Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents

Reemergence of chloroquine (CQ) analogs as multi-targeting antimalarial agents: A review

“…Inclusion of such heterocyclic molecules is often known to enhance the biological activities and malaria is not the exception of it. This is further strengthened by the fact that heme complexation occurs through azole functionality and show its antimalarial activity [64]. To further investigate the antimalarial efficacy of CQ-azole conjugates, Rawat et al [63,[71][72][73][74] did a lot of work in this area.…”

“…Among several excellent molecules, activities of some of the compounds were 7-8 times higher than CQ while it was 2 fold more than artemisnin in CQS strain. Pandey et al [64] designed and synthesized some tetrazole embedded CQ-derivatives joined through variable linkers (compound 19a-b, Figure 11). In-vitro antimalarial activity on CQR strain (K1) showed better activity profile of the compounds (73-1023 nM) than standard drug CQ (~ 255 nM).…”

“…Azoles are an important class of nitrogen containing heterocyclic compounds laced with various biological activities [25, [61][62][63][64][65][66][67][68][69][70][71][72][73][74]. Inclusion of such heterocyclic molecules is often known to enhance the biological activities and malaria is not the exception of it.…”

Novel 5‐(1‐aryl‐1H‐pyrazol‐3‐yl)‐1H‐tetrazoles as glycogen phosphorylase inhibitors: An in vivo antihyperglycemic activity study

“…However, 1,5-disubstituted tetrazoles can be used as isosteres of cis-amide bond of peptides (May & Abell, 2001;May & Abell, 2002). Substances containing 1,5-disubstituted tetrazole fragment are being well studied as they exhibit anti-inflammatory (Rajasekaran & Thampi, 2004), antiviral, (Muraglia et al, 2006), antitubercular (Karabanovich et al, 2015), anticonvulsant, antimicrobial (Rostom, Ashour, Abd El Razik, Abd El Fattah, & El-Din, 2009), antiparasitic (Pedro et al, 2014), antiulcer (Uchida et al, 1989, antihypertensive (Ashton et al, 1992), antimalarial (Pandey et al, 2013), anticancer (Arshad et al, 2014), and COX-2 inhibitory (Al-Hourani et al, 2011) properties. 2,5-Disubstituted tetrazoles have been proved to exhibit antiviral (Chang et al, 2005), antimicrobial (Rostom, Ashour, Abd El Razik, Abd El Fattah, & El-Din, 2009), and glutamate receptor modulating (Vieira et al, 2005) properties.…”

A Quest for New Antimalarial Agents with Improved Specificity Guided by Molecular Docking, 3D QSAR and Molecular Dynamics Simulation Studies

“…A total of 70 molecules [5][6][7][8] with known inhibition of pf 3d7 strain were taken for the present study. Linux operating system was used for molecular modeling calculations.…”