ChemInform Abstract: Azoles. Part 17. β‐(4‐Pyrazole)acrylic and ‐propionic Acid and Their Antiinflammatory Activity.

Bernard, Marek K.; Hulley, Elliott B.; Molenda, H.; Stochla, K; Wrzeciono, U.

doi:10.1002/chin.198702170

Cited by 11 publications

(16 citation statements)

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“…The key intermediate 3-(5-bromo-2-thienyl)-1-phenyl-1H-pyrazole-4-carboxaldehyde 1 was prepared by applying the Vilsmeier-Haack reaction [16,19].The desired series of compounds 2 was synthesized starting by the reaction of 1 with either L-serine in the presence of 2N NaOH at 5°C for 24 h [20], or with Lcysteine or L-penicillamine under reflux in aqueous ethanol [21], followed by N-protection [22] using (Boc) 2 O. Compounds 2 were either subjected to N-deprotection using 4N HCl/dioxane giving rise to series 3 or allowed to react with NH 4 OH in the presence of DCC/HOBt to afford the corresponding amides 4.The latter series upon subjected to N-deprotection afforded series 5.…”

Section: Chemistrymentioning

confidence: 99%

Design and Synthesis of Some Substituted 1H‐Pyrazolyl‐oxazolidines or 1H‐Pyrazolyl‐thiazolidines as Anti‐inflammatory‐Antimicrobial Agents

Bekhit

Fahmy

2003

Archiv der Pharmazie

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Four series of 1 H-pyrazole derivatives have been synthesized. The first series was synthesized starting with the reaction of 3-(5-bromo-2-thienyl)-1-phenyl-1 H-pyrazole-4-carboxaldehyde 1 with L-serine, L-cysteine, or L-penicillamine, followed by N-protection using (Boc)(2)O to provide compounds 2. The latter compounds could be N-deprotected by 4N HCl/dioxane to afford the second series 3 or reacted with NH(4)OH in the presence of DCC/HOBt to give the corresponding amides 4 followed by N-deprotection giving rise to compounds 5. The newly synthesized compounds were evaluated for their anti-inflammatory-antimicrobial activities. In addition, the ulcerogenic and acute toxicity profiles were determined. Compound 5b (2RS, 4R)-2-[3-(5-bromo-2-thienyl)-1-phenyl-1H-pyrazol-4-yl]-5-methylthiazolidine-4-carboxamide, proved to be the most active anti-inflammatory-antimicrobial agent in the present study with a good safety margin and no ulcerogenic effect.

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Section: Chemistrymentioning

confidence: 99%

Design and Synthesis of Some Substituted 1H‐Pyrazolyl‐oxazolidines or 1H‐Pyrazolyl‐thiazolidines as Anti‐inflammatory‐Antimicrobial Agents

Bekhit

Fahmy

2003

Archiv der Pharmazie

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“…In this investigation, reaction of biphenyl methyl ketone phenyl hydazone (1) with phosphorus oxychloride in dimethylformamide (DMF) at 0 C afforded 3-(biphenyl-4-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde (2) in 90% yield. The synthesis of the pyrazole-4-carbaldehyde derivative 2 was carried out according to reported methods [40,41] by applying the Vilsmeier-Haack reaction. The formylating agent, also known as the Vilsmeyer-Haack Reagent, is formed in situ from DMF and phosphorus oxychlorid.…”

Section: Resultsmentioning

confidence: 99%

“…The bacteria and fungi were maintained on nutrient agar and Czapek's-Dox agar media, respectively. The assay medium flasks containing 50mL of nutrient agar for bacteria and Czapek's-Dox agar medium for fungi respectively were allowed to reach [40][41][42][43][44][45][46][47][48][49][50] C to be inoculated with 0.5 mL of the test organism cell suspension.…”

Section: -{[[3-(biphenyl-3-yl)-1-phenyl-1h-pyrazol-4-yl]methylene]-hmentioning

confidence: 99%

Synthesis and antimicrobial activity of substituted [(pyrazol‐4‐yl)methylene]hydrazono‐2,3‐dihydrothiazoles and their sugar derivatives

Abdel‐Rahman¹,

El‐Sayed²,

Zaki³

et al. 2011

Journal of Heterocyclic Chem

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A number of new [(pyrazol-4-yl)methylene]hydrazono-2,3-dihydrothiazole derivatives, their sugar hydrazones and N-glycosides were synthesized. Furthermore, N-substituted oxygenated alkyl and hydroxyl derivatives and 1,3,4,-oxadiazoline acyclic nucleoside analogs were prepared. The newly synthesized compounds were tested for their antimicrobial activities and showed moderate to high inhibition activities.

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“…Substituted 1-phenyl-1H-pyrazole-4-carbaldehyde (4d-g) These were prepared as previously described (Finar and Manning, 1961;Bernard et al, 1986).…”

Section: Methodsmentioning

confidence: 99%

Synthesis of some substituted furan-2(5H)-ones and derived quinoxalinones as potential anti-microbial and anti-cancer agents

et al. 2010

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In search for novel anti-cancer and antimicrobial agents with promising pharmacotoxicological profile, the synthesis of some substituted 4-halofuran-2(5H)-ones (8a-l, 9, 11) and derived halogenated quinoxalin-2(1H)-ones (12a-d) is described. Some of the halogenated furanones were readily oxidized to the corresponding 2-bromo-2-propenoic acids (13a-c) with hydrogen peroxide in alkaline medium. Twenty-two compounds were preliminary tested for their in vitro activity against three bacteria and one fungus and revealed encouraging activity. On the other hand, three compounds were screened as anti-cancer agents using cell line panel protocol and 22 compounds were subjected to cycline-dependent kinases (CDKs) inhibition screening program but were inactive.Keywords 5-Aryl-4-halo-3-hydroxyfuran-2(5H)-ones Á 3-(2-Aryl-1-halovinyl)quinoxalin-2(1H)-ones Á 3-Aryl-2-bromo-2-propenoic acids Á Anti-cancer and anti-microbial properties

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ChemInform Abstract: Azoles. Part 17. β‐(4‐Pyrazole)acrylic and ‐propionic Acid and Their Antiinflammatory Activity.

Cited by 11 publications

References 0 publications

Design and Synthesis of Some Substituted 1H‐Pyrazolyl‐oxazolidines or 1H‐Pyrazolyl‐thiazolidines as Anti‐inflammatory‐Antimicrobial Agents

Design and Synthesis of Some Substituted 1H‐Pyrazolyl‐oxazolidines or 1H‐Pyrazolyl‐thiazolidines as Anti‐inflammatory‐Antimicrobial Agents

Synthesis and antimicrobial activity of substituted [(pyrazol‐4‐yl)methylene]hydrazono‐2,3‐dihydrothiazoles and their sugar derivatives

Synthesis of some substituted furan-2(5H)-ones and derived quinoxalinones as potential anti-microbial and anti-cancer agents

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