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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 [26]. 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 [32] 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 [24]. 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 [23]. 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 [29].

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 [28]. 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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