Ramprasad, J.Nayak, N.Udayakumar, U.Yogeeswari, P.Sriram, D.2026-02-052015Bioorganic and Medicinal Chemistry Letters, 2015, 25, 19, pp. 4169-41730960894Xhttps://doi.org/10.1016/j.bmcl.2015.08.009https://idr.nitk.ac.in/handle/123456789/26210A new series of triazole-imidazo[2,1-b][1,3,4]thiadiazole hybrids (6a-s, 7a) were designed by a molecular hybridisation approach and the target molecules were synthesized via one pot click chemistry protocol. All the intermediates and final molecules were characterised using spectral methods and one of the target compounds (6c) was analysed by the single crystal XRD study. The derivatives were screened for their antimycobacterial activity against Mycobacterium tuberculosis H<inf>37</inf>Rv strain. Two compounds, 6f and 6n, demonstrated significant growth inhibitory activity against the bacterial strain with a MIC of 3.125 ?g/mL. The presence of chloro substituent on the imidazo[2,1-b][1,3,4]thiadiazole ring and ethyl, benzyl or cyanomethylene groups on the 1,2,3-triazole ring enhance the inhibition activity of the molecules. The active compounds are not toxic to a normal cell line which signifies the lack of general cellular toxicity of these compounds. © 2015 Elsevier Ltd. All rights reserved.1,2,3 triazole derivative1,3,4 thiadiazole derivativeethambutolimidazo[2,1 b][1,3,4]thiadiazole derivativetuberculostatic agentunclassified drugimidazo(2,1-b)(1,3,4)thiadiazoleimidazole derivativethiadiazole derivativetriazole derivativeanimal cellantibacterial activityArticlebacterial straincarbon nuclear magnetic resonanceclick chemistrycrystal structurecytotoxicitydrug screeninghybridizationlipophilicityminimum inhibitory concentrationMycobacterium tuberculosisnonhumanone pot synthesispharmacophoreproton nuclear magnetic resonancestructure activity relationX ray diffractionchemical structurechemistrydose responsedrug effectsmicrobial sensitivity testsynthesisX ray crystallographyAntitubercular AgentsClick ChemistryCrystallography, X-RayDose-Response Relationship, DrugImidazolesMicrobial Sensitivity TestsModels, MolecularMolecular StructureStructure-Activity RelationshipThiadiazolesTriazoles