Synthesis and Antibacterial Activity of 2-Morpholino-1-propyl-1<i>H</i>-indole-3-substituted Acylhydrazone Derivatives

巫受群,; 李小琴,; 孟娇,; 甘宜远,; 田坤,; 王贞超,; 欧阳贵平,

doi:10.6023/cjoc201712030

Cited by 3 publications

(3 citation statements)

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“…1,2-Substituted-1H-indole-3-carbaldehydes (8 and 10～ 11) were prepared according to literature procedures. [29,24,30] The physical and spectral data of the prepared compounds 8 and 10～11 were consistent with those in the literature [29,24,30] .…”

Section: Synthesis Of 1h-indole-3-carbaldehyde Derivativessupporting

confidence: 88%

Novel 3-Thioether-4-indolimino-4H-1,2,4-triazole Derivatives Bearing Pyridyl Moiety: Design, Synthesis and Bioactivity Evaluation in vitro

Qi¹,

Liu²,

Li³

et al. 2021

Chinese Journal of Organic Chemistry

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Section: Synthesis Of 1h-indole-3-carbaldehyde Derivativessupporting

confidence: 88%

Novel 3-Thioether-4-indolimino-4H-1,2,4-triazole Derivatives Bearing Pyridyl Moiety: Design, Synthesis and Bioactivity Evaluation in vitro

Qi¹,

Liu²,

Li³

et al. 2021

Chinese Journal of Organic Chemistry

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“…Further study revealed that incorporation of metal ions such as copper(II), cobalt(II), nickel(II), and zinc(II) into the indole‐carbohydrazide hybrids could boost up the activity to some extent, and complexes 72a–d (inhibition zone: 11.15–13.68 mm at 100 μg/ml) were more active than their ligand (inhibition zone: 10.12–10.31 mm at 100 μg/ml) against B. subtilis , E. coli , and S. typhi . [ 146,147 ] The mechanistic study indicated that complexes 72a,b could exhibit their antibacterial activity through DNA cleavage.…”

Section: Indole/isatin–imine Hybridsmentioning

confidence: 99%

Indole/isatin‐containing hybrids as potential antibacterial agents

Song

Bian

et al. 2020

Archiv der Pharmazie

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The emergence and worldwide spread of drug-resistant bacteria have already posed a serious threat to human life, creating the urgent need to develop potent and novel antibacterial drug candidates with high efficacy. Indole and isatin (indole-2,3-dione) present a wide structural and mechanistic diversity, so their derivatives possess various pharmacological properties and occupy a salient place in the development of new drugs. Indole/isatin-containing hybrids, which demonstrate a promising activity against a panel of clinically important Gram-positive and Gram-negative bacteria, are privileged scaffolds for the discovery of novel antibacterial candidates. This review, covering articles published between January 2015 and May 2020, focuses on the development and structure-activity relationship (SAR) of indole/isatincontaining hybrids with potential application for fighting bacterial infections, to facilitate further rational design of novel drug candidates.

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“…As a representative example, indole has pleasing odors at low concentrations and has been widely applied as an additive in food and perfume production . Some analogues derived from indole possess a broad spectrum of biological activities, including bactericidal, − fungicidal, − anticancer, , antiviral, and insecticidal − activities as well (Figure a). The research on indole derivatives has consequently always been one of the hot spots in drug discovery and pesticide development, attracting considerable attention. , Nevertheless, though indoles have exhibited great potential in agrochemical development, there have been insufficient indole-containing commercial pesticides applied in the field to date.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antibacterial Activity, and Mechanisms of Novel Indole Derivatives Containing Pyridinium Moieties

Yang

et al. 2022

J. Agric. Food Chem.

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The development of effective antibacterial agents equipped with novel action modes and unique skeletons starting from natural compounds serves as an important strategy in the modern pesticide industry. Disclosed here are a series of novel indole derivatives containing pyridinium moieties and their antibacterial activity evaluation against two prevalent phytopathogenic bacteria, Xanthomonas oryzae pv. oryzicola (Xoc) and X. oryzae pv. oryzae (Xoo). A three-dimensional (3D)-QSAR model was adopted to discover higher activity like title compounds based on the Xoc antibacterial activity of the tested compounds. Compound 43 was consequently designed, and it displayed higher antibacterial activity as expected with the half-maximal effective concentration EC50 values of 1.0 and 1.9 μg/mL for Xoo and Xoc, respectively, which were better than those of the commercial drug thiodiazole copper (TC) (72.9 and 87.5 μg/mL). Under greenhouse conditions, the results of a rice in vivo pot experiment indicated that the protective and curative activities of compound 43 against rice bacterial leaf streak (BLS) and rice bacterial blight (BLB) were 45.0 and 44.0% and 42.0 and 39.3%, respectively, which were better than those of the commercial agent thiodiazole copper (38.0 and 37.9%, 38.6 and 37.0%) as well. Scanning electron microscopy images, defense enzyme activity tests, and proteomic techniques were utilized in a preliminary mechanism study, suggesting that compound 43 shall modulate and interfere with the physiological processes and functions of pathogenic bacteria.

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Synthesis and Antibacterial Activity of 2-Morpholino-1-propyl-1H-indole-3-substituted Acylhydrazone Derivatives

Cited by 3 publications

References 0 publications

Novel 3-Thioether-4-indolimino-4H-1,2,4-triazole Derivatives Bearing Pyridyl Moiety: Design, Synthesis and Bioactivity Evaluation in vitro

Novel 3-Thioether-4-indolimino-4H-1,2,4-triazole Derivatives Bearing Pyridyl Moiety: Design, Synthesis and Bioactivity Evaluation in vitro

Indole/isatin‐containing hybrids as potential antibacterial agents

Synthesis, Antibacterial Activity, and Mechanisms of Novel Indole Derivatives Containing Pyridinium Moieties

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