TLC Analysis of Mannich Bases Derived from Indolizines

Choulis, N.H.; Harrell, William B.

doi:10.1002/jps.2600600338

Cited by 2 publications

(2 citation statements)

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“…[9] Nevertheless, there are currently no systematic studies available in this field and only sporadic reports are present on the biological activity of indolizines. [10][11][12] The prior literature review suggests that various pharmacological activities, including anticancer, antimicrobial, antifungal, antiviral, VEGF Inhibitors, PDE5 A Inhibitor, antiviral, antiinflammatory, analgesic, and aromatase inhibitory, are exhibited by indolizine derivatives that are obtained through chemical modification. [13][14][15][16][17][18][19][20][21][22] For example, based on the patterns of core structure substitution, a number of indolizines have been found to display varying biological activity with potential therapeutic benefits.…”

Section: Introductionmentioning

confidence: 99%

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Design and Synthesis of 2‐Phenylindolizine Acetamides: Molecular Docking, in Vitro Antimicrobial and Anticancer Activity Evaluation

Kumar Gandham,

Jha,

Kudale

2024

Chemistry & Biodiversity

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In the present work, we synthesized a small library of 2‐phenylindolizine acetamide derivatives 7a‐i and studied their biological activity. The synthesis was accomplished starting with easily available starting material phenacyl bromide 1 proceeding through the key intermediate 6‐methyl‐7‐nitro‐2‐phenylindolizine 4. All the compounds 7a‐i were characterized using spectroscopy viz., 1H NMR, 13C NMR, FTIR, and mass spectrometry. Interestingly, 2‐phenylindolizine scaffolds 7c, 7f and 7g revealed a remarkable antibacterial activity against relevant organisms S. aureus, E. coli, S. pneumoniae, P. aeruginosa. The target compounds 7e and 7h showed excellent anticancer activity against Colo‐205 and MDA‐MB‐231 cell lines with IC50 values of 68.62, 62.91, 54.23 and 46.34 µM respectively. Additionally, all the 2‐phenylindolizine acetamide derivatives 7a‐i were subjected to molecular docking prediction by Autodock 4.2. Compounds 7a, 7f and 7c exhibited very good hydrogen bonding amino acid interactions Asp83 (2.23 Å), Asp83 (2.08 Å), His74 (2.05 Å), His76 (1.71 Å), Ser80 (1.05 Å) with active site of Topoisomerase–IV from S. pneumoniae (4KPE). Further, the compounds 7a‐i have revealed acceptable ranges for drug‐likeliness properties upon evaluation using SwissADME for ADMET and physiochemical properties.

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Section: Introductionmentioning

confidence: 99%

“…1‐Diethylaminomethyl‐3‐methyl‐2‐phenylindolizine was found to have antidepressant effects by Harrell and Doerge [9] . Nevertheless, there are currently no systematic studies available in this field and only sporadic reports are present on the biological activity of indolizines [10–12] …”

Section: Introductionmentioning

confidence: 99%