Medicinal Chem of Antivirals Flashcards

1
Q

SoA - Famciclovir/ Penciclovir

A

HSV1/2 and VZV

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2
Q

Grazoprevir MoA

A

HCV NS3 Protease-i

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3
Q

Delavirdine MoA

A

NNRT-I

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4
Q

Oseltamivir MoA

A

neuraminidase-i

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5
Q

SoA - Acyclovir/ Valacyclovir

A

HSV1/2 and VZV

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6
Q

Rilpivirine MoA

A

NNRT-I

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7
Q

SoA/MoA- Ribavirin

A
  • Inhibits IMDDH
  • Flu A/B
  • Hepatitis A, B, C
  • Genital herpes
  • herpes zoster
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8
Q

Bictegravir MoA

A

Integrase-i

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9
Q

Prodrugs

A
  • 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)
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10
Q

Tenofovir alafenamide MoA

A

NRTI

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11
Q

Velpatasvir MoA

A

HCV NS5A-i

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12
Q

Ledipasvir MoA/Res

A

HCV NS5A-i
- 1st gen (high resistance)

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13
Q

Sofosbuvir MoA

A

HCV RNA Polymerase-i (NS5B-i)

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14
Q

Glecaprevir MoA

A

HCV NS3 Protease-i

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15
Q

Daclatasvir MoA/Res

A

HCV NS5A-i
- 1st gen (high resistance)

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16
Q

Chain Terminators

A
  • Acyclovir / Valacyclovir
  • Ganciclovir / Valganciclovir
  • Cidofovir
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17
Q

Acyclovir/Val MoA

A
  • inhibits viral DNA polymerase
  • chain terminator
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18
Q

SoA - Foscarnet, Cidofovir, and Letermovir

19
Q

Voxilaprevir MoA

A

HCV NS3 Protease-i

20
Q

Nirmatrelvir MoA

A
  • inhibits SARS-COV-2
  • admin w/ Ritonavir (inhibits CYP3A4… inc Nirm levels)
21
Q

Foscarnet MoA

A

Traps polymerase in closed formation

22
Q

Letermovir MoA

A

inhibits terminase complex by binding to pUL56 -> prevents cleaving and packaging

23
Q

Etavirine MoA

24
Q

Darunavir MoA

A

Protease-i

25
Q

Elbasvir MoA/Res

A

HCV NS5A-i
- 1st gen (high resistance)

26
Q

Efavirenz MoA

27
Q

Remdesivir MoA

A

inhibits viral RNA polymerase

28
Q

Atazanavir MoA

A

Protease-i

29
Q

HBV-i

A
  • Lamivudine
  • Entacavir
  • Tenofovir (nucleotide-i)
30
Q

Binding Site of Foscarnet on DNA Polymerase

A

blocks PYROPHOSPHATE binding site of the viral DNA polymerase

31
Q

Pibrentasvir

A

HCV NS5A-i

32
Q

Dasabuvir MoA

A

HCV RNA Polymerase-i (NS5B-i)

33
Q

Lamivudine MoA

34
Q

Abacavir MoA

35
Q

HCV NS3 Protease-i Resistance Mech

A

-Res: Mut in NS3 active site (but keep activity against mut to Gen-1 Protease-i)

36
Q

Nevirapine MoA

37
Q

Atazanavir MoA

A

Protease-i

38
Q

SoA - Ganciclovir/ Valganciclovir

39
Q

Emtricitabine MoA

40
Q

Dolutegravir MoA

A

Integrase-i

41
Q

Fam/Pen/Gan/Valgan MoA

A

competitive inhibitor of DNA polymerase

42
Q

Elvitagravir MoA

A

Integrase-i
- combo w/ cobicistate (inhibits 3A4… inc elvit concentrations)

43
Q

Cidofovir MoA

A

chain terminator

44
Q

PI boosting

A

low doses of Ritonavir inhibits CYP3A4… inc [PI], dec resistance, inc compliance (lower doses and frequency)