Skip to content
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis and evaluation of 7-chloro-4-(piperazin-1-yl)quinoline- sulfonamide as hybrid antiprotozoal agents
Bioorganic and Medicinal Chemistry, Volume 21, No. 11, Year 2013
Notification
URL copied to clipboard!
Description
A new series of 4-aminochloroquinoline based sulfonamides were synthesized and evaluated for antiamoebic and antimalarial activities. Out of the eleven compounds evaluated (F1-F11), two of them (F3 and F10) showed good activity against Entamoeba histolytica (IC50 <5 μM). Three of the compounds (F5, F7 and F8) also displayed antimalarial activity against the chloroquine-resistant (FCR-3) strain of Plasmodium falciparum with IC 50 values of 2 μM. Compound F7, whose crystal structure was also determined, inhibited β-haematin formation more potently than quinine. To further understand the action of hybrid molecules F7 and F8, molecular docking was carried out against the homology model of P. falciparum enzyme dihydropteroate synthase (PfDHPS). The complexes showed that the inhibitors place themselves nicely into the active site of the enzyme and exhibit interaction energy which is in accordance with our activity profile data. Application of Lipinski 'rule of five' on all the compounds (F1-F11) suggested high drug likeness of F7 and F8, similar to quinine. © 2013 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Salahuddin, Attar
India, New Delhi
Jamia Millia Islamia
Inam, Afreen
India, New Delhi
Jamia Millia Islamia
van Zyl, Robyn Lynne
South Africa, Johannesburg
University of the Witwatersrand Faculty of Health Sciences
Heslop, Donovan C.
South Africa, Johannesburg
University of the Witwatersrand Faculty of Health Sciences
Chen, Chien Teng
South Africa, Johannesburg
University of the Witwatersrand Faculty of Health Sciences
Avecilla, Fernando
Spain, A Coruna
Universidade da Coruña
Agarwal, Subhash M.
India, Noida
Institute of Cytology and Preventive Oncology Noida
Azam, Amir
India, New Delhi
Jamia Millia Islamia
Statistics
Citations: 51
Authors: 8
Affiliations: 4
Identifiers
Doi:
10.1016/j.bmc.2013.03.052
ISSN:
09680896
e-ISSN:
14643391