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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles.
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Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles.

机译：新合成的1,2,4-三唑的药理评价和表征。

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摘要

The triazole analogs were obtained via. multistep synthesis sequence beginning with ethyl nicotinoate 3 which on treatment with hydrazine hydrate yields nicotinoyl hydrazide 4. Intermolecular cyclisation of 4 with 4-methylbenzoic acid in presence of phosphorous oxy chloride affords 2-(3-pyridyl)-5-(4-methylphenyl)-1,3,4-oxadiazole 5. Condensation of 5 with various substituted 2-hydrazino benzothiazole 2a-j results in 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-substituted-1,3-benzothiazol-2-amino)-4H-1, 2,4-triazole 6a-j analogs. All the compounds have been characterized by elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data. In vitro antitubercular activity was carried out against Mycobacterium tuberculosis H(37)Rv strain using Lowenstein-Jensen medium and antimicrobial activity against various bacteria and fungi using broth microdilution method. Compounds 2e, 6a, 6b, 6c, 6d, 6g, 6h and 6i emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. Compound 6j showed better antitubercular activity compared to rifampicin.
机译：通过获得三唑类似物。从烟酸乙酯3开始的多步合成序列，该烟酸酯在水合肼处理后产生烟酰肼4。在氯氧化磷存在下，用4-甲基苯甲酸将4进行分子间环化，得到2-（3-吡啶基）-5-（4-甲基苯基） -1,3,4-恶二唑5。将5与各种取代的2-肼基苯并噻唑2a-j缩合，得到3-（3-吡啶基）-5-（4-甲基苯基）-4-（N-取代-1， 3-苯并噻唑-2-氨基）-4H-1，2,4-三唑6a-j类似物。所有化合物均已通过元素分析，IR，（1）H NMR，（13）C NMR和质谱数据表征。使用Lowenstein-Jensen培养基对结核分枝杆菌H（37）Rv菌株进行了体外抗结核活性，并采用肉汤微量稀释法对各种细菌和真菌进行了抗菌活性。化合物2e，6a，6b，6c，6d，6g，6h和6i成为有前途的抗菌剂。还观察到有希望的抗微生物剂已被证明是更好的抗结核药。与利福平相比，化合物6j显示出更好的抗结核活性。

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