Matches in SemOpenAlex for { <https://semopenalex.org/work/W3044368265> ?p ?o ?g. }
- W3044368265 endingPage "1117" @default.
- W3044368265 startingPage "1117" @default.
- W3044368265 abstract "Miltefosine (Milt) is the only oral treatment for visceral leishmaniasis (VL) but its use is associated with adverse effects, e.g., teratogenicity, vomiting, diarrhoea. Understanding how its chemical structure induces cytotoxicity, whilst not compromising its anti-parasitic efficacy, could identify more effective compounds. Therefore, we systemically modified the compound's head, tail and linker tested the in vitro activity of three alkylphosphocholines (APC) series against Leishmania donovani strains with different sensitivities to antimony. The analogue, APC12, with an alkyl carbon chain of 12 atoms, was also tested for anti-leishmanial in vivo activity in a murine VL model. All APCs produced had anti-leishmanial activity in the micromolar range (IC50 and IC90, 0.46- > 82.21 µM and 4.14-739.89 µM; 0.01- > 8.02 µM and 0.09-72.18 µM, respectively, against promastigotes and intracellular amastigotes). The analogue, APC12 was the most active, was 4-10 fold more effective than the parent Milt molecule (APC16), irrespective of the strain's sensitivity to antimony. Intravenous administration of 40 mg/kg APC12 to L. donovani infected BALB/c mice reduced liver and spleen parasite burdens by 60 ± 11% and 60 ± 19%, respectively, while oral administration reduced parasite load in the bone marrow by 54 ± 34%. These studies confirm that it is possible to alter the Milt structure and produce more active anti-leishmanial compounds." @default.
- W3044368265 created "2020-07-29" @default.
- W3044368265 creator A5005274850 @default.
- W3044368265 creator A5042745349 @default.
- W3044368265 creator A5055234599 @default.
- W3044368265 date "2020-07-24" @default.
- W3044368265 modified "2023-10-16" @default.
- W3044368265 title "Structure and Antiparasitic Activity Relationship of Alkylphosphocholine Analogues against Leishmania donovani" @default.
- W3044368265 cites W1969351587 @default.
- W3044368265 cites W1974463950 @default.
- W3044368265 cites W1982338402 @default.
- W3044368265 cites W1986897839 @default.
- W3044368265 cites W1988408881 @default.
- W3044368265 cites W1991471125 @default.
- W3044368265 cites W1996094668 @default.
- W3044368265 cites W2020045592 @default.
- W3044368265 cites W2023837509 @default.
- W3044368265 cites W2033210402 @default.
- W3044368265 cites W2034026521 @default.
- W3044368265 cites W2040914101 @default.
- W3044368265 cites W2043599583 @default.
- W3044368265 cites W2049533986 @default.
- W3044368265 cites W2052704812 @default.
- W3044368265 cites W2053725905 @default.
- W3044368265 cites W2055298323 @default.
- W3044368265 cites W2058649893 @default.
- W3044368265 cites W2064925342 @default.
- W3044368265 cites W2067299341 @default.
- W3044368265 cites W2071952696 @default.
- W3044368265 cites W2072418500 @default.
- W3044368265 cites W2073167514 @default.
- W3044368265 cites W2076644749 @default.
- W3044368265 cites W2079711673 @default.
- W3044368265 cites W2084752824 @default.
- W3044368265 cites W2096439392 @default.
- W3044368265 cites W2105523385 @default.
- W3044368265 cites W2112873305 @default.
- W3044368265 cites W2114457715 @default.
- W3044368265 cites W2122089120 @default.
- W3044368265 cites W2126420606 @default.
- W3044368265 cites W2126512081 @default.
- W3044368265 cites W2131358046 @default.
- W3044368265 cites W2134294475 @default.
- W3044368265 cites W2145946158 @default.
- W3044368265 cites W2147095804 @default.
- W3044368265 cites W2147629140 @default.
- W3044368265 cites W2152820036 @default.
- W3044368265 cites W2153445727 @default.
- W3044368265 cites W2157907127 @default.
- W3044368265 cites W2158168571 @default.
- W3044368265 cites W2168618596 @default.
- W3044368265 cites W2285825634 @default.
- W3044368265 cites W2344726805 @default.
- W3044368265 cites W2620097584 @default.
- W3044368265 cites W2794308705 @default.
- W3044368265 cites W2811473578 @default.
- W3044368265 cites W2894429932 @default.
- W3044368265 cites W2895461171 @default.
- W3044368265 cites W2896442353 @default.
- W3044368265 cites W2916020856 @default.
- W3044368265 cites W2945366182 @default.
- W3044368265 cites W2975935103 @default.
- W3044368265 cites W2980224393 @default.
- W3044368265 cites W3016017041 @default.
- W3044368265 cites W4231256920 @default.
- W3044368265 doi "https://doi.org/10.3390/microorganisms8081117" @default.
- W3044368265 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7463460" @default.
- W3044368265 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32722326" @default.
- W3044368265 hasPublicationYear "2020" @default.
- W3044368265 type Work @default.
- W3044368265 sameAs 3044368265 @default.
- W3044368265 citedByCount "5" @default.
- W3044368265 countsByYear W30443682652021 @default.
- W3044368265 countsByYear W30443682652022 @default.
- W3044368265 crossrefType "journal-article" @default.
- W3044368265 hasAuthorship W3044368265A5005274850 @default.
- W3044368265 hasAuthorship W3044368265A5042745349 @default.
- W3044368265 hasAuthorship W3044368265A5055234599 @default.
- W3044368265 hasBestOaLocation W30443682651 @default.
- W3044368265 hasConcept C109316439 @default.
- W3044368265 hasConcept C136764020 @default.
- W3044368265 hasConcept C150903083 @default.
- W3044368265 hasConcept C185592680 @default.
- W3044368265 hasConcept C202751555 @default.
- W3044368265 hasConcept C203014093 @default.
- W3044368265 hasConcept C207001950 @default.
- W3044368265 hasConcept C2776114741 @default.
- W3044368265 hasConcept C2776555147 @default.
- W3044368265 hasConcept C2777787772 @default.
- W3044368265 hasConcept C2778689377 @default.
- W3044368265 hasConcept C2781092759 @default.
- W3044368265 hasConcept C2781333301 @default.
- W3044368265 hasConcept C2781417161 @default.
- W3044368265 hasConcept C41008148 @default.
- W3044368265 hasConcept C501593827 @default.
- W3044368265 hasConcept C55493867 @default.
- W3044368265 hasConcept C71928629 @default.
- W3044368265 hasConcept C86803240 @default.