (7, 12, 16, and 24) were synthesized, and the spectral analysis confirmed their chemical structures. Additionally, the in vitro COX-2 inhibitory activity of these four compounds was evaluated. Eleven compounds were predicted as non-toxic compounds. The DS of four compounds, 7 (DS = -9.72 kcal/mol), 12 (DS = -10.48 kcal/mol), 16 (DS = -9.71 kcal/mol), and 24 (DS = -9.46 kcal/mol), was better than celecoxib (DS = -9.15). These compounds (7, 12, 16, and 24) also demonstrated better oral absorption (83.53% each) than celecoxib (79.20%) in addition to their promising drug-likeliness properties. The compounds 7 (101.23%; p < 0.05), 12 (109.56%; p < 0.05), 16 (108.25%; p < 0.05), and 24 (103.90%; p < 0.05) also exhibited superior COX-2 inhibition to celecoxib (100%; p < 0.05). Compounds 7, 12, 16, and 24 are useful lead compounds in developing drugs for various diseases in which high levels of COX-2 are implicated.

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Synthesis and Antihypertensive Activity of Some Novel Pyridazinones

Cited by 14 publications

References 17 publications

Synthesis, Characterization and Solubility Determination of 6-Phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents

Synthesis, Characterization and Solubility Determination of 6-Phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents

Pyridazinones and pyrrolones as promising Scaffolds in Medicinal Chemistry

Synthesis and Cyclooxygenase-2 Inhibitory Activity Evaluation of Some Pyridazine Derivatives

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