Design, Synthesis, and Biological Evaluation of Novel Quinazoline Derivatives as Anti-inflammatory Agents against Lipopolysaccharide-induced Acute Lung Injury in Rats

Abstract We described here the synthesis and biological evaluation of a series of 2, 4, 6-trisubstituted quinazoline derivatives as potential anti-inflammatory, analgesic and antibacterial agents. The synthesized compounds were characterized by FTIR, 1H NMR and mass spectroscopy analysis. We found that the compounds 6b, 6e, 6g, 6h and 6j showed better anti-inflammatory activity than indomethacin. Compounds 6b, 6e, 6h, 6j and 6l were found to exhibit appreciable analgesic activity, and 6b, 6g and 6k showed good antibacterial activity against Gram (+) bacteria: B. subtilis, S. aureus, S. epidermis, and Gram (-) bacteria: E. coli, P. aeruginosa and K. pneumoniae. Compound 6b showed overall better anti-inflammatory, analgesic and antibacterial activity among the synthesized compounds. The results of the present study could be helpful for the designing of effective anti-inflammatory, analgesic and antibacterial agents.

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Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2021.116265 ◽

2021 ◽

Vol 43 ◽

pp. 116265

Author(s):

Zhengjie Wang ◽

Limin Liu ◽

Honglin Dai ◽

Xiaojie Si ◽

Luye Zhang ◽

...

Keyword(s):

Signaling Pathway ◽

Biological Evaluation ◽

Pi3k Signaling ◽

Design Synthesis ◽

Pi3k Signaling Pathway ◽

Quinazoline Derivatives ◽

Synthesis And Biological Evaluation

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Design, synthesis and bioactivity evaluation of fisetin derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2021.116456 ◽

2021 ◽

pp. 116456

Author(s):

Xiemin Wang ◽

Jun Yang ◽

Bingyu Ding ◽

Pan Chen ◽

Zhengwei Xu ◽

...

Keyword(s):

Acute Lung Injury ◽

Lung Injury ◽

Design Synthesis ◽

Anti Inflammatory

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Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

International Journal of Scientific Research in Science and Technology ◽

10.32628/ijsrst196535 ◽

2019 ◽

pp. 300-307

Author(s):

Asma D. Ambekari ◽

Shrinivas K. Mohite

Keyword(s):

Antimicrobial Activity ◽

Mass Spectra ◽

Biological Evaluation ◽

Design Synthesis ◽

Pyridine Moiety ◽

Anti Inflammatory ◽

Physicochemical Data ◽

Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

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