Novel Selective PDE4 Inhibitors. 3. In Vivo Antiinflammatory Activity of a New Series of N-Substituted cis-Tetra- and cis-Hexahydrophthalazinones was written by Van der Mey, Margaretha;Boss, Hildegard;Hatzelmann, Armin;Van der Laan, Ivonne J.;Sterk, Geert J.;Timmerman, Hendrik. And the article was included in Journal of Medicinal Chemistry in 2002.Formula: C8H7BrO2 This article mentions the following:
The synthesis and biol. activities of a series of N-substituted cis-4a,5,6,7,8,8a-hexa- and cis-4a,5,8,8a-tetrahydro-2H-phthalazin-1-ones I [XY = (CH2)2, HC:CH; R = Me, cyclopentyl, allyl, PhCOCH2, etc.] are described. It was found that compounds bearing a cycloalkyl group at the 2-position exhibit the highest PDE4 inhibitory activities (pIC50 = 8.6-9.4). The N-cycloheptyl- and N-adamantanyltetrahydrophthalazinones I (XY = HC:CH; R = cycloheptyl, 2-adamantyl) and II [R1 = R2 = Me, R1R2 = (CH2)4] show high in vivo antiinflammatory activities after oral application. Addnl., some phthalazinones were found to exhibit potent suppression of LPS-induced TNFæ¿ž?release and show moderate potency against fMLP-stimulated production of ROS. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Formula: C8H7BrO2).
3-(Bromomethyl)benzoic acid (cas: 6515-58-8) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.Formula: C8H7BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary