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1.
Molecules ; 23(8)2018 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-30049981

RESUMO

A series of novel benzophenone derivatives containing a thiazole heterocyclic nucleus were designed by molecular hybridization. Molecular docking studies have demonstrated the inhibitory potential of the designed compounds against cyclooxygenase (COX) isoenzymes. These compounds were synthesized, characterized, and evaluated for their anti-inflammatory properties by the croton oil-induced ear edema assay to examine their effect on both prostaglandin (PG) production and neutrophils recruitment. The thiazole derivatives displayed a potent effect in terms of reducing ear edema. The analysis suggested that the presence of 4-phenyl-2-hydrazinothiazole and the absence of C4'-OCH3 on the benzophenone derivative structure are strongly related to the inhibition of PG production. In addition, the derivatives 2e, 3a and 3c concomitantly inhibit PG production and neutrophil recruitment, which may be a mechanism of action better than of common NSAIDs due to their inability to inhibit the neutrophil recruitment. Thus, these compounds can be considered as potential lead compounds toward the development of new anti-inflammatory drugs with an innovating mechanism of action.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Benzofenonas/química , Benzofenonas/farmacologia , Desenho de Fármacos , Edema/patologia , Infiltração de Neutrófilos/efeitos dos fármacos , Animais , Anti-Inflamatórios/síntese química , Benzofenonas/síntese química , Sítios de Ligação , Domínio Catalítico , Ciclo-Oxigenase 1/química , Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase/química , Modelos Animais de Doenças , Edema/tratamento farmacológico , Isomerismo , Camundongos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Ligação Proteica , Relação Estrutura-Atividade
2.
Bioorg Med Chem ; 20(8): 2713-20, 2012 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-22401914

RESUMO

Six derivatives of guttiferone-A (LFQM-79, 80, 81, 82, 113 and 114) were synthesized and evaluated for their antimicrobial activity against the opportunistic or pathogenic fungi Candida albicans (ATCC 09548), Candida glabrata (ATCC 90030), Candida krusei (ATCC 6258), Candida parapsilosis (ATCC 69548), Candida tropicalis (ATCC 750), Cryptococcus neoformans (ATCC 90012), Trichophyton tonsurans, Microsporum gypseum and also against the opportunistic and pathogenic Gram-positive bacteria Staphylococcus aureus (ATCC 6538), Staphylococcus epidermidis (ATCC 12228), Bacillus cereus (ATCC 11778) and Gram-negative Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 9027), Salmonella typhimurium (ATCC 14028), Proteus mirabilis (ATCC 25933). The antimicrobial activities of derivatives were compared with guttiferone-A and they presented to be more potent than the original molecule and sometimes greater than standard drugs established in therapeutics. The current study showed that derivatives of guttiferone-A possess potent antimicrobial activity and are relatively non-cytotoxic, which reveal these new molecules as promising new drug prototype candidates, with innovative structural pattern.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Benzofenonas/farmacologia , Fungos/efeitos dos fármacos , Antibacterianos/química , Antifúngicos/química , Bactérias/crescimento & desenvolvimento , Benzofenonas/síntese química , Benzofenonas/química , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Fungos/crescimento & desenvolvimento , Humanos , Leucócitos Mononucleares/citologia , Leucócitos Mononucleares/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Conformação Molecular , Estereoisomerismo , Relação Estrutura-Atividade
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