Discovery of a new class of potent, selective, and orally active prostaglandin D2 receptor antagonists

International Union of Basic and Clinical Pharmacology. LXXXIII: Classification of Prostanoid Receptors, Updating 15 Years of Progress

“…In ONO-AE3-237 (Fig. 3), the acetate unit is located on C4; its binding pK i for the human rc-DP 1 receptor is 7.7 (Torisu et al, 2004). In the Merck series of DP 1 antagonists, the positions of the carboxylic group and the substituents on the benzene ring of the indole template were optimized to yield MK-0524 (laropiprant) (Sturino et al, 2007).…”

A Pd(II)‐Catalyzed Oxidative Cyclization for the Preparation of Aryl‐Fused Six‐Membered Nitrogen Heterocycles with 2‐Acetoxy Functionality

“…[5] They have also shown use as pesticides, [6] antioxidants, [7] and for use in various types of dyes. [8] 1,2,3,4-Tetrahydroquinoxaline derivatives are present in a large number of biologically active compounds, [9] for example as D2 receptor antagonists [10] and as models for tetrahydrofolic acid (coenzyme F) derivatives. [11] Among these derivatives, 2-substituted 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydroquinoxaline derivatives are the most important compounds.…”

“…[11] Among these derivatives, 2-substituted 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydroquinoxaline derivatives are the most important compounds. [4,6,8,10,11] Many syntheses of 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydroquinoxaline derivatives have been reported. [1b,12] Pd(II)-Catalyzed oxidative cyclizations have become a powerful tool for the construction of N-containing heterocycles using relatively mild conditions.…”

Synthesis, antimicrobial and antioxidant activities of 1-(1,4-benzodioxane-2-carbonyl)piperazine derivatives

“…Piperazine sulfonamides are most widely used antibacterial agents [10] in the world, chiefly because of their low cost, low toxicity, and excellent activity against common bacterial disease. 1,4-Benzodioxane-2-carboxylic acid (1) is very important entity in medicinal chemistry since it has chiral building blocks in the design and synthesis of chiral therapeutic agents [11]. Highly efficient resolutions of 1 with p-substituted 1-phenylethylamines [12], crystallographic, theoretical and morphological approach of (S)-1-phenylethylamine p-substitution on the resolution of 1 have been reported [13].…”