Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates

Chikhale, Rupesh; Bhole, Ritesh P.; Khedekar, Pramod B.; Bhusari, Kishore P.

doi:10.1016/j.ejmech.2009.02.021

Cited by 99 publications

(35 citation statements)

References 20 publications

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“…18 Those compounds, which showed good results in antiinflammatory and analgesic activity, were screened for their ulcerogenic activity. The tested compounds exhibited activity in the range of 0.14 to 0.56, whereas standard drug indomethacin presented very high severity index of 1.25.…”

Section: Resultsmentioning

confidence: 99%

“…18 Sprague Dawley rats were used for this study; seventeen groups with six rats per group were formed. All test samples were administered to animals at 100 mg kg −1 dosage, as suspension in 0.5% carboxymethyl cellulose in water.…”

Section: Anti-inflammatory Activitymentioning

confidence: 99%

“…Gastric mucosa of the rats was examined by means of a four times binocular magnifier and the lesions were counted according to earlier reported method. 18 Accordingly, the mean score of each treated group minus the mean score of the control group was considered to determine the severity index of gastric damage for compounds under study.…”

Section: Ulcerogenic Activitymentioning

confidence: 99%

“…13 In the past, many indole and 1,3,4-oxadiazole derivatives showed potential for anti-inflammatory and analgesic activity in animal model of inflammation and pain. [14][15][16][17][18] Compound The need for newer drug molecule and success of hybrid approach compelled us for development of some new NSAIDs. The target moieties selected for formation of a hybrid drug was based on our previous literature study, and it was found that indole and oxadiazole nuclei possess analgesic and anti-inflammatory properties and thus it was found worth to prepare a hybrid derivative from these moieties.…”

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, Pharmacological Evaluation and Molecular Docking Studies of Substituted Oxadiazolyl-2-Oxoindolinylidene Propane Hydrazide Derivatives

Kerzare¹,

Chikhale²,

Bansode³

et al. 2016

Journal of the Brazilian Chemical Society

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The manuscript describes design and synthesis of novel oxadiazolyl-2-oxoindolinylidene propane hydrazides as amide tethered hybrids of indole and oxadiazole and their evaluation for antiinflammatory and analgesic activity. The compounds were synthesized following five step reaction to yield fifteen derivatives as 3- (5-propane hydrazide and 3-[5-(4-methylphenyl)-1,3,4-oxadiazol-2-yl]-N'-[2-oxo-1,2-dihydro-3H-indol-3-ylidene]propane hydrazide were found to be highly promising molecules with severity index of 0.35 and 0.56, respectively, which is promising for an analgesic compound. The hydroxy and methyl substitution on phenyl ring system provided with active anti-inflammatory compounds having increase in reaction time of 84.11 and 83.17%, respectively compared to standard drug at 85.84%. Molecular docking studies exhibit comparable interaction with synthesized derivatives and standard drug having a dock score of −4.44 by the K-nearest neighbour genetic algorithm method.

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Section: Resultsmentioning

confidence: 99%

Section: Anti-inflammatory Activitymentioning

confidence: 99%

Section: Ulcerogenic Activitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, Pharmacological Evaluation and Molecular Docking Studies of Substituted Oxadiazolyl-2-Oxoindolinylidene Propane Hydrazide Derivatives

Kerzare¹,

Chikhale²,

Bansode³

et al. 2016

Journal of the Brazilian Chemical Society

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“…Hence, they are classified as one of the most important groups of drug like scaffold. [4][5][6][7] A recent emphasis in this perspective has been the identification of the structurally simple DHPM derivative viz., monastrol as a mitotic kinesin Eg5 motor protein inhibitor for the development of anticancer drugs. 8 The great potential of DHPMs in biological and pharmaceutical fields has accordingly triggered growing interest in their synthetic study.…”

Section: Introductionmentioning

confidence: 99%

A Convenient One-Pot Biginelli Reaction Catalyzed by Y(OAc)₃: An Improved Protocol for the Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones and Their Sulfur Analogues

Aridoss¹,

Jeong

2010

Bulletin of the Korean Chemical Society

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Yttrium(III) acetate hydrate-catalyzed novel synthesis of 3,4-dihydropyrimidin-2(1H)-(thio)one derivatives was achieved through one-pot three-component condensation of diversified aldehydes, β-ketoesters and urea or N-methylurea or thiourea with a molar ratio of 1:1:1.4. In comparison to the classical Biginelli approach, this catalytic method has the advantages of short reaction time and improved product yield.

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Tailoring of Novel Ru (III) and Cr (III) Salen Complexes as Catalysts for a Sustainable and Green Synthesis of Dihydro‐tetrazolo [1,5‐a] thiazolo [4,5‐d] pyrimidin‐6‐yl morpholine: Experimental and Theoretical Approaches

El‐Remaily,

Eskander,

Alzahrani

et al. 2024

Applied Organom Chemis

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Two novel Cr (III) and Ru (III) salen complexes based on {3,4‐Bis‐[(5‐chloro‐2‐hydroxy‐benzylidene)‐amino]‐phenyl}‐phenyl‐methanone ligand (CSAB) were synthesized. The complexes were characterized using various spectral and analytical methods. The catalytic performance of the CSAB complexes was investigated via a four‐component condensation reaction involving aromatic aldehydes, rhodamine, morpholine, and 5‐aminotetrazole under mild, environmentally friendly conditions. Different Lewis acids, bases, ionic liquid catalysts, solvents, and catalyst amounts were assessed to optimize the reaction parameters. Both catalyst systems demonstrated robust catalytic activity under strictly managed conditions, with the heterogeneous catalyst CSAB‐Ru showing superior efficacy compared to the homogeneous CSAB‐Cr catalyst. The study confirmed the catalytic capabilities of both complexes and evaluated their recyclability and reusability. The heterogeneous catalyst (CSAB‐Ru) could be reused seven times, whereas the homogeneous catalyst (CSAB‐Cr) could be recycled four times. Both complexes demonstrated strong catalytic activity and selectivity, resulting in high product yields. The study provides insights into the synthetic applications of novel CSAB complexes, highlighting their potential in organic transformations. It emphasizes their ease of use, safety, stability, component availability, quick reaction times, and high yields, making them promising for future industrial applications.

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Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates

Cited by 99 publications

References 20 publications

Design, Synthesis, Pharmacological Evaluation and Molecular Docking Studies of Substituted Oxadiazolyl-2-Oxoindolinylidene Propane Hydrazide Derivatives

Design, Synthesis, Pharmacological Evaluation and Molecular Docking Studies of Substituted Oxadiazolyl-2-Oxoindolinylidene Propane Hydrazide Derivatives

A Convenient One-Pot Biginelli Reaction Catalyzed by Y(OAc)₃: An Improved Protocol for the Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones and Their Sulfur Analogues

Tailoring of Novel Ru (III) and Cr (III) Salen Complexes as Catalysts for a Sustainable and Green Synthesis of Dihydro‐tetrazolo [1,5‐a] thiazolo [4,5‐d] pyrimidin‐6‐yl morpholine: Experimental and Theoretical Approaches

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Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates

Cited by 99 publications

References 20 publications

Design, Synthesis, Pharmacological Evaluation and Molecular Docking Studies of Substituted Oxadiazolyl-2-Oxoindolinylidene Propane Hydrazide Derivatives

Design, Synthesis, Pharmacological Evaluation and Molecular Docking Studies of Substituted Oxadiazolyl-2-Oxoindolinylidene Propane Hydrazide Derivatives

A Convenient One-Pot Biginelli Reaction Catalyzed by Y(OAc)3: An Improved Protocol for the Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones and Their Sulfur Analogues

Tailoring of Novel Ru (III) and Cr (III) Salen Complexes as Catalysts for a Sustainable and Green Synthesis of Dihydro‐tetrazolo [1,5‐a] thiazolo [4,5‐d] pyrimidin‐6‐yl morpholine: Experimental and Theoretical Approaches

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A Convenient One-Pot Biginelli Reaction Catalyzed by Y(OAc)₃: An Improved Protocol for the Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones and Their Sulfur Analogues