e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521

Structure-activity relationships for antiplasmodial activity among 7-substituted 4-aminoquinolines

…, FM Krogstad, LD Byers, DJ Krogstad

Index: De, Dibyendu; Krogstad, Frances M.; Byers, Larry D.; Krogstad, Donald J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 25 p. 4918 - 4926

Full Text: HTML

Citation Number: 170

Abstract

Aminoquinolines (AQs) with diaminoalkane side chains (-HNRNEt2) shorter or longer than the isopentyl side chain [-HNCHMe (CH2) 3NEt2] of chloroquine are active against both chloroquine-susceptible and-resistant Plasmodium falciparum.(De, D.; et al. Am. J. Trop. Med. Hyg. 1996, 55, 579-583). In the studies reported here, we examined structure-activity relationships (SARs) among AQs with different N, N-diethyldiaminoalkane side chains and ...

7-FLUOROQUINOLIN-4-OL Structure

7-FLUOROQUINOLI...

~%

4-Chloro-7-fluoroquinoline Structure

4-Chloro-7-fluo...

N/A Structure

~%

4-Chloro-7-fluoroquinoline Structure

4-Chloro-7-fluo...

7-Fluoro-4-hydroxyquinoline-3-carboxylic acid Structure

7-Fluoro-4-hydr...

~%

4-Chloro-7-fluoroquinoline Structure

4-Chloro-7-fluo...

ethyl 7-fluoro-4-oxo-1H-quinoline-3-carboxylate Structure

ethyl 7-fluoro-...

~%

4-Chloro-7-fluoroquinoline Structure

4-Chloro-7-fluo...

3-Iodoaniline Structure

~%

4-HYDROXY-7-IODOQUINOLINE Structure

4-HYDROXY-7-IOD...

N/A Structure

~%

ETHYL 7-BROMO-4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXYLATE Structure

ETHYL 7-BROMO-4...

4-hydroxy-7-iodo-quinoline-3-carboxylic acid Structure

4-hydroxy-7-iod...

~%

N',N'-diethyl-N-(7-iodoquinolin-4-yl)ethane-1,2-diamine Structure

N',N'-diethyl-N...

4-hydroxy-7-iodo-quinoline-3-carboxylic acid ethyl ester Structure

4-hydroxy-7-iod...

~%

N',N'-diethyl-N-(7-iodoquinolin-4-yl)ethane-1,2-diamine Structure

N',N'-diethyl-N...

N/A Structure

~%

N',N'-diethyl-N-(7-iodoquinolin-4-yl)ethane-1,2-diamine Structure

N',N'-diethyl-N...

3-Iodoaniline Structure

~%

N',N'-diethyl-N-(7-iodoquinolin-4-yl)ethane-1,2-diamine Structure

N',N'-diethyl-N...

4-HYDROXY-7-IODOQUINOLINE Structure

4-HYDROXY-7-IOD...

~%

N',N'-diethyl-N-(7-iodoquinolin-4-yl)ethane-1,2-diamine Structure

N',N'-diethyl-N...

4-Chloro-7-iodoquinoline Structure

4-Chloro-7-iodo...

2-aminoethyldiethylamine Structure

2-aminoethyldie...

~%

N',N'-diethyl-N-(7-iodoquinolin-4-yl)ethane-1,2-diamine Structure

N',N'-diethyl-N...

3-anisidine Structure

Diethyl ethoxymethylenemalonate Structure

Diethyl ethoxym...

~99%

2-[(3-METHOXYPHENYLAMINO)-METHYLENE]MALONIC ACID DIETHYL ESTER Structure

2-[(3-METHOXYPH...

3-(Trifluoromethyl)aniline Structure

3-(Trifluoromet...

Diethyl ethoxymethylenemalonate Structure

Diethyl ethoxym...

~97%

Propanedioic acid,2-[[[3-(trifluoromethyl)phenyl]amino]methylene]-, 1,3-diethyl ester Structure

Propanedioic ac...

3-anisidine Structure

~%

4-Hydroxy-7-methoxyquinoline-3-carboxylic acid Structure

4-Hydroxy-7-met...

4-Hydroxy-7-methoxyquinoline-3-carboxylic acid Structure

4-Hydroxy-7-met...

~%

1,4-Pentanediamine,N1,N1-diethyl-N4-(7-methoxy-4-quinolinyl)- Structure

1,4-Pentanediam...

Ethyl 4-hydroxy-7-methoxy-3-quinolinecarboxylate Structure

Ethyl 4-hydroxy...

~%

1,4-Pentanediamine,N1,N1-diethyl-N4-(7-methoxy-4-quinolinyl)- Structure

1,4-Pentanediam...

2-[(3-METHOXYPHENYLAMINO)-METHYLENE]MALONIC ACID DIETHYL ESTER Structure

2-[(3-METHOXYPH...

~%

1,4-Pentanediamine,N1,N1-diethyl-N4-(7-methoxy-4-quinolinyl)- Structure

1,4-Pentanediam...

3-anisidine Structure

~%

1,4-Pentanediamine,N1,N1-diethyl-N4-(7-methoxy-4-quinolinyl)- Structure

1,4-Pentanediam...

7-Methoxy-4-quinolinol Structure

7-Methoxy-4-qui...

~%

1,4-Pentanediamine,N1,N1-diethyl-N4-(7-methoxy-4-quinolinyl)- Structure

1,4-Pentanediam...

3-fluoroaniline Structure

3-fluoroaniline

~%

ethyl 7-fluoro-4-oxo-1H-quinoline-3-carboxylate Structure

ethyl 7-fluoro-...