Synthesis, Anti-Bacterial and Antioxidant Properties of Ethyl 7-Amino-3-Benzoyl-2-Methylindolizine-1-Carboxylate Derivatives.

Uppar, Vijayakumar; Basarikatti, Atiyaparveen I.; Padmashali, Basavaraj; Chandrashekharappa, Sandeep; Chougala, Mallikarjun; Mudnakudu-Nagaraju, Kiran Kumar; Mohan, Mahendra K.; Banuprakash, Govindappa; Ningegowda, Raghu; Rachotimath, Beena B

doi:10.1063/5.0022905

Cited by 5 publications

(3 citation statements)

References 29 publications

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“…For instance, recent publications from V. Uppar et al (2020) and others shows that pyrrolo[1,2-a]quinoline derivatives effectively inhibit the activity of microbial pathogens such as bacteria (both Gram-positive and Gram-negative) [ 44 , 53 , 54 , 55 , 56 ], and fungus [ 57 ], followed by various disease conditions such as cancer [ 58 ], malaria [ 59 ], inflammation [ 60 ] and Alzheimer disease [ 61 ]. In addition, these derivatives possess antioxidant activity [ 44 , 54 , 55 , 56 ]. Further, ethyl-1-(subbenzoyl)-5-methylpyrrolo[1,2-a]quinoline-3-carboxylate and dimethyl 1-(subbenzoyl)-5-methylpyrrolo[1,2-a]quinoline-2,3-dicarboxylate derivatives have been tested for their larvicidal activity against Anopheles arabiensis [ 56 ].…”

Section: Introductionmentioning

confidence: 99%

“…Collectively, the broad-spectrum nature of the compounds intensified further to investigate whether newly synthesized derivatives target C. albicans fungal pathogens. Herein, the synthesized dimethyl-4-bromo-1-(4-substituted benzoyl) pyrrolo[1,2-a]quinoline-2,3-dicarboxylate methyl 4-bromo-1-(4-sub-benzoyl)pyrrolo[1,2-a]quinoline-3-carboxylate 1a-n ( Scheme 1 ) [ 55 ], a novel analogue derivative ( Figure 1 ), was tested for its inhibitory activity against C. albicans in vitro. As shown in Figure 1 , these derivatives consist of methyl ester groups present at the second and third positions (highlighted) of BQ-01, 03, 05 and 07, and only one ester group at the third position of BQ-02, 04, 06 and 08.…”

Section: Introductionmentioning

confidence: 99%

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Investigation of Antifungal Properties of Synthetic Dimethyl-4-Bromo-1-(Substituted Benzoyl) Pyrrolo[1,2-a] Quinoline-2,3-Dicarboxylates Analogues: Molecular Docking Studies and Conceptual DFT-Based Chemical Reactivity Descriptors and Pharmacokinetics Evaluation

et al. 2021

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Candida albicans, an opportunistic fungal pathogen, frequently colonizes immune-compromised patients and causes mild to severe systemic reactions. Only few antifungal drugs are currently in use for therapeutic treatment. However, evolution of a drug-resistant C. albicans fungal pathogen is of major concern in the treatment of patients, hence the clinical need for novel drug design and development. In this study, in vitro screening of novel putative pyrrolo[1,2-a]quinoline derivatives as the lead drug targets and in silico prediction of the binding potential of these lead molecules against C. albicans pathogenic proteins, such as secreted aspartic protease 3 (SAP3; 2H6T), surface protein β-glucanase (3N9K) and sterol 14-alpha demethylase (5TZ1), were carried out by molecular docking analyses. Further, biological activity-based QSAR and theoretical pharmacokinetic analysis were analyzed. Here, in vitro screening of novel analogue derivatives as drug targets against C. albicans showed inhibitory potential in the concentration of 0.4 µg for BQ-06, 07 and 08, 0.8 µg for BQ-01, 03, and 05, 1.6 µg for BQ-04 and 12.5 µg for BQ-02 in comparison to the standard antifungal drug fluconazole in the concentration of 30 µg. Further, in silico analysis of BQ-01, 03, 05 and 07 analogues docked on chimeric 2H6T, 3N9K and 5TZ1 revealed that these analogues show potential binding affinity, which is different from the therapeutic antifungal drug fluconazole. In addition, these molecules possess good drug-like properties based on the determination of conceptual Density Functional Theory (DFT)-based descriptors, QSAR and pharmacokinetics. Thus, the study offers significant insight into employing pyrrolo[1,2-a]quinoline analogues as novel antifungal agents against C. albicans that warrants further investigation.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Investigation of Antifungal Properties of Synthetic Dimethyl-4-Bromo-1-(Substituted Benzoyl) Pyrrolo[1,2-a] Quinoline-2,3-Dicarboxylates Analogues: Molecular Docking Studies and Conceptual DFT-Based Chemical Reactivity Descriptors and Pharmacokinetics Evaluation

et al. 2021

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“…Plants have been used as a source of raw material for remedies since ancient practice and several of them are globally recognized as medicine [1]. They contain biologically active constituents to protect human beings and such constituents act as protective agents against several human ailments steps such as mortal carcinogenesis, performing origination, development phases, or terminating the DNA destructing cell mutations.…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial, anti-inflammatory, and anticancer activities of leaves extracts of Filicium decipiens

Basarikatti¹,

Mishra²,

Uppar³

et al. 2021

J App Biol Biotech

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Filicium decipiens (fern-tree) belongs to the family Sapindaceae. It grows in Asia and Africa region and is traditionally used for diabetes treatment in India. The plant has been documented to have molluscicidal, diabetic nephropathy, and anti-inflammatory properties. In the present study, experimental data on different leaves extracts of F. decipiens were collected for their preliminary phytochemical investigations along with antimicrobial, anti-inflammatory, and anticancer activities using in-vitro assays. The phytochemical investigations display the existence of alkaloids, tannins, flavonoids, saponins, glycosides, steroids, triterpenoids, and carbohydrates in the extracts prepared using three different solvents. Antimicrobial property was established against six bacterial and fungal strains. Petroleum ether extract exhibited higher antimicrobial activity as compared to chloroform and water extract. Anti-inflammatory assay was performed on RAW264.7 murine macrophage cells and petroleum ether extract exhibited reduced nitrite oxide production having IC 50 value 493.7 µg/ml. Cytotoxicity was determined against MCF-7 (Breast) and A-549 (Lung) cancer cells and paclitaxel was used as a standard drug, whereas cytocompatibility was assessed against mouse fibroblast cells (L929). Different sensitivities were observed against different study cell lines in a dosedependent manner. These study findings may provide biological evidence for the application of Filicium decipiens extract.

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The cyclization and functionalization reactions involving N-phenacylpyridinium salts

Doraghi,

Serajian,

Karimian

et al. 2024

Chem. Pap.

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Synthesis, Anti-Bacterial and Antioxidant Properties of Ethyl 7-Amino-3-Benzoyl-2-Methylindolizine-1-Carboxylate Derivatives.

Cited by 5 publications

References 29 publications

Investigation of Antifungal Properties of Synthetic Dimethyl-4-Bromo-1-(Substituted Benzoyl) Pyrrolo[1,2-a] Quinoline-2,3-Dicarboxylates Analogues: Molecular Docking Studies and Conceptual DFT-Based Chemical Reactivity Descriptors and Pharmacokinetics Evaluation

Investigation of Antifungal Properties of Synthetic Dimethyl-4-Bromo-1-(Substituted Benzoyl) Pyrrolo[1,2-a] Quinoline-2,3-Dicarboxylates Analogues: Molecular Docking Studies and Conceptual DFT-Based Chemical Reactivity Descriptors and Pharmacokinetics Evaluation

Antimicrobial, anti-inflammatory, and anticancer activities of leaves extracts of Filicium decipiens

The cyclization and functionalization reactions involving N-phenacylpyridinium salts

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