Organic Medicinal Chemistry
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Questions and Answers

Which of the following medications is a derivative of 8-hydroxyquinoline and is used in veterinary practice as an anthelmintic in livestock?

  • Mebendazole
  • Albendazole
  • Iodoquinol (correct)
  • Diloxanide

Which medication is used to treat asymptomatic carriers of Entamoeba histolytica?

  • Mebendazole
  • Diloxanide (correct)
  • Albendazole
  • Iodoquinol

Which drug's mechanism of action is based on irreversibly blocking glucose uptake, leading to depletion of glucose and antimitotic/antimicrotubule effects?

  • Ivermectin
  • Mebendazole (correct)
  • Albendazole
  • Iodoquinol

Which of the following is NOT a broad-spectrum anthelmintic?

<p>Diethylcarbamazine (DEC) (D)</p> Signup and view all the answers

Which medication is derived from Streptomyces avermitilis and works by stimulating GABA, leading to blocked interneuron-motor neuron transmission?

<p>Ivermectin (A)</p> Signup and view all the answers

Which medication is the drug of choice for Pneumocystis carinii pneumonia (PCP)?

<p>Cotrimoxazole (B)</p> Signup and view all the answers

Which medication is used for the prophylaxis of African trypanosomiasis and is rapidly distributed to tissues where it is stored?

<p>Pentamidine Isethionate (B)</p> Signup and view all the answers

Which medication's mechanism of action involves interfering with the electron transport chain as antimetabolite for ubiquinone, an analog of ubiquinone, a component of the mitochondrial electron transport chain?

<p>Atovaquone (C)</p> Signup and view all the answers

Which of the following drugs is a protoplasmic poison that inhibits protein synthesis?

<p>Emetine (C)</p> Signup and view all the answers

Which drug is effective against intestinal amebiasis?

<p>Metronidazole (C), 8-hydroxyquinoline (D)</p> Signup and view all the answers

What is the mechanism of action of Piperazine?

<p>Blocking the response of ascaris muscle to acetylcholine (C)</p> Signup and view all the answers

Which of the following drugs should not be used concurrently with Piperazine?

<p>Pyrantel Pamoate (C)</p> Signup and view all the answers

Which drug acts by covalent binding to DNA after reduction of its 5-nitro group?

<p>Metronidazole (C)</p> Signup and view all the answers

Which of the following is a valid treatment for pinworm infection?

<p>Piperazine (A), Pyrantel Pamoate (D)</p> Signup and view all the answers

Which of the following drugs is known to have a disulfiram-like effect when taken with alcohol?

<p>Metronidazole (A)</p> Signup and view all the answers

Which of the following drugs is used to treat paragonimiasis?

<p>Emetine (B)</p> Signup and view all the answers

What is the mechanism of action of Eflornithine?

<p>Irreversible inactivation of Ornithine decarboxylase (B)</p> Signup and view all the answers

Which drug is specifically indicated for the treatment of Schistosoma mansoni?

<p>Oxamniquine (C)</p> Signup and view all the answers

Which drug is the choice for liver flukes such as Fasciola hepatica?

<p>Bithionol (C)</p> Signup and view all the answers

What type of drug is Nifurtimox used to treat?

<p>South American trypanosomiasis (C)</p> Signup and view all the answers

What is the primary mechanism of action for Oxamniquine?

<p>Inhibit DNA, RNA, Protein synthesis (C)</p> Signup and view all the answers

Which agent is the drug of choice for later stages of African trypanosomiasis?

<p>Melarsoprol (C)</p> Signup and view all the answers

Which drug is indicated for the treatment of Chagas disease?

<p>Benznidazole (D)</p> Signup and view all the answers

What is a significant side effect associated with Eflornithine usage?

<p>Myelosuppression (C)</p> Signup and view all the answers

What is the primary mechanism of action of tetracyclines?

<p>Binds to the 30s subunit of ribosomes (B)</p> Signup and view all the answers

Which antibiotic is derived from Bacillus polymyxa?

<p>Polymyxin B (B)</p> Signup and view all the answers

Which of the following is a short-acting tetracycline?

<p>Oxytetracycline (D)</p> Signup and view all the answers

What type of bacteria does Polymyxin B primarily target?

<p>Both gram-positive and gram-negative (C)</p> Signup and view all the answers

Roxithromycin is classified as what type of antibiotic?

<p>Semisynthetic macrolide (C)</p> Signup and view all the answers

What is the mechanism of action of lincosamides?

<p>Binds to the 50s ribosomal subunit (D)</p> Signup and view all the answers

Which of the following is classified as a long-acting tetracycline?

<p>Doxycycline (B)</p> Signup and view all the answers

What common property do all tetracyclines share?

<p>They bind to ribosomes (A)</p> Signup and view all the answers

What impact does food have on the absorption of Azithromycin?

<p>It decreases absorption. (A)</p> Signup and view all the answers

Which of the following is a requirement for the structure-activity relationship (SAR) of the 1st generation quinolone?

<p>The para-amino group must be unsubstituted. (D)</p> Signup and view all the answers

What is the primary mechanism of action for Azithromycin?

<p>Inhibition of DNA Gyrase Topoisomerase. (D)</p> Signup and view all the answers

Which generation of quinolone drugs improved activity against both gram-negative and gram-positive bacteria?

<p>2nd generation. (C)</p> Signup and view all the answers

What type of form does Zithromax represent for Azithromycin?

<p>Dehydrate form. (C)</p> Signup and view all the answers

Which functional groups are essential in the structure-activity relationship for the 2nd generation quinolones?

<p>Sulfonamide functional group and amino group. (B)</p> Signup and view all the answers

Gatifloxacin, Gemifloxacin, and Sparfloxacin belong to which generation of quinolones?

<p>3rd generation. (B)</p> Signup and view all the answers

What is the active form of quinolones classified as?

<p>Ionized. (D)</p> Signup and view all the answers

Which of the following cephalosporins is a 1st generation antibiotic?

<p>Cefazolin (A)</p> Signup and view all the answers

What is the primary difference between 2nd and 3rd generation cephalosporins?

<p>3rd generation cephalosporins generally have increased activity against Gram-negative bacteria. (D)</p> Signup and view all the answers

Which cephalosporin is listed as a 4th generation antibiotic?

<p>Cefepime (D)</p> Signup and view all the answers

Which of the following is an example of a 2nd generation cephalosporin?

<p>Cefaclor (C)</p> Signup and view all the answers

Which two antibiotics are considered 1st generation cephalosporins?

<p>Cefalexin and Cefadroxil (D)</p> Signup and view all the answers

Which antibiotic is classified as a 3rd generation cephalosporin to treat severe infections?

<p>Cefotaxime (A)</p> Signup and view all the answers

What type of activity does Cefuroxime primarily exhibit?

<p>Broad-spectrum including some resistant strains. (B)</p> Signup and view all the answers

Which of the following antibiotics is a 2nd generation cephalosporin that also offers anaerobic coverage?

<p>Cefoxitin (D)</p> Signup and view all the answers

Identify the cephalosporin that is not a 1st generation antibiotic.

<p>Cefuroxime (D)</p> Signup and view all the answers

Which antibiotic listed can be classified as a 'carboxy' related cephalosporin?

<p>Cefoperazone (C)</p> Signup and view all the answers

Flashcards

Emetine

An alkaloid from Ipecac that inhibits protein synthesis.

Dehydroemetine

An alkaloid similar to Emetine, with the same MOA.

Anthelmintics

Drugs that eliminate parasitic worms or helminths.

Piperazine

A drug that induces placid paralysis in roundworm infections.

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Pyrantel Pamoate

A drug that causes spastic paralysis in helminths.

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Thiabendazole

Inhibits fumarate reductase; used as an antibiotic for worms.

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Metronidazole

A drug that binds to DNA, treating various infections.

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Tinidazole

Similar to Metronidazole, an amebicide for intestinal infections.

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Iodoquinol

A broad spectrum anthelminthic and derivative of 8-hydroxyquinoline used in livestock.

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Mebendazole

An anthelmintic that blocks glucose uptake, depleting energy in worms; treats various helminths.

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Albendazole

Antimitotic agent that targets microtubules; used for broad spectrum antiparasitic treatment.

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Ivermectin

Derived from Streptomyces avermitilis; stimulates GABA to block transmission in certain parasites.

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Diethylcarbamazine (DEC)

An unknown mechanism drug used to treat filariasis.

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Praziquantel

Increases Ca2+ membrane permeability in trematodes, leading to paralysis of the worms.

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Cotrimoxazole

Combination of Sulfamethoxazole and Trimethoprim used as the drug of choice for PCP.

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Atovaquone

An analog of ubiquinone that interferes with the electron transport chain in mitochondria.

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Eflornithine

A drug that irreversibly inactivates Ornithine decarboxylase, treating African sleeping sickness.

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Irreversible inhibition

A permanent inactivation of an enzyme, preventing its function.

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Bithionol

Agent of choice for treating liver and lung flukes.

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Suramin

A prophylactic agent used for long-term control of trypanosomiasis.

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Niclosamide

A drug that inhibits oxidative phosphorylation in cestodes.

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Oxamniquine

Inhibits DNA, RNA, and protein synthesis to treat Schistosoma mansoni.

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Melarsoprol

The drug of choice for later stages of African trypanosomiasis.

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Azithromycin

An antibiotic with a 15-membered macrocycle design that includes a N-methyl group, noted for extensive tissue distribution.

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Food Effect on Azithromycin

Food reduces the absorption of Azithromycin, affecting its efficacy.

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Hydrated Forms of Azithromycin

Comes in two forms: Dehydrate (Zithromax) and Monohydrate (Azytha), each with antibacterial properties.

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Mechanism of Action (MOA)

Azithromycin inhibits DNA gyrase topoisomerase, impacting bacterial DNA replication.

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Quinolones

A class of antibiotics; divided into generations, each with unique activity against bacterial types.

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1st Generation Quinolones

Includes Nalidixic acid and Cinoxacin, with moderate Gram-negative activity.

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2nd Generation Quinolones

Improved Gram-negative and positive activity, includes Ciprofloxacin and Ofloxacin.

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Structure Activity Relationship (SAR)

Specific chemical groups are essential for the activity of Quinolones, such as para-amino and sulfonamide groups.

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1st Generation Cephalosporins

Cephalosporins effective against Gram-positive bacteria, includes drugs like Cefalexin and Cefazolin.

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Dicloxacillin

A narrow-spectrum penicillin, effective against staphylococci, part of the 1st generation.

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2nd Generation Cephalosporins

Cephalosporins with broader activity against Gram-negative bacteria, includes Cefaclor and Cefoxitin.

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Cefuroxime

A 2nd generation cephalosporin, good for respiratory tract infections.

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3rd Generation Cephalosporins

Cephalosporins with enhanced activity against Gram-negative bacteria and some resistant strains.

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Ceftriaxone

A broad-spectrum 3rd generation cephalosporin, often used for serious infections.

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4th Generation Cephalosporins

Cephalosporins with even more resistance to beta-lactamases and broader spectrum.

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Cefepime

A 4th generation cephalosporin with broad-spectrum activity against resistant strains.

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B-lactamase Resistance

The ability of certain antibiotics to resist breakdown by enzymes called beta-lactamases, which some bacteria produce.

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Amoxicillin

A widely used penicillin antibiotic with enhanced activity against Gram-positive and Gram-negative bacteria.

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Polymyxin B

An antibiotic with broad spectrum activity against gram-positive, gram-negative, spirochetes, and atypical bacteria.

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Bacitracin

An antibiotic used in combination with Polymyxin B for skin infections.

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Dexamethasone

A corticosteroid used with Neomycin for treating eye infections.

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Mechanism of Action (MOA) of Tetracyclines

Binds to the 30s subunit of ribosomes, preventing aminoacyl-tRNA from binding to the mRNA complex.

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Short Acting Tetracyclines

Includes Tetracycline and Oxytetracycline, characterized by their short duration of action.

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Long Acting Tetracyclines

Includes Doxycycline and Minocycline, known for their longer duration of action.

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Roxithromycin

A semisynthetic macrolide antibiotic derived from erythromycin with an added N-oxime side chain.

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Lincosamides

A class of sulfur-containing antibiotics with a specific mechanism of action.

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Study Notes

Organic Medicinal Chemistry

  • Medicinal chemistry focuses on drug discovery and development.
  • Metabolism is the biotransformation of drugs within the body.
  • Glycine and glutamine conjugation is a common pathway for eliminating drugs from the body. This involves attaching the drug to glycine or glutamine, making it more soluble and non-toxic, for easier elimination.
  • Glutathione is a critical component in detoxification, neutralizing chemically reactive compounds, and assisting in excretion. It's composed of cysteine, glycine, and glutamine.
  • Acetylation is a phase I reaction frequently seen in the metabolism of drugs, notably sulfonamides. This reaction modifies the drug using an acetyl group. Acetylation capacity varies between individuals (slow and fast acetylators), affecting drug dose and response.
  • Glucuronidation is a major phase II reaction, commonly involving glucuronic acid. It's crucial in rendering drugs inactive and more water-soluble for excretion.
  • Sulfation is another key phase II reaction often using 3'phosphoadenosine-5'phosphosulfate (PAPS) as a coenzyme. Important in detoxification and making drugs water-soluble.
  • Methylation through S-adenosylmethionine as a coenzyme is a minor pathway for non-polar and inactive compound formation. Important for processes like epinephrine biosynthesis.
  • First-pass metabolism (pre-systemic metabolism) occurs when orally administered drugs are substantially metabolized before reaching the systemic circulation. It can be impacted by enzyme inhibitors and inducers affecting drug metabolism and effectiveness.

Anti-Infective Agents

  • Antisepsis is using an agent on living tissue to prevent infection.
  • Decontamination involves reducing or destroying microorganisms.
  • Disinfection is treating inanimate surfaces to reduce microorganisms.
  • Sanitization is reducing microbial load to a safe public health level on inanimate surfaces.
  • Sterilization is eliminating all microorganisms.
  • Pasteurization kills non-spore-forming microorganisms using heat.
  • Germicides are locally applied anti-infective agents.
  • Cidal agents kill, static agents prevent growth.

Oxidizing Agents

  • Hydrogen peroxide (H₂O₂) is a transient agent used in wound cleansing.
  • Carbamide peroxide consists of urea and hydrogen peroxide.
  • Hydrous benzoyl peroxide is an effective topical treatment for acne.
  • Iodine (I₂) is used for antiseptic purposes, particularly to inactivate proteins in tissues/cells.
  • Various iodine preparation types exist in medicine (solution, tincture).
  • Chlorine (Cl₂) is used to disinfect water supplies, with hypochlorous acid as a key active species.
  • Other halogen-containing compounds like halazone, chloroazodin, and oxychlorosene sodium perform similar functions.

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Organic Medicinal Chemistry PDF RJAV 2022

Description

This quiz explores key concepts in organic medicinal chemistry, including drug metabolism and the pathways involved in drug elimination. You'll learn about the roles of glycine, glutamine, and glutathione in detoxification processes, as well as the mechanisms of acetylation and glucuronidation in drug transformation. Test your understanding of these crucial biochemical reactions.

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