Design, synthesis and antimycobacterial evaluation of 1-(4-(2-substitutedthiazol-4-yl)phenethyl)-4-(3-(4-substitutedpiperazin-1-yl)alkyl)piperazine hybrid analogues

Nagesh, Hunsur Nagendra; Suresh, A.; Sirigina, Devesh Sathya Sri Sairam; Sriram, Dharmarajan; Yogeeswari, Perumal; Sekhar, Kondapalli Venkata Gowri Chandra

doi:10.1016/j.ejmech.2014.07.067

Cited by 13 publications

(3 citation statements)

References 29 publications

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“…People with XDR-TB and TDR-TB don't get better with the usual TB drugs, so they have to take less effective, more expensive, and sometimes toxic medicines for a longer time, up to 2 years. It is a big challenge to deal with drug-resistant TB [7].…”

Section: Introductionmentioning

confidence: 99%

Spectroscopic Studies on Structurally Modified Anthraquinone Azo Hydrazone Tautomer: Theoretical and Experimental Approach

Shekharagouda,

Mamatha,

Nagaraju

et al. 2024

J Fluoresc

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A series of unique four mono-azo substituted anthraquinone analogue were synthesized by using the anthraquinone components in the diazo-coupling technique. The FT-IR, 1 H NMR, and HRMS, data were used to con rm the structure of the molecules, and spectroscopic techniques like UV-Vis, and photoluminescence spectroscopy were employed to estimate the photophysical properties of the molecules. The molecular optimized geometry and frontier molecular orbitals were estimated using density functional theory. Further, global chemical reactivity descriptors parameter was theoretically estimated using the value of the highest occupied molecular orbit and lowest unoccupied molecular orbits. The anti-tubercular action of the synthesised dyes were also examined. The results of this biological activity showed that N-isopropyl aniline combined with anthraquinone Nisopropyl aniline had superior anti-tubercular activity when compared to Rifampicin as the standard. As per molecular docking studies, the synthesized compound Q1 showed excellent binding energy (-10.0 kcal/mol) among all compounds against the 3ZXR Protein. These results agreed with our in-vitro anti-TB activity results.

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Section: Introductionmentioning

confidence: 99%

Spectroscopic Studies on Structurally Modified Anthraquinone Azo Hydrazone Tautomer: Theoretical and Experimental Approach

Shekharagouda,

Mamatha,

Nagaraju

et al. 2024

J Fluoresc

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“…Thiazole derivatives have well established with antituberculosis effects in many studies [25][26][27][28][29][30] . Studies combined these two rings, thiazole and isatin have also been reported 31,32 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antimycobacterial activity evaluation of isatin-derived 3- [(4- aryl - 2- thiazolyl])hydrazone]-1h- indol- 2, 3- diones

Yurttaş¹,

Ertaş²,

Cankılıç³

et al. 2017

actapharm

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“…These compounds elicited 99% inhibition in the range of 3.10-6.25 µg/mL against H 37 Rv strain of M. tuberculosis[273]. Amongst various derivatives developed by Nagesh et al compound 170 was reported as most active with MIC of 1.56 µg/mL against H37Rv strain of M. tuberculosis[274]. Patel and Telvekar developed piperazine substituted cinnamide derivatives.…”

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confidence: 99%

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

Shaquiquzzaman

Verma

Marella

et al. 2015

European Journal of Medicinal Chemistry

187

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Design, synthesis and antimycobacterial evaluation of 1-(4-(2-substitutedthiazol-4-yl)phenethyl)-4-(3-(4-substitutedpiperazin-1-yl)alkyl)piperazine hybrid analogues

Cited by 13 publications

References 29 publications

Spectroscopic Studies on Structurally Modified Anthraquinone Azo Hydrazone Tautomer: Theoretical and Experimental Approach

Spectroscopic Studies on Structurally Modified Anthraquinone Azo Hydrazone Tautomer: Theoretical and Experimental Approach

Synthesis and antimycobacterial activity evaluation of isatin-derived 3- [(4- aryl - 2- thiazolyl])hydrazone]-1h- indol- 2, 3- diones

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

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