Med Chem Tutoring January 25 By Alaina Darby

Know the objectives… I’m sure you have realized this by now. Some TB drugs are prodrugs that required activation by bacterial enzymes. List up. What is a general stain method for Mtb? Is Mtb Gram-negative or Gram-positive? Mtb survive in host for many years by entering dormancy. Study about non-replicating Mtb. List up the second-line TB drugs. Which one is aminoglycoside? Molecular target of bedaquline Molecular target of ethambutol Structure of delemanide and its mode of action Molecular target of rifampicin \ Study Crohn’s disease. Are antibiotic effective? What are NOD1 and NOD2? Structure of chloroquine Structure of artesunate. Is it orally bioavailable? Combination chemotherapy for Plasmodium falciparum infections. Mode of action and utility of metronidazole Study about interferons What are causative organisms of sexually transmitted infections (STIs)? Study about HIV/AIDS Nucleoside-based antiviral drugs Antiretroviral drugs used for the treatment of HIV/AIDS . General structures of nucleoside reverse-transcriptase inhibitors and SAR Non-nucleoside reverse transcriptase inhibitor for the treatment of HIV Tamiflu and its mode of action

Study about interferons Which of the following types of interferon has been approved from prophylactic treatment of CMV? Interferon-α Interferon-β Interferon-γ Interferon-δ A

What are causative organisms of sexually transmitted infections (STIs)? Which of the following viral infections can cause an STI? Hepatitis A Hepatitis B Hepatitis C Hepatitis D B

What are causative organisms of sexually transmitted infections (STIs)? Which of the following bacteria causes syphilis? Haemophilus ducreyi Neisseria gonorrhea Lymphogranuloma vereum Treponema pallidum D

What are causative organisms of sexually transmitted infections (STIs)? Which of the following is a protozoal infection that also causes a STI? Chlamydia trachomatis Trichomonas vaginalis Candida albicans Human immunodeficiency virus B

Study about HIV/AIDS Which of the following is not true of HAART? May have severe side effects Compliance is important to prevent resistance May be of benefit to patients with low viral loads There are no risks for patients with low viral loads D

Study about HIV/AIDS Which of the following is true of HIV/AIDS? HIV-1 is more infective than HIV-2 HIV-2 is more infective than HIV-1 HIV-1 and HIV-2 are equally infective Neither HIV-1 and HIV-2 are very infective A

Nucleoside-based antiviral drugs Which of the following is not true of NRTI resistance? Mutations in the N-terminal polymerase domain reduce enzyme affinity to bind the drug Mutations may occur as insertions or deletions in the background Excision enhancement mutations are selected for by thymidine analogs Resistance to one NRTI does not confer resistance to the other NRTIs D Slide 85

Antiretroviral drugs used for the treatment of HIV/AIDS . Which of the following is not included in Atripla? Efavirenz Emtricitabine Zidovudine Tenofovir C

Antiretroviral drugs used for the treatment of HIV/AIDS . Which of the following is not a component of Trizivir? Abacavir Emtricitabine Zidovudine Lamivudine B

General structures of nucleoside reverse-transcriptase inhibitors and SAR Which of the following is not a nucleoside reverse-transcriptase inhibitor? A. B. C. D. B… Nevirapine (non-nucleoside)

General structures of nucleoside reverse-transcriptase inhibitors and SAR Which of the following describes the blue highlighted portion of the NRTIs? May not be modified Improves PK Increases hydrophobicity May be slightly modified D

General structures of nucleoside reverse-transcriptase inhibitors and SAR Which of the following describes the arrow portion of the NRTIs? May not be modified Improves PK Increases hydrophobicity May be slightly modified A

General structures of nucleoside reverse-transcriptase inhibitors and SAR Which of the following describes the arrow portion of the NRTIs? Acetylation site Phosphorylation site Hydroxylation site Amination site B

General structures of nucleoside reverse-transcriptase inhibitors and SAR Which of the following sites increases hydrophobicity of the NRTI? Arrow Green Blue Orange B

Non-nucleoside reverse transcriptase inhibitor for the treatment of HIV Which of the following is not true of NNRTIs (vs NRTIs)? Lack nucleoside structure Highly selective for HIV-1 strains Require cellular activation Interact with a non substrate binding site C

Non-nucleoside reverse transcriptase inhibitor for the treatment of HIV Which of the following is true of resistance of NNRTIs? There is cross resistance between NNRTIs and NRTIs NNRTIs require multiple mutations for HIV to gain resistance NNRTIs resistance is acquired faster than to NRTIs More mutations are required to gain resistance to NNRTIs than for NRTIs C

Tamiflu and its mode of action Which of the following does not describe Tamiflu? It is the neuraminidase inhibitor It mimics the oxonium intermediate It impedes an enzyme found inside viruses It is active against the influenza virus C

Tamiflu and its mode of action Which of the following depicts Tamiflu? A. B. C. D. B and C A is the step that it blocks!