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Related Concept Videos

Antihypertensive Drugs: Thiazide-Class Diuretics01:15

Antihypertensive Drugs: Thiazide-Class Diuretics

Thiazide diuretics are sulfonamide derivatives featuring a benzothiadiazine ring system in their molecular structure. Based on this structure, thiazide diuretics can be categorized into two groups: thiazide-type and thiazide-like diuretics. Thiazide-type diuretics, including hydrochlorothiazide and chlorothiazide, consist of a benzothiadiazine backbone with an attached sulfonamide group. Thiazide-like diuretics, such as chlorthalidone and indapamide, lack the thiazide ring but demonstrate...
Aryldiazonium Salts to Azo Dyes: Diazo Coupling01:11

Aryldiazonium Salts to Azo Dyes: Diazo Coupling

The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the para position.
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood glucose levels...
Sedatives and Hypnotics Drugs: Benzodiazepines01:19

Sedatives and Hypnotics Drugs: Benzodiazepines

Benzodiazepines have both sedative and hypnotic properties. They include compounds such as diazepam (Valium) and alprazolam (Xanax). Structurally, their cores are similar, consisting of the fusion of a benzene ring and a diazepine ring, but they share a common mechanism of action in the central nervous system (CNS).
Benzodiazepines work by enhancing the effects of the inhibitory neurotransmitter GABA. They bind to the GABAA receptor, increasing its affinity for GABA, which opens chloride...
Transdermal Drug Delivery Systems01:18

Transdermal Drug Delivery Systems

Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions01:20

Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions

Arenediazonium substitution reactions occur when the diazonium group is substituted by various functional groups such as halides, hydroxyl, nitrile, etc. For instance, arenediazonium salts react with copper(I) salts of chloride, bromide, or cyanide to form corresponding aryl chlorides, bromides, and nitriles. These reactions are named Sandmeyer reactions. Although the mechanism of this reaction is complicated, as illustrated in Figure 1, they are believed to progress via an aryl copper...

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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
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Thiazolidine-2,4-diones: progress towards multifarious applications.

Viral S Jain1, Dhagash K Vora, C S Ramaa

  • 1Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Sector-8, CBD Belapur, Navi Mumbai 400614, Maharashtra, India.

Bioorganic & Medicinal Chemistry
|February 20, 2013
PubMed
Summary

Thiazolidine-2,4-dione compounds show diverse therapeutic potential, including anti-diabetic and anti-cancer effects. This review details their pharmacological activities and structural modifications to guide new drug development.

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Preparation of N-(2-alkoxyvinyl)sulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
10:42

Preparation of N-(2-alkoxyvinyl)sulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines

Published on: January 3, 2018

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Thiazolidine-2,4-dione derivatives exhibit significant biological activities, including anti-hyperglycemic, anti-cancer, and anti-inflammatory properties.
  • The nucleus serves as a crucial scaffold for developing novel therapeutic agents, with diverse substituents modulating its activity spectrum.

Purpose of the Study:

  • To consolidate recent advancements in thiazolidine-2,4-dione research.
  • To provide a comprehensive overview of pharmacological activities linked to substitution patterns and docking studies.
  • To aid medicinal chemists in structure-activity relationship (SAR) development for novel drug candidates.

Main Methods:

  • Literature review of thiazolidine-2,4-dione derivatives and their pharmacological profiles.
  • Analysis of structure-activity relationships based on substitution patterns.
  • Inclusion of molecular docking studies against relevant biological targets.

Main Results:

  • Compilation of diverse pharmacological activities associated with various thiazolidine-2,4-dione derivatives.
  • Correlation of specific structural modifications with enhanced biological effects.
  • Identification of key interactions through docking studies to inform drug design.

Conclusions:

  • Thiazolidine-2,4-diones are versatile scaffolds with broad therapeutic applications.
  • Understanding SAR and target interactions is crucial for designing potent and selective drug candidates.
  • This review facilitates the rational design of new thiazolidine-2,4-dione-based therapeutics.