Synthesis, In silico Molecular Docking and Pharmacokinetic Studies, In vitro Antimycobacterial and Antimicrobial Studies of New Imidozolones Clubbed with Thiazolidinedione

Khan, Imran H.; Patel, Navin B.; Patel, Vatsal M.

doi:10.2174/1573409914666180516113552

Cited by 13 publications

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“…The derivatives of thiazolidines, thiazoles and thiazolidinediones are molecules recognized in the literature for presenting a series of relevant pharmacological activities [ 1 , 2 , 3 ]. Among these activities are antimicrobial [ 3 , 4 ], antiviral [ 1 , 2 ], neurodegenerative [ 5 ], antitumor [ 6 , 7 ] and antioxidant [ 8 ] activities.…”

Section: Introductionmentioning

confidence: 99%

“…Its nucleus has been reported to be responsible for most of its pharmacological actions. These compounds are known to influence the regulation of different molecular cascades and have several biological activities, such as antimicrobial [ 4 , 15 ], neurodegenerative [ 5 ], hypoglycemic [ 16 ], antitumor [ 17 ], anti-inflammatory [ 18 ], and antioxidant [ 19 ] activities, among others.…”

Section: Introductionmentioning

confidence: 99%

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Neurolocomotor Behavior and Oxidative Stress Markers of Thiazole and Thiazolidinedione Derivatives against Nauphoeta cinerea

et al. 2022

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Thiazolidine compounds NJ20 {(E)-2-(2-(5-bromo-2-methoxybenzylidene)hydrazinyl)-4-(4-nitrophenyl)thiazole} and NW05 [(2-(benzo (d) (1,3) dioxol-4-ylmethylene)-N-(4-bromophenyl)-thiosemicarbazone] potentiated the effect of norfloxacin in resistant bacteria; however, there are no reports on their effects on Nauphoeta cinerea in the literature. The objective of this work was to evaluate the behavioral effects and oxidative markers of NW05 and NJ20 in lobster cockroach N. cinerea. To evaluate the behavioral study, a video tracking software was used to evaluate the locomotor points and the exploratory profile of cockroaches in the horizontal and vertical regions of a new environment. The total concentration of thiol and reduced glutathione (GSH), substances reactive to thiobarbituric acid (TBARS), free iron (II) content and mitochondrial viability were determined. The antioxidant potential was evaluated by the DPPH method. Both substances induced changes in the behavior of cockroaches, showing a significant reduction in the total distance covered and in the speed. In the cell viability test (MTT), there was a significant reduction for NJ20 (1 mM). NJ20 caused a significant increase in total levels of thiol and non-protein thiol (NPSH), although it also slightly increased the content of malondialdehyde (MDA). Both compounds (NW05 and NJ20) caused a significant reduction in the content of free iron at a concentration of 10 mM. In conclusion, the compound NJ20 caused moderate neurotoxicity (1 mM), but had good antioxidant action, while NW05 did not show toxicity or significant antioxidant activity in the model organism tested. It is desirable to carry out complementary tests related to the antioxidant prospection of these same compounds, evaluating them at different concentrations.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Neurolocomotor Behavior and Oxidative Stress Markers of Thiazole and Thiazolidinedione Derivatives against Nauphoeta cinerea

et al. 2022

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“…ADME calculations were also assessed for the synthesized compound where compound 24a showed good drug‐likeliness properties with only a single violation and hence can be considered an orally active drug candidate. [ 87 ]…”

Section: Biological Spectrum Of Tzdsmentioning

confidence: 99%

“…Further, compounds were also screened properties with only a single violation and hence can be considered an orally active drug candidate. [87] A new series of new thiazolidine-2,4-dione based halogenbenzohydrazones and pyridinecarbohydrazone derivatives were synthesized and biologically evaluated (25-27, Figure 11) by Trotsko et al…”

Section: Characterization Of the Tzd Corementioning

confidence: 99%

The medicinal perspective of 2,4‐thiazolidinediones based ligands as antimicrobial, antitumor and antidiabetic agents: A review

Singh

Kajal

Pradhan

et al. 2022

Archiv der Pharmazie

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2,4-Thiazolidinedione (2,4-TZD), commonly known as glitazone, is a ubiquitous heterocyclic pharmacophore possessing a plethora of pharmacological activities and offering a vast opportunity for structural modification. The diverse range of biological activities endowed with a novel mode of action, low cost, and easy synthesis has attracted the attention of medicinal chemists. Several researchers have integrated the TZD core with different structural fragments to develop a wide range of lead molecules against various clinical disorders. The most common sites for structural modifications at the 2,4-TZD nucleus are the N-3 and the active methylene at C-5. The review covers the recent development of TZD derivatives such as antimicrobial, anticancer, and antidiabetic agents. Various 2,4-TZD based agents or drugs, which are either under clinical development or in the market, are discussed in the study. Different synthetic methodologies for synthesizing the 2,4-TZD core are also included in the manuscript.The importance of various substitutions at N-3 and C-5 and the mechanisms of action and structure-activity relationships are also discussed. We hope this study will serve as a valuable tool for the scientific community engaged in the structural exploitation of the 2,4-TZD core for developing novel drug m\olecules for life-threatening ailments.

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Identification of novel C-15 fluoro isosteviol derivatives for GABA-AT inhibition by in silico investigations

Salaria

Akshinthala²,

Kapavarapu³

et al. 2023

J Mol Model

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Synthesis, In silico Molecular Docking and Pharmacokinetic Studies, In vitro Antimycobacterial and Antimicrobial Studies of New Imidozolones Clubbed with Thiazolidinedione

Abstract: The wet lab result for compound 3n along with Glide XP docking score and the calculated ADME parameters give the best choice for the preparation of new derivatives in order to improve antitubercular activity in future with more improved potency.

Cited by 13 publications

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Neurolocomotor Behavior and Oxidative Stress Markers of Thiazole and Thiazolidinedione Derivatives against Nauphoeta cinerea

Neurolocomotor Behavior and Oxidative Stress Markers of Thiazole and Thiazolidinedione Derivatives against Nauphoeta cinerea

The medicinal perspective of 2,4‐thiazolidinediones based ligands as antimicrobial, antitumor and antidiabetic agents: A review

Identification of novel C-15 fluoro isosteviol derivatives for GABA-AT inhibition by in silico investigations

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