Details
Stereochemistry | ACHIRAL |
Molecular Formula | C3H2N4S |
Molecular Weight | 126.14 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
N#CNC1=NN=CS1
InChI
InChIKey=YUCHAYRHHXJNQK-UHFFFAOYSA-N
InChI=1S/C3H2N4S/c4-1-5-3-7-6-2-8-3/h2H,(H,5,7)
Molecular Formula | C3H2N4S |
Molecular Weight | 126.14 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Amitivir [LY217896], an amino thiadiazole derivative, is an inhibitor of the enzyme inosine monophosphate dehydrogenase. Amitivir has activity against several influenza A and B viruses. Amitivir possesses broad antiviral activity in vitro and in animal models against or thomyxo-and paramyxoviruses. In phase I studies with healthy volunteers, single doses of up to 500 mg were well tolerated and had predictable pharmacokinetics. Oral LY217896 was in trial for prevention of experimental influenza A virus infection and illness in humans. LY217896 was associated with asymptomatic rises in serum uric acid levels and was ineffective in modifying the virologic or clinical course of experimental influenza A (H1N1) virus infection. Amitivir development was discontinued.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL613740 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2080866 |
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Target ID: CHEMBL613129 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2080866 |
PubMed
Title | Date | PubMed |
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Evaluation of the anti-influenza virus activities of 1,3,4-thiadiazol-2-ylcyanamide (LY217896) and its sodium salt. | 1990 Nov |
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Biotransformation of the antiviral agent 1,3,4-thiadiazol-2-ylcyanamide (LY217896) and characteristics of a mesoionic ribose metabolite. | 1993 Jan-Feb |
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Oral LY217896 for prevention of experimental influenza A virus infection and illness in humans. | 1994 May |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8067760
The efficacy and safety of oral LY217896 for prevention of experimental influenza A/Kawasaki/86 (H1N1) virus infection were assessed in susceptible males randomly assigned to receive LY217896 (75 mg) or placebo once daily for 7 days beginning 24 h prior to viral challenge.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2073106
In nondividing confluent MDCK cells, the 50% inhibitory concentration of LY217896 ranged from 0.37 to 1.19 ug/ml against various strains of influenza A virus and from 0.75 to 1.54 ug/ml against various strains of influenza B virus, with no apparent cytotoxicity.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:34:43 GMT 2023
by
admin
on
Fri Dec 15 16:34:43 GMT 2023
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Record UNII |
R4KR9A9165
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C2087
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NCI_THESAURUS |
C281
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R4KR9A9165
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65912
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CHEMBL2104066
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6963
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CC-89
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100000087422
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C73194
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SUB05460MIG
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111393-84-1
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DTXSID70149637
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
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