Pharmacological Properties of Indazole Derivatives: Recent Developments

Abstract

The chemistry of furoxans (1, 2, 5-oxadiazole-2-oxides) and benzofuroxans (benzo[1, 2-c]1, 2, 5-oxadiazole-1-oxides) is very well known. These systems are widely used in organic chemistry as intermediate compounds for the synthesis of numerous heterocycles. In the other hand, furoxan and benzofuroxan derivatives were extensively studied as bioactive compounds. They possess remarkable biological activities, such as anti-microbial and anti-parasitic properties, mutagenic, immunosuppressive and anticancer effects, anti-aggregating and vasorelaxant activity, among others. In some cases, molecular mode of action was proposed. Recently, the research and development in the medicinal chemistry of these systems have produced hybrid compounds in which furoxan or benzofuroxan moieties together with a classical drug moieties are present in a single molecule. So, new anti-ulcer drugs, calcium channel modulators and vasodilator derivatives were described and they are currently in study. In this presentation recent developments in the medicinal chemistry of furoxans and benzofuroxans will be reviewed.

An expedient general synthesis of pyrrolo[3,2-e]indazoles: domino Sonogashira/Cacchi coupling-heteroannulation reactions

“…1,2 More than 10,000 bioactive indoles are known, of which over 200 are either used as drugs or are in clinical trials. 3 Substituted indazoles too are of considerable pharmaceutical importance because of their therapeutic potential and use, 4 amongst which benzydamine is a notable anti-inflammatory agent. 5,6 In continuation of our ongoing interest in the development of general synthetic routes to potentially bioactive condensed nitrogen heterocycles, [7][8][9][10][11][12][13][14] we recently focused our attention on a relatively less studied class of heterocycles which incorporate both the indole and the indazole nuclei, viz.…”

Temperature‐Dependent Regioselective Synthesis of 1,2,4‐Triazino[2,3‐b]indazoles and 3H‐1,4‐Benzodiazepines by Domino‐Staudinger/Aza‐Wittig/Isomerization Reaction

“…[2] Many indazole derivatives have exhibited anti-HIV, [3] antiplatelet, [4] anticancer, [5] antimicrobial, [6,7] and antifungal activities. [8,9] Much effort has been invested in the synthesis of derivatives of these compounds to deduce structure-activity relationships and to discover new analogues with improved properties, especially in medicinal chemistry.…”

Synthesis of 3‐(Tosylalkyl)indazoles and their Desulfonylation Reactions – A New Entry to 3‐Substituted Indazoles by an Unprecedented Friedel–Crafts Process

“…[1] Conversely, a large amount of synthetically prepared compounds recognize a key structural feature in the indazole ring that is responsible for their enhanced biological activity. [2] Indazole-containing derivatives are known for their anti-aggregatory and vasorelaxant properties, [3] antimicrobial, [4] anti-inflammatory activities, [5] and anticancer effects. [6] From a synthetic standpoint, the indazole ring may be assembled by exploiting an intramolecular coupling of arenediazo groups with vicinal o-methyl groups or by reaction of hydrazines with functionalized arenecarbonyl derivatives.…”