Medicinal Chem of Antivirals Flashcards
SoA - Famciclovir/ Penciclovir
HSV1/2 and VZV
Grazoprevir MoA
HCV NS3 Protease-i
Delavirdine MoA
NNRT-I
Oseltamivir MoA
neuraminidase-i
SoA - Acyclovir/ Valacyclovir
HSV1/2 and VZV
Rilpivirine MoA
NNRT-I
SoA/MoA- Ribavirin
- Inhibits IMDDH
- Flu A/B
- Hepatitis A, B, C
- Genital herpes
- herpes zoster
Bictegravir MoA
Integrase-i
Prodrugs
- Acyclovir (viral enzyme and triphosphorolated)
- Valacyclovir (converted into Acyclovir)
- Famciclovir (converted to Pen by 1st pass metabolism in the intestine/liver)
- Valganciclovir (hydrolyzed to Gan in intestine/liver)
- Cidofovir (phosphorylated by cellular kinase)
Tenofovir alafenamide MoA
NRTI
Velpatasvir MoA
HCV NS5A-i
Ledipasvir MoA/Res
HCV NS5A-i
- 1st gen (high resistance)
Sofosbuvir MoA
HCV RNA Polymerase-i (NS5B-i)
Glecaprevir MoA
HCV NS3 Protease-i
Daclatasvir MoA/Res
HCV NS5A-i
- 1st gen (high resistance)
Chain Terminators
- Acyclovir / Valacyclovir
- Ganciclovir / Valganciclovir
- Cidofovir
Acyclovir/Val MoA
- inhibits viral DNA polymerase
- chain terminator
SoA - Foscarnet, Cidofovir, and Letermovir
CMV
Voxilaprevir MoA
HCV NS3 Protease-i
Nirmatrelvir MoA
- inhibits SARS-COV-2
- admin w/ Ritonavir (inhibits CYP3A4… inc Nirm levels)
Foscarnet MoA
Traps polymerase in closed formation
Letermovir MoA
inhibits terminase complex by binding to pUL56 -> prevents cleaving and packaging
Etavirine MoA
NNRT-I
Darunavir MoA
Protease-i
Elbasvir MoA/Res
HCV NS5A-i
- 1st gen (high resistance)
Efavirenz MoA
NNRT-I
Remdesivir MoA
inhibits viral RNA polymerase
Atazanavir MoA
Protease-i
HBV-i
- Lamivudine
- Entacavir
- Tenofovir (nucleotide-i)
Binding Site of Foscarnet on DNA Polymerase
blocks PYROPHOSPHATE binding site of the viral DNA polymerase
Pibrentasvir
HCV NS5A-i
Dasabuvir MoA
HCV RNA Polymerase-i (NS5B-i)
Lamivudine MoA
NRTi
Abacavir MoA
NRTi
HCV NS3 Protease-i Resistance Mech
-Res: Mut in NS3 active site (but keep activity against mut to Gen-1 Protease-i)
Nevirapine MoA
NNRT-I
Atazanavir MoA
Protease-i
SoA - Ganciclovir/ Valganciclovir
CMV
Emtricitabine MoA
NRTi
Dolutegravir MoA
Integrase-i
Fam/Pen/Gan/Valgan MoA
competitive inhibitor of DNA polymerase
Elvitagravir MoA
Integrase-i
- combo w/ cobicistate (inhibits 3A4… inc elvit concentrations)
Cidofovir MoA
chain terminator
PI boosting
low doses of Ritonavir inhibits CYP3A4… inc [PI], dec resistance, inc compliance (lower doses and frequency)