Article ; Online: Novel (quinolin-8-yl-oxy)-pyrazole/thiophene derivatives
Results in Chemistry, Vol 4, Iss , Pp 100281- (2022)
Synthesis, characterization and their pharmacological evaluation
2022
Abstract: Two novel series of pyrazole and thiophene-linked quinoline analogues via amide bond were conveniently synthesized and characterized by IR, NMR, and HRMS analysis. The synthesized compounds were evaluated for their antimicrobial, anti-inflammatory, and ... ...
Abstract | Two novel series of pyrazole and thiophene-linked quinoline analogues via amide bond were conveniently synthesized and characterized by IR, NMR, and HRMS analysis. The synthesized compounds were evaluated for their antimicrobial, anti-inflammatory, and anti-leukemic activity. The antimicrobial evaluation of the target compounds clearly showed that compound 11c has better activity compared to other compounds against tested pathogens. The anti-inflammatory assay of the selected compounds showed that 12c with IC50 value 118.73 µg/ml exhibited significant activity than standard drug Aspirin (IC50, 107.75 µg/ml). The compound 12a out of the twelve newly prepared quinoline heterocycles displayed superior antileukemic activity and was comparable with the standard drug against human monocytic leukemia cell lines (THP-1). Representing the two different quinolinyl-pyrazole/thiophene analogues, compounds 11d, 11e, and 12a displayed the remarkable cytotoxicity against THP-1 cell lines with IC50 values 112.46, 105.42, and 98.88 µg/ml respectively. |
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Keywords | 8-Hydroxyquinoline ; Pyrazole ; Thiophene ; Antimicrobial ; Anti-inflammatory ; Antileukemic ; Chemistry ; QD1-999 |
Subject code | 540 |
Language | English |
Publishing date | 2022-01-01T00:00:00Z |
Publisher | Elsevier |
Document type | Article ; Online |
Database | BASE - Bielefeld Academic Search Engine (life sciences selection) |
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