RESUMO
A modest, competent and green synthetic procedure for novel coumarinyl-1,3,4-oxadiazolyl-2-mercaptobenzoxazoles 8i-t has been reported. Analysis of the docked (PDB ID: 5IKR; A-Chain) poses of the compounds illustrated that they adopt identical conformations to the extremely selective COX-2 inhibitor. The biological outcomes as well as computational study suggested that the compounds originated to have elevated resemblance towards COX-2 enzyme than COX-1. The compounds 8i, 8l, 8q, 8r, 8s and 8t emerged as most potent and selective COX-2 inhibitors in contrast with Mefenamic acid. The selectivity index of 8l, 8n and 8r was respectively found to be 33.95, 20.25 and 24.98 which manifested their high selectivity against COX-2. Interestingly, the compounds which were active as COX-2 inhibitors were also active as antioxidant agents.
Assuntos
Antioxidantes/farmacologia , Inibidores de Ciclo-Oxigenase 2/farmacologia , Ciclo-Oxigenase 2/metabolismo , Química Verde , Oxidiazóis/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/antagonistas & inibidores , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/química , Humanos , Micro-Ondas , Modelos Moleculares , Estrutura Molecular , Oxidiazóis/síntese química , Oxidiazóis/química , Picratos/antagonistas & inibidoresRESUMO
In the field of plastic reconstructive surgery, development of new innovative matrices for skin repair is in demand. The ideal biomaterial should promote attachment, proliferation and growth of cells. Additionally, it should degrade in an appropriate time period without releasing harmful substances, not exerting a pathological immune response. The materials used should display optimized mechanical properties to sustain cell growth and limit scaffold contraction. Wound healing is a biological process directed towards restoration of tissue that has suffered an injury. An important phase of wound healing is the generation of a basal epithelium wholly replacing the epidermis of the wound. Wild silk from Antheraea mylitta meets these demands to a large extent. To evaluate the effects of the treatment, Antheraea mylitta and Bombyx mori samples were characterized by SEM-EDX, FT-IR, XRD and TGA-DSC techniques. Preliminary cell growth behavior was carried out by culturing epidermal cells and proliferation was quantified via viability assay. Moreover, Antheraea mylitta possesses excellent cell-adhesive capability, effectively promoting cell attachment and proliferation. Antheraea mylitta serves as a delivery vehicle for cells. With all these unique features, it is expected that Antheraea mylitta mat will have wide utility in the areas of tissue engineering and regenerative medicine.