ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF DIFFERENT TRIAZOLE ANALOGUES
A series of 1,4- and 1,5-diaryl substituted 1,2,3-triazoles (21) were tested for in vitro cyclooxygenase (COX) assays to determine the combined electronic and steric effects on COX-1 and COX-2 inhibitory potency and selectivity. The high COX-2 inhibition potency of some 1,2,3-triazoles having a vicinal diaryl substitution pattern along with their ease in synthesis through versatile Ru(II)-catalysed click chemistry make this class of compounds interesting candidates for further design and synthesis of highly selective and potent COX-2 inhibitors . A series of new 1,2,4-triazole-5-thione derivatives (22) were evaluated for their anti-inflammatory and analgesic activities. Some compounds exhibited comparable anti-inflammatory activity to that of Indomethacin where as other compounds were more potent analgesics than acetyl salicylic acid . A series of compound 5-[(Biphenyl-4-yloxy) -methyl]-4-nsubstituents-3-marcapto-(4H)-1,2,4-triazole. Synthesized compounds were screened for anti-inflammatory activity out of the synthesized compounds 5-[(Biphenyl-4-yloxy) methyl]-4-n-butyl-3-marcapto-(4H)-1,2,4-triazole (23) showed potent anti-inflammatory activity . Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles (24) for their possible anti-inflammatory and analgesic effect and most of these compounds showed potent and significant results compared to Indomethacin. Moreover, ulcerogenicity and the median lethal dose of the most active compound were determined in mice .A new series of 1,2,4-triazole derivatives of 5-Mercepto-1,2,4-triazole derivatives (25 and 26) have been evaluated anti-inflammatory activity of when compared with standard drug .Some derivatives of 1,2,4- triazolo[2,3-a]benzimidazoles (27), for their possible anti-inflammatory and analgesic effect and most of these compounds showed potent and significant results compared to indomethacin. Moreover, ulcerogenicity and the median lethal dose of the most active compound were determined in mice; and found to be 275 mg/kg . A series of 5-[(Biphenyl-4-yloxy) methyl]-4-n-substituents-3-mercapto-(4H)-1,2,4-triazole. Its derivatives such as 5-[(Biphenyl-4-yloxy)methyl]-4-fluorophenyl-3-mercapto-(4H)-1,2,4-triazole (28) screened for the analgesic activity. And that compound showed analgesic activity ranging from 16.9% to 72.8%, whereas the standard drug flurbiprofen showed 69.5% inhibition .
Now a day’s research is concentrated towards the introduction of new and safe therapeutic agents of clinical importance. The success of imidazole as an important moiety of number of medicinal agents led to introduction of the triazoles. The triazoles are said to be the isosters of imidazoles in which the carbon atom of imidazole is isosterically replaced by nitrogen. The Triazole derivatives possess a wide a range of pharmacological activities. Triazoles nucleus have been incorporated into a wide variety of therapeutically interesting drug candidates including antiinflammatory, analgesic, analeptics, sedatives, antianxiety, anticonvulsant, antioxidants, antimicrobial, antifungal, antiviral, antimalarial, antituberculosis, anticancer, antioxidant, insecticidal and other anticipated activies [1-5]. They are also used as optical brightening agents, corrosion inhibitors and additives with a variety of other functions. Many dye stuffs and pigments have heterocyclic. The importance of triazole derivatives lies in the field that these have good position in heterocyclic chemistry, due to its various biological activities. More investigations must be carried out to evaluate more activities of triazole for many diseases whose treatment are difficult in the medical sciences. This has been noticed so far, that modifications on triazole moiety results in the formation of compounds with valuable biological activities. It will be interesting to observe that these modifications can be utilized as potent therapeutic agents in future [57,58]. Thus many more modifications on triazole moiety can be possible and needs to be continued for the use of mankind.
Triazoles have attracted considerable attention in the fields of medicine and agrochemical research as well as in materials science, due to their unique structures and properties. Triazole derivatives belong to a class of exceptionally active compounds possessing many pharmacological properties. Triazoles have clinched much importance as they have also been investigated for their biological effects. Triazole is a unique moiety that is responsible for various biological activities. This review has presented comprehensive details of triazole analogues reported for particular analgesic and inflammatory activities. Triazoles derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous heterocyclic compounds with different biological activities. Thus triazole acts as a promising medicinal agent for the scientists working over this field. This review can be helpful to develop various more new compounds possessing triazoles moiety that could be better in terms of efficacy and lesser toxicity. Triazole is a five member heterocyclic nucleus has attracted a wide attention of the chemist in search for the new therapeutic molecules and play vital role in biological fields. This review provides a brief summary of the medicinal chemistry of triazole system and highlights some examples of recent drug containing this moiety.
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