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Related Concept Videos

Preparation of Amines: Reduction of Oximes and Nitro Compounds01:29

Preparation of Amines: Reduction of Oximes and Nitro Compounds

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Oximes can be reduced to primary amines using catalytic hydrogenation, hydride reduction, or sodium metal reduction. The reduction of aliphatic and aromatic nitro compounds to primary amines takes place by either catalytic hydrogenation or by using active metals like Fe, Zn, and Sn in the presence of an acid.
Though catalytic hydrogenation can reduce nitrobenzenes, the reduction is nonselective in the presence of other functional groups. For instance, if nitrobenzene contains an aldehyde group,...
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Pharmacokinetics: Drug–Drug Interactions01:25

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Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
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Bioequivalence of Drugs: Drugs with Multiple Indications01:09

Bioequivalence of Drugs: Drugs with Multiple Indications

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The concept of therapeutic equivalence (TE) in drugs with multiple indications is complex. A generic drug may be therapeutically equivalent to a brand-name product for one specific indication, but this doesn't necessarily mean it's equivalent for all other indications. Evidence of TE in one patient group and bioequivalence shown in healthy volunteers can support—but not confirm—TE for other indications. However, definitive proof requires individual clinical studies for each...
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FDA Approved Drugs: Changes to Approved Drugs01:26

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Post-approval, manufacturers may modify an approved new or generic drug product. Such modifications can encompass alterations in the Active Pharmaceutical Ingredient (API), manufacturing process, formulation, batch size, manufacturing site, and container closure system (FDA Guidance for Industry, April 2004). Often, a drug product may undergo multiple changes.These modifications require careful evaluation to determine their potential impact on the drug product's identity, strength, quality,...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Factors Affecting Protein-Drug Binding: Drug-Related Factors01:18

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Drug binding to proteins is a complex phenomenon influenced by various drug-related factors, each playing a significant role in the interaction between drugs and proteins within the body.
One crucial factor in drug-protein binding is the drug's lipophilicity or its affinity for fat. More lipophilic drugs tend to have higher binding extents. For example, highly lipophilic drugs like cloxacillin exhibit substantial protein binding, with as much as 95% of the drug binding to proteins. In...
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A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
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Nitro-Group-Containing Drugs.

Kunal Nepali1, Hsueh-Yun Lee1, Jing-Ping Liou1

  • 1School of Pharmacy, College of Pharmacy , Taipei Medical University , 250 Wuxing Street , Taipei 11031 , Taiwan .

Journal of Medicinal Chemistry
|October 9, 2018
PubMed
Summary
This summary is machine-generated.

Nitro groups in medicinal chemistry offer unique therapeutic potential but raise toxicity concerns. This review explores their mechanisms, toxicity, and applications in anticancer, antitubercular, and antiparasitic drug development.

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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Toxicology

Background:

  • The nitro group is a versatile functional group in medicinal chemistry with a complex history in therapeutics.
  • Nitro-containing drugs are often associated with mutagenicity and genotoxicity, acting as structural alerts.
  • Evidence regarding the safety and efficacy of nitro-containing drugs is often contradictory.

Purpose of the Study:

  • To provide a comprehensive overview of nitro-containing agents.
  • To discuss the bioreductive activation mechanisms and toxicities associated with nitro groups.
  • To highlight strategies for mitigating nitro group toxicity and review recent advances in therapeutic applications.

Main Methods:

  • Review of literature on nitro-containing compounds.
  • Analysis of bioreductive activation pathways.
  • Examination of structure-mutagenicity and structure-genotoxicity relationships.
  • Survey of patents related to hypoxia-activated prodrugs.

Main Results:

  • Nitro groups undergo bioreductive activation, which can lead to toxic effects.
  • Significant research efforts focus on understanding and mitigating the genotoxicity of nitro compounds.
  • Recent advances show promise for nitro-containing agents in anticancer, antitubercular, and antiparasitic applications.

Conclusions:

  • Despite toxicity concerns, nitro groups remain valuable in drug design, particularly for targeted therapies.
  • Understanding activation mechanisms and toxicity is crucial for developing safer nitro-containing drugs.
  • Hypoxia-activated prodrugs represent a promising area for nitro-containing therapeutics.