Synthesis, antimicrobial and antioxidative activity of some new isatin derivatives

Sekularac, M Gavrilo; Nikolić, Biljana; Petrović, Predrag; Bugarski, Branko; Djurovic, Boban; Drmanic, Z Sasa

doi:10.2298/jsc140709084s

Cited by 14 publications

(17 citation statements)

References 14 publications

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“…Hence different derivatives of isatin like hydrazine derivatives, acetone and ketone derivatives, thiosemicarbazone derivates etc are being explored for their potential against tuberculosis, leprosy, fungal, viral and bacterial infections and Trypnosomiasis. Besides this, antioxidative activity of Isatin derivatives has also been reported [18].…”

Section: Mechanism Of Actionmentioning

confidence: 90%

“…The most potent antimicrobial compound was found to be 1,3dihydro-3-[(5-mercapto-1,3,4-thiadiazol-2-yl)imino]-2H--indol-2-one. All the isatin derivatives showed better antibacterial activity against gram positive bacteria as compared to gram negative bacteria [18]. Antifungal activity of 12 organic compounds derived from amino alcohols was measured.…”

Section: Antimicrobial Properties Of Functionally Substituted Chemicamentioning

confidence: 99%

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Functionally Substituted Chemical Organic Compounds: Potential Antimicrobial Substances

Ganbar¹

2019

OAJMB

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The development of resistance to antimicrobial agents is a global health problem for humans as well as animals. Over the past decade, the rate of microbial resistance to antibiotics has alarmingly increased. Factors contributing to this ever increasing antibiotic resistance pertain to microorganism as well as excessive and unwise use of the antibiotics. Biofilm formation and use of efflux pumps are the examples of microbial factors responsible for emergence of antimicrobial resistance. To ameliorate this condition, it is dire need of time to develop new antimicrobial agents. In this regard, chemical organic compounds are best available substances with potential antimicrobial properties. This review summarizes the antimicrobial activities of some important organic compounds as well as potential of functionally substituted chemical organic compounds as probable antimicrobial agents of future. These important organic compounds include functionally substituted derivatives of cyclohexane, quaternary ammonium compounds, hydrazones, pyrazolone, triazole, thiones, isatin, indole, chalcones, quinoxaline, anthraquinones, coumarins, thiophenes, piperidine, benzoxazolinone, phthalazinone, sulfones, thiazole and volatile organic compounds.

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Section: Mechanism Of Actionmentioning

confidence: 90%

Section: Antimicrobial Properties Of Functionally Substituted Chemicamentioning

confidence: 99%

Functionally Substituted Chemical Organic Compounds: Potential Antimicrobial Substances

Ganbar¹

2019

OAJMB

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“…The biological data used in this study were antimicrobial activity against Ecoli, (in terms oflog MIC), of a set of 86 isatin derivatives [29][30][31][32][33][34][35]. Firstly, the outlier data was removed from the data set according to principle component analysis, it was shown in Fig.…”

Section: Data Setmentioning

confidence: 99%

QSAR, Docking Study of Isatin Analogues as Anti-bacterial Agents for Design New Compounds

Sabet

Jafroudi

2019

JPRI

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Computational chemistry is unique method in drug discovery which reduce cost. In this study 86 molecules containing isatin core were subjected to quantitative structure-activity relationship analysis and docking study to find the structure requirements for ligand binding. The structures were sketched and optimized in Hyperchem. The structural invariants used in this study were those obtained from whole molecular structures: by both hyperchem and dragon software (16 types of descriptors). Four chemometrics methods including MLR, FA-MLR, PCR and GA-PLS were employed to make connection between structural parameters and anticancer effects. MLR analysis explained the positive effect of the number of urea derivatives, thio urea, amide, thioamide, hydrazone, thiocarbohydrazone, nBnz with the halogen substitution on 5 position of isatin ring on the antimicrobial activity. It also shows nArCN, nPyridines have negative effects on the antimicrobial activity of studied compound. The FA-MLR describes the effect of 3D-MORSE and Galvez Topological charge descriptors and on antimicrobial activity of the studied compounds. The quality of PCRA equation is better than those derived from FA-MLR. A comparison between the different statistical methods employed revealed that GA-PLS represented superior results and it could explain and predict 73% and 68% of variances in the –LogMIC data, respectively. Comparison between QSAR and docking analysis revealed that by decreasing in number of ring and lipophilicity (also Logp) for design of new compounds can have better activity. Substitutions such as urea, thiourea, thiocarbohydrazone, benzhydrazide as on isatin ring, can cause better interaction with receptor.

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“…1 Recently, a published study on the antimicrobial activity of isatin derivatives, performed by the agar dilution method, against selected strains of bacteria and one fungus, as well as on their antioxidative activity, showed that the examined isatin derivatives possessed moderate to significant activity. 2 Derivatives of isatin, as well as of its Schiff and Mannich bases, have already been reported to show a variety of biological activities, such as antibacterial, 3 antifungal 4 and anti-HIV activities. 5,6 However, to the best of our knowledge, there have hitherto been no reports on the solvatochromic effects of isatin derivatives.…”

Section: Introductionmentioning

confidence: 99%

Solvatochromism of isatin based Schiff bases: An LSER and LFER study

et al. 2016

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The derivatives of isatin have already been reported to show a variety of biological activities. However, there has been no report on solvatochromic effect of isatin derivatives so far, and that could be of interest to study and relate to their electronic structure, as a part of the characterisation of these compounds. Linear solvation energy relationships (LSER) were used to analyze solvent influence on the UV absorption maxima shifts of investigated isatin derivatives, i.e. isatin based Schiff bases, by using Kamlet-Taft model. Linear free energy relationships (LFER) were applied to the substituent-induced NMR chemical shifts (SCS) using SSP (single substituent parameter). The obtained correlations together with theoretical calculations gave insight into the influence of the molecular conformation on the transmission of substituent effects, as well as on solute/solvent interactions. The molecular electrostatic potential (MEP) surface map was plotted over the optimized geometry of the molecules in order to visualize electron density distribution and explain origin of solvent/solute interactions. [Projekat Ministarstva nauke Republike Srbije, br. 172013]

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Synthesis, antimicrobial and antioxidative activity of some new isatin derivatives

Cited by 14 publications

References 14 publications

Functionally Substituted Chemical Organic Compounds: Potential Antimicrobial Substances

Functionally Substituted Chemical Organic Compounds: Potential Antimicrobial Substances

QSAR, Docking Study of Isatin Analogues as Anti-bacterial Agents for Design New Compounds

Solvatochromism of isatin based Schiff bases: An LSER and LFER study

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