Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H18FN3O4 |
| Molecular Weight | 371.3623 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)C(C(=O)NCCO)=C(O)C2=NC=C(CC3=CC=C(F)C=C3)C=C12
InChI
InChIKey=QWLNINWUBHHOLU-UHFFFAOYSA-N
InChI=1S/C19H18FN3O4/c1-23-14-9-12(8-11-2-4-13(20)5-3-11)10-22-16(14)17(25)15(19(23)27)18(26)21-6-7-24/h2-5,9-10,24-25H,6-8H2,1H3,(H,21,26)
GlaxoSmithKline was developing GSK-364735 as a human immunodeficiency virus (HIV) integrase inhibitor. The inhibition of viral DNA integration takes place by interacting at the two-metal binding site within the catalytic center of HIV integrase. GSK-364735 was successfully studied at Phase II in HIV-infected patients; however, adverse liver effects of GSK364735 were recently observed in a long-term preclinical safety study in the monkey and preclude further development of the compound.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects. | 2007 Dec |
|
| Mirabamides A-D, depsipeptides from the sponge Siliquariaspongia mirabilis that inhibit HIV-1 fusion. | 2007 Nov |
|
| The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral. | 2008 Mar |
|
| Potent inhibitors of HIV-1 integrase display a two-step, slow-binding inhibition mechanism which is absent in a drug-resistant T66I/M154I mutant. | 2009 Feb 24 |
Patents
Sample Use Guides
In part A, three alternating cohorts of 10 subjects (8 receiving the active drug and 2 receiving a placebo) received single doses of 50 to 400 mg while fasting or 200 mg and 400 mg coadministered with food. In part B, five cohorts received repeated doses of 100 to 600 mg daily coadministered with food for 8 days.
Route of Administration:
Oral
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54718859
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DB13119
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SXN0KXT60S
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863434-13-3
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admin on Sat Dec 16 10:41:48 GMT 2023 , Edited by admin on Sat Dec 16 10:41:48 GMT 2023
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)
