ChemInform Abstract: 3,5‐Diphenyl‐1H‐pyrazole Derivatives. Part. 1. Esters and N‐Substituted Carbamates of 1‐(2‐Hydroxyethyl)‐3,5‐diphenyl‐1H‐pyrazole and Its 4‐Bromo Derivative with Depressant, Antiarrhythmic, Analgesic, and Other Activities.

Bondavalli, Francesco; Bruno, Olga; Ranise, Angelo; Schenone, P; Addonizio, P.; Novellis, Vito de; Loffreda, A.; Marmo, E

doi:10.1002/chin.198912181

Cited by 3 publications

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“…Among the organic compounds, aza-heterocycles such as pyrazole and indazole derivatives, which present considerable biological importance, 1,2 are embedded in a wide range of natural products and medicinal synthetic compounds exerting anti-aggregatory, 3 anti-arrhythmic, 4 muscle relaxing, 5 and anti-diabetic activities. 6 For example, Celecoxib is a pyrazole derivative used as an analgesic.…”

Section: Introductionmentioning

confidence: 99%

A Modified and Practical Synthetic Route to Indazoles and Pyrazoles Using Tungstate Sulfuric Acid

Rahmatzadeh

Karami

Khodabakhshi³

2014

J Chinese Chemical Soc

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Tungstate sulfuric acid-catalyzed Knorr reaction have been used as a simple, rapid, atom economic and green method for the synthesis of indazole and pyrazole derivatives based on the condensation of hydrazine derivatives and b-dicarbonyl compounds under solvent-free conditions. It was found that the catalyst could be recovered and reused without significant loss of its activity. The use of this method provides a novel and improved modification of Knorr synthesis in terms of clean reaction profile, use of a safe catalyst and solvent-free conditions.

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Section: Introductionmentioning

confidence: 99%

A Modified and Practical Synthetic Route to Indazoles and Pyrazoles Using Tungstate Sulfuric Acid

Rahmatzadeh

Karami

Khodabakhshi³

2014

J Chinese Chemical Soc

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“…One of the important heterocyclic structure, pyrazoles have attracted the attention of organic chemists in recent years due to their wide biological activity properties. Compounds containing pyrazole nucleus are known to have analgesic, anti-inflammatory, antipyretic, antiarrhythmic, muscle relaxant, psychoanaleptic, anticonvulsant, hypotensive, antidiabetic and antibacterial activities (10)(11)(12)(13)(14)(15)(16). The yield, which is one of the problems experienced in the field of synthetic organic chemistry, has an important place in modern drugs discovery.…”

Section: Introductionmentioning

confidence: 99%

Microwave and ultrasound promoted greener synthesis of thiazolyl-pyrazoline derivatives and investigation of their biological activities

Mermer

2020

Journal of the Turkish Chemical Society Section A: Chemistry

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Six thiazolyl-pyrazoline derivatives were synthesized starting from corresponding chalcone compounds for their antioxidant capacity and antiurease inhibitory activities. In addition to the conventional method, ultrasonic sonication and microwave irradiation methods which are environmental methods were used in the synthetic stage. Compound 2-(5-(3-bromophenyl)-3-phenyl-4,5-dihydro-1Hpyrazol-1-yl)-4-phenyl thiazole (5a) exhibited the most potent antiurease activity with IC50 of 2,28±0,02, which was comparable to the positive control.

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“…8 In the same sense, compounds including a pyrazole nucleus are known to possess analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxant, psychoanaleptic, anticonvulsant, hypotensive, monoamine oxidase inhibitor, antidiabetic, and antibacterial activities. [9][10][11][12][13][14][15][16] Also, some thiazole derivatives have been reported to possess tuberculostatic, antibacterial, and antifungal activities. 17 Moreover various sulfur compounds have been found to have other biological properties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Characterization of Some New Heterocycles Incorporating the 1-Phenyl-5-(2-thienyl)pyrazole Moiety

Abdel‐Wahab

El-Ahl

2010

Phosphorus, Sulfur, and Silicon and the Related Elements

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1-Phenyl-3-(2-thienyl)-1H-pyrazole-5-carbohydrazide 4 was prepared from 2-acetylthiophene by reaction with diethyl oxalate and phenylhydrazine followed by hydrazine hydrate. The reaction of the hydrazide 4 with phthalic anhydride, aromatic aldehydes, and alkene derivatives gave imide 5, hydrazones 6a-d, and bis-pyrazoles 7 and 8, respectively, while its reaction with phenyl isothiocyanate led to thiosemicarbazide 9. The reaction of the latter with ethyl bromoacetate and phenacylbromide afforded 4-thiazolidinone 10 and 1,3-thiazole 11 derivatives, respectively. Reaction of 4 with carbon disulfide in the presence of potassium hydroxide gave potassium hydrazinecarbodithioate derivative 12, which was used as a starting material in the preparation of 2-thioxothiazol-3(2H)-yl)-5-(2-thienyl)-1H-pyrazole-3-carboxamide 14; 1,3,4-thiadiazol-2(3H)-ylidene)-1-phenyl-5-(2-thienyl)-1H-pyrazole-3-carbohydrazides 16a-c; 4-amino-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)pyrazole derivative 13; Schiff bases 17a,b; and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine derivatives 18 and 19a-e.

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ChemInform Abstract: 3,5‐Diphenyl‐1H‐pyrazole Derivatives. Part. 1. Esters and N‐Substituted Carbamates of 1‐(2‐Hydroxyethyl)‐3,5‐diphenyl‐1H‐pyrazole and Its 4‐Bromo Derivative with Depressant, Antiarrhythmic, Analgesic, and Other Activities.

Abstract: Chalcone (I) is transformed into the epoxide (II) which undergoes cyclocondensation with hydrazinoethanol (III), yielding the pyrazoline (IV).

Cited by 3 publications

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A Modified and Practical Synthetic Route to Indazoles and Pyrazoles Using Tungstate Sulfuric Acid

A Modified and Practical Synthetic Route to Indazoles and Pyrazoles Using Tungstate Sulfuric Acid

Microwave and ultrasound promoted greener synthesis of thiazolyl-pyrazoline derivatives and investigation of their biological activities

Synthesis and Characterization of Some New Heterocycles Incorporating the 1-Phenyl-5-(2-thienyl)pyrazole Moiety

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