Synthesis and biological evaluation of 3,4-dihydro-1H-[1,4] oxazepino [6,5,4-hi] indol-1-ones and 4,6-dihydrooxepino [5,4,3-cd] indol-1(3H)-ones as Mycobacterium tuberculosis inhibitors

Champciaux, Bastien; Raynaud, Clément; Viljoen, Albertus; Chêne, Loïc P.; Thibonnet, J.; Vincent, Stéphane; Kremer, Laurent; Thiery, Emilie

doi:10.1016/j.bmc.2021.116248

Cited by 6 publications

(2 citation statements)

References 31 publications

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“…Its derivatives possess a broad spectrum of biological activities, including antimicrobial [ 12 , 13 , 14 , 15 ], antitubercular [ 16 , 17 , 18 ], anti-tumor [ 19 , 20 , 21 , 22 , 23 ], antiviral [ 17 , 24 , 25 ], antioxidant [ 12 , 21 ], anti-inflammatory [ 17 , 25 , 26 , 27 ], antifungal [ 28 , 29 , 30 ], antimalarial [ 17 , 31 ], antidepressants [ 17 ], antidiabetic [ 25 , 26 , 32 ], аnti-Alzheimer’s [ 26 , 33 ], and antibacterial [ 26 , 34 ] properties.…”

Section: Introductionmentioning

confidence: 99%

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

2023

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Indoles and hydantoins are important heterocycles scaffolds which present in numerous bioactive compounds which possess various biological activities. Moreover, they are essential building blocks in organic synthesis, particularly for the preparation of important hybrid molecules. The series of hybrid compounds containing indoles and imidazolidin-2-one moiety with direct С─С bond were synthesized using an amidoalkylation one-pot reaction. All compounds were investigated as a growth regulator for germination, growth and development of wheat seeds (Triticum aestivum L). Their effect on drought resistance at very low concentrations (4 × 10−5 М) was evaluated. The study highlighted identified the leading compounds, 3a and 3e, with higher growth-regulating activity than the indole-auxin analogues.

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Section: Introductionmentioning

confidence: 99%

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

2023

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“…Indole is an important nitrogen-containing heterocyclic compound. Indole and indole derivatives have a broad spectrum of biological activities such as antifungal [ 20 , 21 , 22 , 23 , 24 , 25 , 26 ], antibacterial [ 27 , 28 , 29 ], antimycobacterial [ 30 ], antitubercular [ 31 , 32 , 33 ], antioxidant [ 34 ], antimalarial [ 35 , 36 , 37 ], antiviral [ 38 , 39 , 40 , 41 ], anti-leishmanial [ 42 , 43 ], anti-inflammatory [ 44 ], and anti-tumor [ 45 , 46 , 47 ] activities. The design and synthesis of new indole derivatives with excellent biological activity is one of the emerging fields in pharmaceutical chemistry.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Novel Indole Schiff Base Compounds and Their Antifungal Activities

et al. 2022

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A series of novel indole Schiff base derivatives (2a–2t) containing a 1,3,4-thiadiazole scaffold modified with a thioether group were synthesized, and their structures were confirmed using FT-IR, 1H NMR, 13C NMR, and HR-MS. In addition, the antifungal activity of synthesized indole derivatives was investigated against Fusarium graminearum (F. graminearum), Fusarium oxysporum (F. oxysporum), Fusariummoniliforme (F.moniliforme), Curvularia lunata (C. lunata), and Phytophthora parasitica var. nicotiana (P. p. var. nicotianae) using the mycelium growth rate method. Among the synthesized indole derivatives, compound 2j showed the highest inhibition rates of 100%, 95.7%, 89%, and 76.5% at a concentration of 500 μg/mL against F. graminearum, F. oxysporum, F.moniliforme, and P. p. var. nicotianae, respectively. Similarly, compounds 2j and 2q exhibited higher inhibition rates of 81.9% and 83.7% at a concentration of 500 μg/mL against C. lunata. In addition, compound 2j has been recognized as a potential compound for further investigation in the field of fungicides.

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