Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles

European Journal of Medicinal Chemistry
Navin B PatelSmita D Rajani

Abstract

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.

Citations

Feb 26, 2013·European Journal of Medicinal Chemistry·Navin B PatelGildardo Rivera
Sep 11, 2013·European Journal of Medicinal Chemistry·Christophe MenendezMichel Baltas
Aug 13, 2011·Acta Crystallographica. Section E, Structure Reports Online·Xu-Feng LiuShao-Liang Jiang
Mar 5, 2014·European Journal of Medicinal Chemistry·Fauzia MirM S Alam
Dec 3, 2014·European Journal of Medicinal Chemistry·Rangappa S KeriSrinivasa Budagumpi
Feb 4, 2015·Chemical Biology & Drug Design·Rangappa S KeriBhari Mallanna Nagaraja
Jun 10, 2017·Medicinal Research Reviews·Vajinder KumarRahul Jain
Feb 21, 2021·Molecular Diversity·Shima NasriKhudaidad Kochia
Jul 18, 2020·Recent Patents on Anti-cancer Drug Discovery·Katerina I SlavovaIrena P Kostova
Apr 4, 2021·Pharmaceuticals·Małgorzata Strzelecka, Piotr Świątek
Mar 6, 2019·Journal of Medicinal Chemistry·Ge ChenJidong Zhu
Oct 27, 2021·Future Medicinal Chemistry·Yingdong Cao, Hong Lu

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