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The present investigation is concerned with synthesis of new 2 and 6 - substituted 4H-chromen-4-One derivatives with the objectives of discovering novel and potent anti-inflammatory agents and anti-oxidants. The results of anti-inflammatory activity were revealed that the compound has indole 2 substitution with 4-nitrophenyl amino methyl (at 6th position) on 4H- chromen-4-one having more anti-inflammatory activity as compared to other substituent's. While, indole 2 substituted 4-methoxy phenyl amino methyl (at 6th position) 4H-chromen-4-one showed outperformed anti-oxidant activity in different anti-oxidant model as compared to other substituent's. The all newly synthesized compounds displayed moderate to potent anti-inflammatory and anti-oxidant activity and has therapeutic potential in combating this devastating inflammatory and oxidative condition of the body, might be deserve promising substances for further in vivo evaluation as anti-inflammatory and anti-oxidant properties. However the anti-inflammatory activity is not related to antioxidant potential.
Heterocycles bearing a triazole ring residue are reported to show anticancer, anti-inflammatory, analgesic, antifungal, antitubercular, antimicrobial, antiviral, antioxidant, CNS depressant, and plant growth regulatory activity etc. Keeping in view the importance of Triazole from the literature survey I found various triazole derivatives & from that I planned to work the substituted triazole derivatives from m-nitro benzoic acid, which gives various anticipated biological activities. Among the all synthesized compound, compound 6-(2-chloro-phenyl)-3-(4-nitro-phenyl)- 1,2,4]triazolo 3,4-b] 1,3,4]thiadiazole (PLP 105b) with MIC value of (16ug/ml) against gram-positive (B.subtilis) and (16ug/ml) against gram-negative (E.coli, p.aeroginosa)and the compound3,6-bis-(4-nitro-phenyl)- 1,2,4]triazolo 3,4-b] 1,3,4]thiadiazole (PLP 105d) with MIC value of (16ug/ml) against gram-negative (p.aeroginosa) give better antimicrobial activity than other synthesized compound."
The NSAIDs have known to cause serious problems such as gastric ulceration, bleeding and renal disorders on long term medication. These severe side effects are partially due to their nonselectivity towards to COX-2 enzyme. Hence, newer, selective COX-2 enzyme inhibitors have been developed to overcome the toxicity problems. Recently, Rofecoxib and Celecoxib were withdrawn due to cardiac toxicity.1,2-disubstituted five-membered heterocyclic compounds have shown selectivity towards COX-2 inhibition. But, the toxicity reports of drugs like Rofecoxib and Celecoxib in this category prompted us to synthesize 1,2-diaryl diazepines (E) and their derivatives as, survey of literature indicated the diazepine heterocyclic system to have anti-inflammatory activity.
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