Synthesis, Biological Evaluation of Some 2,3-dihydropyrazoles and Thiazoles as Anti-inflammatory and Antibacterial Agents

Elgazwy, Abdel Sattar S Hamad

doi:10.4172/2161-0401.1000112

Cited by 7 publications

(5 citation statements)

References 67 publications

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“…Consequently, compounds 11, 14, and 18 were selected and tested against a panel of 60 different tumor cell lines at a 5 -log dose range [1][2][3][4][5].…”

Section: Methodsmentioning

confidence: 99%

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Synthesis and Antiproliferative Activity of 1-(4-(1H-Indol-3-Yl)-6-(4-Methoxyphenyl)Pyrimidin-2-yl)Hydrazine and Its Pyrazolo Pyrimidine Derivatives

Nassar¹,

Badry²,

Eltoukhy³

2016

Med chem

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“…Consequently, compounds 11, 14, and 18 were selected and tested against a panel of 60 different tumor cell lines at a 5 -log dose range [1][2][3][4][5].…”

Section: Methodsmentioning

confidence: 99%

“…Chalcones constitute an important group of natural products and are the precursors of flavonoids, isoflavonoids and many synthetic heterocycles of different biological activities including pyrimidines, pyrazolines, pyrazolopyrimidines and diazepines [1][2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antiproliferative Activity of 1-(4-(1H-Indol-3-Yl)-6-(4-Methoxyphenyl)Pyrimidin-2-yl)Hydrazine and Its Pyrazolo Pyrimidine Derivatives

Nassar¹,

Badry²,

Eltoukhy³

2016

Med chem

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“…The nitrogen-containing five-membered heterocycles-pyrrole, diazole, triazole, thiazole, thiadiazole, oxadiazole, benzimidazole demonstrate a wide diversity of biological properties. Thiazoles are commonly reported as active antimicrobial [1][2][3][4][5][6][7][8], anti-tuberculous [9][10][11][12], anti-HIV [13], antiviral [14,15], antihistamine [16,17], antipyretic [18], antitumor [3,19], antidepressant [20], fungicidal [21,22] property bearing compounds. 2-Aminothiazoles has found application in agriculture as herbicides and fungicides [23,24].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Bioassay of Novel Substituted 1-(3-(1,3-Thiazol-2-yl)phenyl)-5-oxopyrrolidines

Sapijanskaitė-Banevič

Šovkovaja

Vaickelionienė

et al. 2020

Molecules

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Thiazole derivatives attract the attention of scientists both in the field of organic synthesis and bioactivity research due to their high biological activity. In the present study, thiazole ring was obtained by the interaction of 1-(4-(bromoacetyl)phenyl)-5-oxopyrrolidine-3-carboxylic acid with thiocarbamide or benzenecarbothioamide, as well as tioureido acid. A series of substituted 1-(3-(1,3-thiazol-2-yl)phenyl)-5-oxopyrrolidines with pyrrolidinone, thiazole, pyrrole, 1,2,4-triazole, oxadiazole and benzimidazole heterocyclic fragments were synthesized and their antibacterial properties were evaluated against Gram-positive strains of Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes and Gram-negative Pseudomonas aeruginosa, Escherichia coli and Salmonella enterica enteritidis. The vast majority of compounds exhibited between twofold and 16-fold increased antibacterial effect against the test-cultures when compared with Oxytetracycline.

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“…For example, "antipyrine", "analgin", "amidopyrine" are successfully used in the medical practice as anti-inflammatory and antipyretic agent; "pyramidon" -as analgesic agent; "celebrex" as a pain relief in joints, etc. [1][2][3][4][5]. In addition, the pyrazole derivatives are also used in fine organic synthesis, supramolecular and polymer chemistry; in the preparation of liquid crystals and agrochemical preparations [6][7][8][9].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Conversion of Pyrazole Derivatives

Karayeva¹

2019

Chemical Problems

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The new representatives of functionally substituted pyrazoles were synthesized and their interactions with secondary amines studied. It found that the interaction of 3,4-bis(diethylamino)but-2en-1-ones with hydrazine hydrate gave rise to 3-alkyl-5-(diethylaminomethyl)pyrazoles. Appropriate 1acetyl and 1-(2-chloromethyl carbonyl)pyrazoles were synthesized through the acylation of the last products with acetyl-and monochloroacetyl chloride in the presence of triethylamine. It revealed that 1-(2-chloromethyl carbonyl)pyrazoles react with twofold quantity of diethylamine and morpholine under mild reaction conditions to form new polyfunctional pyrazole derivatives. The composition and structure of the synthesized compounds were confirmed by IR-and NMR 1 Н-spectroscopy. It established that 3-methyl-and 3-ethyl-5-(diethylaminomethyl) pyrazoles were biologically active substances out of synthesized functionally pyrazole derivatives.

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Synthesis, Biological Evaluation of Some 2,3-dihydropyrazoles and Thiazoles as Anti-inflammatory and Antibacterial Agents

Cited by 7 publications

References 67 publications

Synthesis and Antiproliferative Activity of 1-(4-(1H-Indol-3-Yl)-6-(4-Methoxyphenyl)Pyrimidin-2-yl)Hydrazine and Its Pyrazolo Pyrimidine Derivatives

Synthesis and Antiproliferative Activity of 1-(4-(1H-Indol-3-Yl)-6-(4-Methoxyphenyl)Pyrimidin-2-yl)Hydrazine and Its Pyrazolo Pyrimidine Derivatives

Synthesis, Characterization and Bioassay of Novel Substituted 1-(3-(1,3-Thiazol-2-yl)phenyl)-5-oxopyrrolidines

Synthesis and Conversion of Pyrazole Derivatives

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