Synthesis and anticonvulsant properties of 1-(amino-N-arylmethanethio)-3-(1-substituted benzyl-2, 3-dioxoindolin-5-yl) urea derivatives

Siddiqui, Nadeem; Alam, Md Shamsher; Stables, James P.

doi:10.1016/j.ejmech.2011.03.004

Cited by 33 publications

(12 citation statements)

References 23 publications

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“…The results revealed that compound 31f was found active in MES screening while compounds 31h, 351, 31k and 31l showed significant anticonvulsant activity in both the screenings and were devoid of any neurotoxicity. Compound 31h and 31i showed marked protection at 300 mg/kg against MES and scPTZ screening 29 .…”

Section: Anticonvulsant Activitymentioning

confidence: 96%

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2021

IJPSR

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Section: Anticonvulsant Activitymentioning

confidence: 96%

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2021

IJPSR

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“…Compounds 2, 3 and N-benzylisatins were prepared by reported [24][25][26]32) procedures and their physical and spectral data are in accordance with the earlier reports. [24][25][26][32][33][34] General Method for Synthesis of Isatin Substituted Ciprofloxacin Derivatives (4-6) To a mixture of appropriate N-benzylisatin (1 mmol) and ciprofloxacin acid hydrazide…”

Section: Experimental Molecular Property Prediction Molsoft Molinspimentioning

confidence: 99%

Design, Synthesis and Pharmacological Evaluation of Some C<sub>3</sub> Heterocyclic-Substituted Ciprofloxacin Derivatives as Chimeric Antitubercular Agents

Niveditha¹,

Begum²,

Prathibha³

et al. 2020

CHEMICAL & PHARMACEUTICAL BULLETIN

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A series of new C 3 heterocyclic-substituted ciprofloxacin derivatives were prepared from ciprofloxacin acid hydrazide as possible chimeric molecules. They were evaluated for their possible in vitro antibacterial (agar cup/bore diffusion method) and antitubercular (Lowenstein-Jensen (LJ) slant method) activities. The results indicated that all the test compounds are highly effective against all the bacterial strains and have shown excellent anti-tubercular activity against normal, multidrug resistant and extensively drug resistant strains of Mycobacterium tuberculosis. They were found to be more potent antibacterial and antitubercular agents than the standard, ciprofloxacin. The minimum inhibitory concentration (MIC)'s of all the compounds against M. tuberculosis were found to be 0.0625 µg/mL as compared to ciprofloxacin (MIC 2 to > 8 µg/mL). Molecular docking studies were performed by using AUTODOCK 4.2 on the new ciprofloxacin derivatives at the active site of crystal structure of fluoroquinolones target enzyme Mtb DNA gyrase GyrA N-terminal domain (PDB ID: 3ILW) and also on the active site of crystal structure of chosen heterocyclics target enzyme enoyl-acyl carrier protein (ACP) reductase enzyme (PDB ID: 4TZK). Interestingly, almost all the compounds have shown relatively greater binding affinity at both the active sites than ciprofloxacin. Compound 6 exhibited the highest affinity for 3ILW and 4TZK.

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“…According to the reported literature, the 5-nitroisatin 2 was prepared [33]. In 500 ml round-bottomed flask (RBF), 0.33 mol of isatin (48.5 g) was added slowly to a mixture of 0.5 mol conc.…”

Section: Preparation Of 5-nitroisatin (2)mentioning

confidence: 99%

Design and Synthesis of Novel 1-((Dimethylamino)methyl)-3-(4-(3-(Substitute Dphenyl)-4-Oxothiazolidin-2-Yl)phenylimino)-5-Nitroindolin-2-Ones as Potent Antitubercular Agents

Lahari¹,

Sundararajan

2019

Asian J Pharm Clin Res

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Objective: Isatins have emerged as antimicrobial agents due to their broad spectrum of in vitro and in vivo antimicrobial activities. In addition, thiazolidinone also reported to possess various biological activities particularly antimicrobial activity. Due to the importance, we planned to synthesize compounds with isatin functionality coupled with thiazolidinone as possible antitubercular and antimicrobial agents which could furnish better therapeutic results. Methods: In vitro Mycobacterium tuberculosis method and agar streak dilution test are used to estimate antitubercular and antimicrobial potency of title analogs, respectively. Minimum inhibitory concentration of entire title compounds was determined against all tested microorganism such as M. tuberculosis, four Gram-positive, three Gram-negative bacteria, and two fungi. Results: A series of new thiazolidinone substituted Schiff and Mannich bases of 5-nitroisatins were designed and synthesized by a multistep synthesis from isatin. Structures of synthesized compounds are characterized using Fourier-transform infrared, proton nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. Mild to good antitubercular and antimicrobial activity was showed by synthesized 5-nitroisatin analogs. The relationship between the biological activity and the functional group variation of the tested compounds was discussed. Conclusion: 3-(4-(3-(4-Aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethyl amino)methyl)-5-nitroindolin-2-one 6 and 3-(4-(3- (2-aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethylamino)methyl)-5-nitroindolin-2-one 13 were found to be the most potent compounds of this series which might be extended as a novel class of antimicrobial agents.

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Synthesis and anticonvulsant properties of 1-(amino-N-arylmethanethio)-3-(1-substituted benzyl-2, 3-dioxoindolin-5-yl) urea derivatives

Cited by 33 publications

References 23 publications

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Design, Synthesis and Pharmacological Evaluation of Some C<sub>3</sub> Heterocyclic-Substituted Ciprofloxacin Derivatives as Chimeric Antitubercular Agents

Design and Synthesis of Novel 1-((Dimethylamino)methyl)-3-(4-(3-(Substitute Dphenyl)-4-Oxothiazolidin-2-Yl)phenylimino)-5-Nitroindolin-2-Ones as Potent Antitubercular Agents

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