Matches in SemOpenAlex for { <https://semopenalex.org/work/W2313532955> ?p ?o ?g. }
- W2313532955 endingPage "3431" @default.
- W2313532955 startingPage "3411" @default.
- W2313532955 abstract "Chloroquine (CQ) has been used as first line malaria therapeutic drug for decades. Emergence of CQ drug-resistant Plasmodium falciparum malaria throughout endemic areas of the world has limited its clinical value. Mefloquine (MQ) has been used as an effective malaria prophylactic drug due to its being long-acting and having a high potency against blood stage P. falciparum (Pf). However, serious CNS toxicity of MQ has compromised its clinical value as a prophylaxis drug. Therefore, new and inexpensive antimalarial drugs with no cross-resistance to CQ or CNS toxicity are urgently needed to combat this deadly human disease. In this study, a series of new 4-amidinoquinoline (4-AMQ) and 10-amidinobenzonaphthyridine (10-AMB) derivatives were designed, prepared, and assessed to search for new therapeutic agents to replace CQ and MQ. The new derivatives displayed high activity in vitro and in vivo, with no cross-resistance to CQ, and none were toxic in mice up to 160 mpk × 3. The best compound shows IC50 < 1 ng/mL against D6, W2 and C235 Pf clones, low inhibitory activity in hERG K+ channel blockage testing, negativity in the Ames test, and 5/5 cure @ <15 mpk × 3 in mice infected with Plasmodium berghei. In addition to these desirable pharmacological profiles, compound 13b, one of the most active compounds, is metabolically stable in both human and mouse liver microsomal preparations and has a plasma t1/2 of 50 h in mice, which made it a good MQ replacement candidate." @default.
- W2313532955 created "2016-06-24" @default.
- W2313532955 creator A5002936928 @default.
- W2313532955 creator A5006605648 @default.
- W2313532955 creator A5006752154 @default.
- W2313532955 creator A5012061122 @default.
- W2313532955 creator A5020873877 @default.
- W2313532955 creator A5032966568 @default.
- W2313532955 creator A5055732602 @default.
- W2313532955 creator A5070659566 @default.
- W2313532955 date "2015-04-09" @default.
- W2313532955 modified "2023-10-17" @default.
- W2313532955 title "Antimalarial Activity of 4-Amidinoquinoline and 10-Amidinobenzonaphthyridine Derivatives" @default.
- W2313532955 cites W1493715460 @default.
- W2313532955 cites W1581382551 @default.
- W2313532955 cites W1588684706 @default.
- W2313532955 cites W1974720373 @default.
- W2313532955 cites W1982454265 @default.
- W2313532955 cites W1988605236 @default.
- W2313532955 cites W1988662106 @default.
- W2313532955 cites W1996808398 @default.
- W2313532955 cites W1997368078 @default.
- W2313532955 cites W2004390083 @default.
- W2313532955 cites W2006250595 @default.
- W2313532955 cites W2010387696 @default.
- W2313532955 cites W2011099146 @default.
- W2313532955 cites W2016203598 @default.
- W2313532955 cites W2017194393 @default.
- W2313532955 cites W2025765364 @default.
- W2313532955 cites W2029939998 @default.
- W2313532955 cites W2031636523 @default.
- W2313532955 cites W2036613603 @default.
- W2313532955 cites W2043969235 @default.
- W2313532955 cites W2045795106 @default.
- W2313532955 cites W2051527307 @default.
- W2313532955 cites W2065314419 @default.
- W2313532955 cites W2073445003 @default.
- W2313532955 cites W2075055204 @default.
- W2313532955 cites W2079395738 @default.
- W2313532955 cites W2081517567 @default.
- W2313532955 cites W2082171250 @default.
- W2313532955 cites W2090924548 @default.
- W2313532955 cites W2092370541 @default.
- W2313532955 cites W2093253421 @default.
- W2313532955 cites W2094367634 @default.
- W2313532955 cites W2095458479 @default.
- W2313532955 cites W2101587942 @default.
- W2313532955 cites W2105668259 @default.
- W2313532955 cites W2114168178 @default.
- W2313532955 cites W2116172270 @default.
- W2313532955 cites W2116581628 @default.
- W2313532955 cites W2132923209 @default.
- W2313532955 cites W2138573735 @default.
- W2313532955 cites W2139242164 @default.
- W2313532955 cites W2143228423 @default.
- W2313532955 cites W2146805807 @default.
- W2313532955 cites W2149917315 @default.
- W2313532955 cites W2150534844 @default.
- W2313532955 cites W2158905026 @default.
- W2313532955 cites W2161836547 @default.
- W2313532955 cites W2171476493 @default.
- W2313532955 cites W2320474630 @default.
- W2313532955 cites W2327336360 @default.
- W2313532955 cites W2329567717 @default.
- W2313532955 cites W2412903130 @default.
- W2313532955 cites W2899632572 @default.
- W2313532955 cites W2949186145 @default.
- W2313532955 cites W2949369058 @default.
- W2313532955 cites W2952268681 @default.
- W2313532955 cites W4293049708 @default.
- W2313532955 doi "https://doi.org/10.1021/jm501809x" @default.
- W2313532955 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25654185" @default.
- W2313532955 hasPublicationYear "2015" @default.
- W2313532955 type Work @default.
- W2313532955 sameAs 2313532955 @default.
- W2313532955 citedByCount "18" @default.
- W2313532955 countsByYear W23135329552015 @default.
- W2313532955 countsByYear W23135329552016 @default.
- W2313532955 countsByYear W23135329552017 @default.
- W2313532955 countsByYear W23135329552018 @default.
- W2313532955 countsByYear W23135329552019 @default.
- W2313532955 countsByYear W23135329552020 @default.
- W2313532955 countsByYear W23135329552021 @default.
- W2313532955 countsByYear W23135329552023 @default.
- W2313532955 crossrefType "journal-article" @default.
- W2313532955 hasAuthorship W2313532955A5002936928 @default.
- W2313532955 hasAuthorship W2313532955A5006605648 @default.
- W2313532955 hasAuthorship W2313532955A5006752154 @default.
- W2313532955 hasAuthorship W2313532955A5012061122 @default.
- W2313532955 hasAuthorship W2313532955A5020873877 @default.
- W2313532955 hasAuthorship W2313532955A5032966568 @default.
- W2313532955 hasAuthorship W2313532955A5055732602 @default.
- W2313532955 hasAuthorship W2313532955A5070659566 @default.
- W2313532955 hasConcept C114851261 @default.
- W2313532955 hasConcept C150903083 @default.
- W2313532955 hasConcept C178790620 @default.
- W2313532955 hasConcept C185592680 @default.
- W2313532955 hasConcept C19831878 @default.