Dual evaluation of some novel 2-amino-substituted coumarinylthiazoles as anti-inflammatory-antimicrobial agents and their docking studies with COX-1/COX-2 active sites.
J Enzyme Inhib Med Chem
; 29(4): 476-84, 2014 Aug.
Article
en En
| MEDLINE
| ID: mdl-23777557
ABSTRACT
Synthesis of total eighteen 2-amino-substituted 4-coumarinylthiazoles including sixteen new compounds (3a-o and 5b) bearing the benzenesulfonamide moiety is described in the present report. All the synthesized target compounds were examined for their in vivo anti-inflammatory (AI) activity and in vitro antimicrobial activity. Results revealed that six compounds (3 d, 3 f, 3 g, 3 h, 3 j and 3 n) exhibited pronounced anti-inflammatory activity comparable to the standard drug indomethacin. AI results were further confirmed by the docking studies of the most active (3n) and the least active compound (3a) with COX-1 and COX-2 active sites. In addition, most of the compounds exhibited moderate antimicrobial activity against Gram-positive bacteria as well as fungal yeast, S. cervisiae. Comparison between 3 and 5 indicated that incorporation of additional substituted pyrazole nucleus into the scaffold significantly enhanced AI activity.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Tiazoles
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Antiinflamatorios no Esteroideos
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Inhibidores de la Ciclooxigenasa
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Cumarinas
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Dominio Catalítico
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Edema
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Simulación del Acoplamiento Molecular
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Antibacterianos
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Antifúngicos
Límite:
Animals
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Humans
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Male
Idioma:
En
Año:
2014
Tipo del documento:
Article