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1, 2, 4-TRIAZOLES: AS BIOLOGICALLY IMPORTANT AGENTS
E. Huntsman et al, 31 have synthesized [1, 2, 4] Triazolo[1, 5-a]pyridines (11) have been prepared in good yields from 2-aminopyridines by cyclization of N-(pyrid-2-yl) formamidoximes under mild reaction conditions with trifluoroacetic anhydride.
1,2,4-triazole-possessing thiosemicarbazides(Fig. 9),synthesized by Esra Dugdu et al., have shown very good antibacterial and antifungal activities . They regarded that thiosemicarbazide groups in the triazole compounds should be considered for the synthesis of lead compounds.
Biological Activities of 1, 2, 4-Triazoles:
INTRODUCTION: The 1, 2, 4-triazole is a five membered heterocyclic compound containing two carbons and three nitrogens with a molecular formula of C2H3N3. It exists in two tautomeric forms. 1H and 4H-1, 2, 4-triazole is considered to be pharmacologically important nucleus.
The literature review shows that 1, 2, 4-triazole possess wide spectrum of biological activities. In particular compounds having 1, 2, 4-triazole nucleus are known to have excellent antibacterial, antifungal, antitubercular, antioxidant, anticancer, anti-inflammatory, analgesic, anticonvulsant, anxiolytic activities 1.
1, 2, 3-TRIAZOLE 1, 2, 4-TRIAZOLE
R.K. Mali et al, 45have synthesized5-(N-substituted carboxamidomethylthio)–3-(3'-pyridyl) - 1, 2, 4-triazole derivatives and were evaluated in for their antibacterial activity.
Anti-inflammatory Activity: Mohammad et al, 46 synthesized a series of 1, 3, 4-oxadiazole [6a-6b] and 1, 2, 4-triazole [6c] derivatives of 4-hydroxyphenyl acetic acid and evaluated for their anti-inflammatory activity by carrageenan induced rat paw edema method. The compounds, which showed good anti-inflammatory activity, were screened for their ulcerogenic and lipid peroxidation activities.
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1,2,4-Triazoles will be available on
Mohamed et al., have screened a library of new 1-(4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides (Fig. 16)for their antiinflammatory activity  using carrageenan induced rat paw edema method and the tested compounds exhibited safer UI comparative to indomethacin.
V. Ram et al, 33 have synthesized (14) triazole derivatives as below;
Saini MS and Dwivedi J: A Review: Synthesis and Biological significances of 1, 2, 4-triazole and its derivatives. Int J Pharm Sci Res 2013: 4(8); 2866-2879. doi: 10.13040/IJPSR. 0975-8232.4(8).2866-79
Received: 02 Jun 2014 Revised and Accepted: 22 Jul 2014
Kumudha et al., have followed Carrageenan induced rat paw edema method to evaluate the anti inflammatory activity of 4,5-diphenyl 4H-1,2,4-triazole-3-thiols (Fig. 7) at the dose of 50mg in albino rats using diclofenac sodium as a standard drug . Values are articulated as ANOVA followed by New mann’sKeul’s multiple range tests.
Fig. 2: Active pharmaceutical products containing 1,2,4-triazole ring
5-substituted-3- pyridine-1, 2, 4 triazoles(Fig. 6)synthesized by Nitin Muthalet al., are screened for the anti inflammatory activity too . Compounds are observed to display good results.
Scheme 1: Synthesis of 3-mercapto-1, 2, 4-triazoles
Xiang Li et al., have reported potent anticancer activities exhibited by new chiral 1,2,4-triazole compounds (Fig. 12) towards Hela .
Scheme 5: Synthesis of 3-mercapto-1, 2, 4-triazoles
Ya-Ping Hou et al., have screened a series of 1,2,4-triazole derivatives containing 1,4 benzodioxan (Fig. 11)for their ability to anti proliferative activity against HEPG2, HELA, SW1116 and BGC823 . The tested compounds show potent activities against HEPG2 than other three cancer cell lines. Analysis of structure-activity relationship (SAR) indicates that compounds with electron-withdrawing group show stronger activity than that with electron-donating group, with all the IC50 values below 50 lM against HEPG2. Compounds with different electron-withdrawing groups, are able to portray different antitumor activities, and the potency order follows F (fluorine) >Cl (chlorine) > Br (bromine)> NO2 (nitro-group). With regard to the F-substituted compounds, monosubstitution is preferred over di-substitution. The placement of substituents based on their effects is ortho- > meta- >para-. The work is continued with MetAP2 inhibitory assay, apoptosis assay, and Western-blot assay.
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