Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H42N2O2S2 |
Molecular Weight | 454.732 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 2 |
SHOW SMILES / InChI
SMILES
CC1=C(CCO)SC=[N+]1CCCCCCCCCCCC[N+]2=CSC(CCO)=C2C
InChI
InChIKey=UZPXHZIQHWKNPF-UHFFFAOYSA-N
InChI=1S/C24H42N2O2S2/c1-21-23(13-17-27)29-19-25(21)15-11-9-7-5-3-4-6-8-10-12-16-26-20-30-24(14-18-28)22(26)2/h19-20,27-28H,3-18H2,1-2H3/q+2
Molecular Formula | C24H40N2O2S2 |
Molecular Weight | 452.717 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Albitiazolium (SAR97276) is a clinical antimalarial candidate from a series of choline analogs designed to inhibit plasmodial phospholipid metabolism. Albitiazolium exerts powerful in vitro and in vivo antimalarial activities. Albitiazolium has been shown to have appropriate pharmacokinetic and safety parameters in humans and it was being tested in phase II clinical trials by Sanofi, with confirmed antimalarial activity in adult patients. However, Sanofi discontinued development of Albitiazolium.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28472957
A total of 113 malaria patients received SAR97276. Adults were randomized to receive a single dose SAR97296 given either intramuscularly (IM) (0.18 mg/kg) or intravenously (IV) (0.14 mg/kg). If a single dose was not efficacious a second adult group was planned to test a three dose regimen administered IM once daily for 3 days. Single dose SAR97276 showed insufficient efficacy in adults (IM: 20 of 34 cured, 59%; and IV: 23/30 cured, 77%). The 3-day IM regimen showed acceptable efficacy in adults (27/30, 90%) but not in children (13/19, 68%).
Route of Administration:
Parenteral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25470252
Albitiazolium strongly inhibited in vitro plasmodial growth with an IC50 value of 4.2 nM.
Substance Class |
Chemical
Created
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admin
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Edited
Mon Mar 31 18:43:07 GMT 2025
by
admin
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Mon Mar 31 18:43:07 GMT 2025
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Record UNII |
HKM715W3UT
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Validated (UNII)
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TARGET ORGANISM->INHIBITOR |
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
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