871883-56-6Relevant articles and documents
Synthesis, characterization, and antileishmanial activity of certain quinoline-4-carboxylic acids
Abdelwahid, Mazin A. S.,Elsaman, Tilal,Mohamed, Malik S.,Latif, Sara A.,Mukhtar, Moawia M.,Mohamed, Magdi A.
, (2019)
Leishmaniasis is a fatal neglected parasitic disease caused by protozoa of the genus Leishmania and transmitted to humans by different species of phlebotomine sandflies. The disease incidence continues to increase due to lack of vaccines and prophylactic drugs. Drugs commonly used for the treatment are frequently toxic and highly expensive. The problem of these drugs is further complicated by the development of resistance. Thus, there is an urgent need to develop new antileishmanial drug candidates. The aim of this study was to synthesize certain quinoline-4-carboxylic acids, confirm their chemical structures, and evaluate their antileishmanial activity. Pfitzinger reaction was employed to synthesize fifteen quinoline-4-carboxylic acids (Q1-Q15) by reacting equimolar mixtures of isatin derivatives and appropriate α-methyl ketone. The products were purified, and their respective chemical structures were deduced using various spectral tools (IR, MS, 1H NMR, and 13C NMR). Then, they were investigated against L. donovani promastigote (clinical isolate) in different concentration levels (200 μg/mL to 1.56 μg/mL) against sodium stibogluconate and amphotericin B as positive controls. The IC50 for each compound was determined and manipulated statistically. Among these compounds, Q1 (2-methylquinoline-4-carboxylic acid) was found to be the most active in terms of IC50.
A computational study of molecular interactions and in vitro antibacterial activity of 6-substituted quinoline carboxylic acid derivatives as DNA gyrase inhibitors
Dubey, Sonal,Bhardwaj, Sakshi,Singh, Ekta,Prabhakaran, Prabitha,Cherian, Ayda
, p. 643 - 653 (2018/06/06)
Background: Quinoline nucleus is found in a vast range of biologically active compounds. The quinoline group of compounds which are anti-infective in nature are found to act by inhibiting different enzymes. DNA gyrase being one of the more common site of
STAT3 INHIBITOR CONTAINING QUINOLINECARBOXAMIDE DERIVATIVE AS ACTIVE INGREDIENT
-
Page/Page column 65, (2011/06/24)
The present invention provides a STAT3 inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR34; and Rs