In:
ChemistrySelect, Wiley, Vol. 3, No. 27 ( 2018-07-23), p. 7813-7821
Abstract:
A series of novel ethyl 9‐(trifluoromethyl) pyrido [2′, 3′:3,4]pyrazolo[1, 5‐ a ]quinazoline‐8‐carboxylate 4 , 9‐(trifluoromethyl)pyrido[2′, 3′:3,4]pyrazolo[1, 5‐ a ]quinazoline‐8‐carboxylic acid 5, aryl amide functionalized pyrido[2′, 3′:3,4]pyrazolo [1, 5‐ a ] quinazoline derivatives 6 a‐f , secondary amide functionalized pyrido[2′, 3′:3,4] pyrazolo[1, 5‐ a ]quinazoline derivatives 7 a‐d and primary amide functionalized pyrido[2′, 3′:3,4]pyrazolo[1, 5‐ a ] quinazoline derivatives 8 a‐h were prepared starting from 2(1 H )pyridone 1 . All the compounds were evaluated for antibacterial activity against Gram‐positive and Gram‐negative bacterial strains and the compounds 5 , 6 a , 6 c , 6 f , 7 a , 8 c , 8 f and 8 h exhibited promising antibacterial activity against various bacterial strains. Compound 5 showed high antibacterial (MIC value of 3.9 μg/mL) and broad‐spectrum anti bio‐film activity. Compound 5 and 8 b also showed good antifungal activity against the tested panel of various Candida strains. Molecular docking studies revealed that, the compound 5 and 8 b showed good binding interactions and corroborates with the antifungal results. All the compounds also screened for cytotoxicity and the compounds 7 d , 8 a , 8 b and 8 d exhibited above 90% inhibition against MCF7 (breast) cancer cell line and the compounds 6 d , 7 a , 8 a , 8 b , 8 f and 8 g exhibited above 90% inhibition against SKOV3 (ovarian) cell line, with reference to Doxorubicin (Control) drug in terms of inhibition.
Type of Medium:
Online Resource
ISSN:
2365-6549
,
2365-6549
DOI:
10.1002/slct.201801186
Language:
English
Publisher:
Wiley
Publication Date:
2018
detail.hit.zdb_id:
2844262-3
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