Synthesis and antidepressant-like action of stereoisomers of imidobenzenesulfonylaziridines in mice evaluated in the forced swimming test

Duarte, Filipe S.; Andrade, Evilazio da Silva; Vieira, Ricardo A.; Uieara, Marina; Nunes, Ricardo José; Lima, Thereza Christina Monteiro de

doi:10.1016/j.bmc.2006.03.036

Cited by 13 publications

(1 citation statement)

References 24 publications

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“…Many derivatives possess biological activity. They have antibacterial (Albuquerque et al 1999;Zentz et al 2002;Struga et al 2008a, b), anticonvulsive (Stratford and Curley 1983), hypnotic, sedative (Duarte et al 2006;Kozioł et al 2006), anxiolytic (Chilmończyk et al 1995), and antitumor properties (Di Pardo et al 2001;Kumar and Rajkumar 2006;Nakamura et al 2006). It is also known that compounds bearing short-amine fragment possess antibacterial and antifungal activity (Stefańska et al 2008).…”

Section: Introductionmentioning

confidence: 94%

Antimicrobial activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

et al. 2010

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Antibacterial and antifungal activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.0 2,6 ]dec-8-ene-3,5-dione derivatives were examined by the disk diffusion method (growth inhibition zone diameter in agar medium). The minimal inhibitory concentrations (MICs) for the most active agents were determined. Title compounds were also evaluated in vitro against HIV-1 virus and their cytotoxicity was determined. Aminoalkanol derivatives exhibited activity against the majority of microorganisms studied.

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Section: Introductionmentioning

confidence: 94%

Antimicrobial activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

et al. 2010

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Design, synthesis, and computational studies of phenylacetamides as antidepressant agents

et al. 2022

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In the present work, a hit molecule obtained from zinc ‘clean drug-like database’ by systematically performed computational studies was modified chemically to obtain different derivatives ( VS1–VS25 ). Structures of synthesized derivatives were confirmed by IR, 1 H-NMR, 13 C-NMR, 13 C-DEPT, MS, and elemental analysis. All the synthesized compounds were biologically evaluated for their antidepressant activity by using tail suspension test and forced swimming test in albino mice. All these derivatives showed moderate to good antidepressant activity. The most potent compound ( VS25) among the synthesized compounds showed better antidepressant potential than the standard drugs moclobemide, imipramine, and fluoxetine. To understand the time-dependent interactions of this most active compound with MAO-A molecular dynamics was carried out and reported here. Additionally, acute oral toxicity was performed for the most active compound as per OECD guidelines. Graphic abstract Supplementary Information The online version contains supplementary material available at 10.1007/s11030-021-10374-5.

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Sulphonamide and sulphonyl-hydrazone cyclic imide derivatives: Antinociceptive activity, molecular modeling and In Silico ADMET screening

et al. 2012

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In this paper, we describe the antinociceptive activity, molecular modeling and in silico ADMET screening of a series of sulphonyl-hydrazone and sulphonamide imidobenzene derivatives. Among these compounds, the sulphonyl-hydrazones 9 and 11 showed the most potent analgesic activity (ID(50) = 5.1 and 6.8 μmol/kg, respectively). Interestingly, all derivatives evaluated in this study have a better analgesic profile than the control drugs, acetyl salicylic acid and acetaminophen. Derivative 9 was the most promising compound; with a level of activity that was 24 times higher than the control drugs. Our SAR study showed a relationship among the distribution of the frontier orbital HOMO coefficients, HOMO-LUMO energy gap of these molecules and their reactivity. The best analgesic compounds (including 6, 9, 10, 11 and 12) fulfilled the Lipinski "rule-of-five", which is theoretically important for good drug absorption and permeation.

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Synthesis and antidepressant-like action of stereoisomers of imidobenzenesulfonylaziridines in mice evaluated in the forced swimming test

Cited by 13 publications

References 24 publications

Antimicrobial activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

Antimicrobial activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

Design, synthesis, and computational studies of phenylacetamides as antidepressant agents

Sulphonamide and sulphonyl-hydrazone cyclic imide derivatives: Antinociceptive activity, molecular modeling and In Silico ADMET screening

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