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1.
Curr Org Synth ; 19(6): 693-701, 2022 08 06.
Artigo em Inglês | MEDLINE | ID: mdl-35249494

RESUMO

AIMS: The aim of this present work was to design and establish an efficient synthesis of new thienyl pyrazolo[1,5-a] pyrimidines using an environmentally friendly reaction solvent. Further, the newly synthesized compounds were evaluated for antimicrobial activity. MATERIALS AND METHODS: A series of thienyl pyrazolo[1,5-a] pyrimidines have been synthesized by the condensation reaction of 4-(4'-chloro-phenylazo)-5-amino pyrazole with α, ß- unsaturated carbonyl composites (chalcones) using NaOH in polyethylene glycol- 400 as a green reaction solvent. The dissemination technique recommended by the National Clinical Laboratory Standards Committee was used to study the antimicrobial activities of synthesized compounds. RESULTS AND DISCUSSION: Polyethylene glycol-400 prompting an efficient synthesis of thienyl pyrazolo[1,5-a] pyrimidines have been discussed. Excellent yields of the products were obtained in a shorter reaction time using PEG 400 as a green reaction solvent. The reaction solvent was recovered and reused without the loss of its activity. The synthesized compounds have shown interesting antibacterial activity. Hydroxyl and halo substitution with thienyl moiety emerged as an active antibacterial and antifungal study. CONCLUSION: The advantage of this methodology is that it incorporates the green method, has excellent yields, easy workup, avoids toxic solvents, and an expensive catalyst. The new dimension pyrazolo[1,5-a] pyrimidine derivatives with thienyl moiety exhibit promising anti-microbial activity.


Assuntos
Polietilenoglicóis , Pirimidinas , Antibacterianos/farmacologia , Pirimidinas/farmacologia , Solventes
2.
Bioorg Med Chem Lett ; 20(7): 2292-6, 2010 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-20207143

RESUMO

A series of nitrogen-containing benzophenone analogues were synthesized by Mannich reaction and evaluated for the inhibition of pro-inflammatory cytokines, TNF-alpha and IL-6. DPPH (1,1-diphenyl-2-picryl hydrazine) radical scavenging activity and its kinetics were studied to determine the antioxidant potential of the test samples. All the synthesized compounds exhibited promising activity against IL-6 in a range of 81-89%, 09-42% at 10 and 1 microM, respectively, concentration. Exceptionally, the compound 20e was observed to be an effective inhibitor of TNF-alpha (54%) and IL-6 (97%), (47%) at 10 and 1 microM concentrations with minimum toxicity (22%) against CCK-8 cells. With few exceptions, all other compounds were found to be excellent inhibitors of IL-6 and moderate to excellent inhibitors of TNF-alpha, however the toxicity profiles of these compounds need to be ameliorated in further optimization studies. Amongst the tested compounds, 16a, 17g, 18f, 18g, 19g and 20e were found to possess significant antioxidant activity.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Benzofenonas/farmacologia , Interleucina-6/antagonistas & inibidores , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Anti-Inflamatórios/química , Antioxidantes/química , Benzofenonas/química , Linhagem Celular , Humanos , Interleucina-6/metabolismo , Nitrogênio/química , Nitrogênio/farmacologia , Fator de Necrose Tumoral alfa/metabolismo
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