761458-01-9Relevant academic research and scientific papers
One-Pot Synthesis of Some Dynamic 2-Substituted Benzoxazinones and Their Corresponding Qinazolinones of Anticipated Biological Activity
El-Hashash, Maher A.,Azab, Mohamed E.,Morsy, Jehan M.
, p. 95 - 101 (2016)
(Chemical Equation Presented) Reactions of 6-bromo-2-isopropyl-4(3H)-3,1-benzoxazin-4-one toward mono- and di-dentate nitrogen nucleophiles, e.g. primary aliphatic and aromatic amines, 1,2-phenylenediamine, hydrazine hydrate, and formamide, have been investigated and afford the corresponding quinazolinones which are expected to have some interesting biological activity. The behavior of 3, 1-benzoxazin-4-one toward active methylene compounds, namely, acetylacetone in basic medium has been studied and gave 3-acetylquinoline. The last reaction is considered as an illustrative model of heterocyclic transformation reactions.
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity
Rudolph, Joachim,Esler, William P.,O'Connor, Stephen,Coish, Philip D. G.,Wickens, Philip L.,Brands, Michael,Bierer, Donald E.,Bloomquist, Brian T.,Bondar, Georgiy,Chen, Libing,Chuang, Chih-Yuan,Claus, Thomas H.,Fathi, Zahra,Fu, Wenlang,Khire, Uday R.,Kristie, James A.,Liu, Xiao-Gao,Lowe, Derek B.,McClure, Andrea C.,Michels, Martin,Ortiz, Astrid A.,Ramsden, Philip D.,Schoenleber, Robert W.,Shelekhin, Tatiana E.,Vakalopoulos, Alexandras,Tang, Weifeng,Wang, Lei,Yi, Lin,Gardell, Stephen J.,Livingston, James N.,Sweet, Laurel J.,Bullock, William H.
, p. 5202 - 5216 (2008/03/12)
The peptide hormone ghrelin is the endogenous ligand for the type 1a growth hormone secretagogue receptor (GHS-R1a) and the only currently known circulating appetite stimulant. GHS-R1a antagonism has therefore been proposed as a potential approach for obe
QUINAZOLINONE DERIVATIVES USEFUL FOR THE REGULATION OF GLUCOSE HOMEOSTASIS AND FOOD INTAKE
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Page/Page column 57-58, (2010/10/19)
This invention relates to substituted quinazolinone derivatives, compositions, and methods for treating diabetes, obesity and related disorders, and regulation of food intake (e.g., stimulation and suppression).
Quinazolineacetic Acids and Related Analogues as Aldose Reductase Inhibitors
Malamas, Michael S.,Millen, Jane
, p. 1492 - 1503 (2007/10/02)
A variety of 2,4-dioxoquinazolineacetic acids (10, 11) were synthesized as hybrids of the known aldose reductase inhibitors alrestatine (8), ICI-105,552 (9), and ICI-128,436 (2) and evaluated for their ability to inhibit partially purified bovine lens aldose reductase (in vitro) and their effectiveness to decrease galactitol accumulation in the 4-day galactosemic rat model (in vivo).In support to SAR studies, related analogues pyrimidinediones (12), dihydroquinazolones (13), and indazolidinones (14, 15) were synthesized and tested in the in vitro and in vivo assays.All prepared compounds (10-15) have shown a high level of in vitro activity (IC50 ca. 10-6 to 4 10-8 M).However, only the 2,4-quinazolinedione analogues 10 and 11, with similar N-aralkyl substitution found in 2 and 9, have exhibited good oral potency.The remaining compounds were either inactive or had only a marginal in vivo activity.The structure-activity data support the presence of a secondary hydrophobic pocket in the vicinity of the primary lipophilic region of the enzyme.
