Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents.

Synthesis and antiinflammatory activity of heterocyclic indole derivatives.

Owing to the significant biological activities, quinazoline derivatives have drawn more and more attention in the synthesis and bioactivities research. This review summarizes the recent advances in the synthesis and biological activities investigations of quinazoline derivatives. According to the main method the authors adopted in their research design, those synthetic methods were divided into five main classifications, including Aza-reaction, Microwave-assisted reaction, Metal-mediated reaction, Ultrasound-promoted reaction and Phase-transfer catalysis reaction. The biological activities of the synthesized quinazoline derivatives also are discussed.

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Quinazoline derivatives: synthesis and bioactivities

https://community.dur.ac.uk/i.r.baxendale/papers/Tetrahedron2005.61.5323.pdf

The rapid preparation of 2-aminosulfonamide-1,3,4-oxadiazoles using polymer-supported reagents and microwave heating

Synthesis of new substituted azetidinoyl and thiazolidinoyl-1,3,4-thiadiazino (6,5-b) indoles as promising anti-inflammatory agents.

Biologically active indolylmethyl-1,3,4-oxadiazoles, 1,3,4-thiadiazoles, 4H--1,3,4-triazoles and 1,2,4-triazines*

Benzopyran-2-one derivatives : antiinflammatory, analgesic and antiproteolytic agents

Biologically Active Indolylmethyl‐1,3,4‐oxadiazoles, 1,3,4‐ Thiadiazoles, 4H‐1,3,4‐Triazoles, and 1,2,4‐Triazines

6-Substituted-2-alkyl-3-(4-aminobenzene sulphonamido)quinazolin-4-(3H) ones (1a-b) were converted either to 2-methyl 3-[(N-aminoacylbenzoate)benzenes sulphonamido]quinazolin-4 (3H) ones (2a-c) or to 6-substituted-2-alkyl-3-(N-arylidene benzene sulphonamido)-quinazolin-4- (3H) ones (3a-h). 3 on reduction, yielded 6-substituted-2-alkyl-3-(N-arylmethyl sulphonamido)-quinazolin-4(3H)ones (4a-l). Reaction of 3a-h with thioglycolic acid afforded 2-alkyl-3-[4'-(5'-arylthiazolidin-3'-one)benzene sulphonamido]quinazolin-4(3H)ones (5a-h). All these compounds were evaluated for their anti-inflammatory activity against carrageenin induced rat's paw oedema. Active compounds were also evaluated for ulcerogenic liability and ALD50 values.

A. Hitkari

Papers

Biologically active indolylmethyl-1,3,4-oxadiazoles, 1,3,4-thiadiazoles, 4H--1,3,4-triazoles and 1,2,4-triazines*

Benzopyran-2-one derivatives : antiinflammatory, analgesic and antiproteolytic agents

Biologically Active Indolylmethyl‐1,3,4‐oxadiazoles, 1,3,4‐ Thiadiazoles, 4H‐1,3,4‐Triazoles, and 1,2,4‐Triazines

Substituted quinazolinones and their anti-inflammatory activity.

Benzopyran-2-one Derivatives: Antiinflammatory, Analgesic and Antiproteolytic Agents.