Synthesis, characterization, and evaluation of antioxidant, antimicrobial and drug likeness properties of indole containing 1,3,4-oxadiazoles

被引:1
作者
Madugula, Aravinda Kumar [1 ]
Kiran, Bachina [2 ]
Dendukuri, B. N. Suresh Varma [3 ]
Kishore, T. V. N. [4 ]
Rao, P. Srinivasa [1 ]
Ranagaih, Gururaja [1 ]
Jagadeesh, K. [3 ]
机构
[1] PRIST Univ, Ponnaiyah Ramajayam Inst Sci & Technol, Ctr Res & Dev, Thanjavur 613403, India
[2] BV Raju Coll, Bhimavaram 534202, Andhra Pradesh, India
[3] Shri Vishnu Engn Coll Women, Dept Chem, Bhimavaram 534202, Andhra Pradesh, India
[4] Andhra Univ, Dept Chem, Visakhapatnam 530003, Andhra Pradesh, India
关键词
Indole; 4-oxadiazole; Hybrid compound; Characterization; Biological evaluation; Drug likeness; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; DERIVATIVES; OXADIAZOLES; DESIGN;
D O I
10.1016/j.rechem.2024.101664
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
We have synthesized fourteen new 1,3,4-oxadiazole hybrid compounds (68a-68n) that contain indole. The characterization of fourteen new indolo-3,4-oxadiazoles derivatives (68a-68n) was performed using techniques such as Proton Nucelar Magnetic Resonance (1H NMR) and Liquid Chromatography - Mass spectrometry (LCMS). All indolo-3,4-oxadiazoles derivatives (68a-68n) were examined for its antioxidant and antibacterial properties in in-vitro conditions. The scavenging activity was measured in order to assess their antioxidant capabilities. Among 14 compounds, 68a, 68i and 68n showed better scavenging activity. The antibacterial activity of all indolo-3,4-oxadiazoles derivatives (68a-68n) was tested against Staphylococcus aureus, Escherichia coli, Pseudomonas aeroginosa and Klebsiella pneumonia. All of the compounds (68a-n) exhibited moderate to significant activity. The indolo-3,4-oxadiazoles derivatives 68b, 68e, 68h and 68j shown more effectiveness against Staphylococcus aureus, Escherichia coli, Pseudomonas aeroginosa. The drug-likeness property of all indolo-3,4oxadiazoles derivatives (68a-68n) was tested following Lipinski's policies. The compounds (68a-68n) are all in accordance with Lipinski's policies and proved to have enhanced oral bioavailability.
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页数:9
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