- ACETYLATED PRODRUGS FOR DELIVERY ACROSS THE BLOOD-BRAIN BARRIER
-
The present disclosure relates to pharmaceutical compositions including a compound derived from a parent compound having a hydroxyl or amino moiety, wherein the hydroxyl in the parent compound is presented as an ester in the compound or the amino in the parent compound is presented as an amide in the compound, and their use to prevent or treat neurological disease.
- -
-
Page/Page column 36
(2019/11/12)
-
- Synthesis of scyllo-inositol derivatives and their effects on amyloid beta peptide aggregation
-
scyllo-Inositol has shown promise as a potential therapeutic for Alzheimer's disease, by directly interacting with the amyloid β (Aβ) peptide to inhibit Aβ42 fiber formation. To explore the molecular details of the inositol-Aβ42 interaction, a series of scyllo-inositol derivatives have been synthesized which contain deoxy, fluoro, chloro, and methoxy substitutions. The effects of these compounds on the aggregation cascade of Aβ42 have been investigated using electron microscopy (EM). EM analyses revealed that the 1-deoxy-1-fluoro- and 1,4-dimethyl-scyllo-inositols significantly inhibit the formation of Aβ42 fibers. The other derivatives showed some alterations in the morphology of the Aβ42 fibers produced. These findings indicate the importance of all of the hydroxyl groups of scyllo-inositol for complete inhibition of Aβ aggregation.
- Sun, Yedi,Zhang, Guohua,Hawkes, Cheryl A.,Shaw, James E.,McLaurin, JoAnne,Nitz, Mark
-
p. 7177 - 7184
(2008/12/22)
-
- Synthesis of 2-deoxy-2-fluorinated inositol-1-O-dodecylphosphonates as inhibitors of glycosyl phosphatidylinositol phospholipase C
-
Three 2-deoxy-2-fluorinated inositols and their 1-O-dodecylphosphonate derivatives have been synthesized as non-cleavable inhibitors of glycosyl phosphatidylinositol phospholipase C. Their structure-activity relationship is discussed.
- Zhai,Lei,Morris,Mensa-Wilmot,Shen
-
p. 7403 - 7406
(2007/10/02)
-
- Synthesis of (±)-4-deoxy-4-fluoro-myo-inositol
-
4-Deoxy-4-fluoro-myo-inositol was prepared by means of DAST with reaction of configuration due to the assistance of a neighbouring benzyl ester.
- Ballereau,Guedat,Spiess,Rehnberg,Schlewer
-
p. 7449 - 7450
(2007/10/02)
-
- Total Synthesis of Fluorinated Analogues of Inositol and Inositol 1,4,5-Trisphosphate
-
Syntheses of fluorinated analogues of inositol and inositol 1,4,5-trisphosphate are described. 1-Deoxy-1-fluoro-scyllo-inositol, 2-deoxy-2,2-difluoro-myo-inositol, DL-2-deoxy-2-fluoro-scyllo-inositol 1,4,5-trisphosphate and DL-2-deoxy-2,2-difluoro-myo-ino
- Sawyer, Deborah A.,Potter, Barry V. L.
-
p. 923 - 932
(2007/10/02)
-
- Synthesis of -Labelled and Unlabelled 2-Deoxy-2-fluoro-myo-inositol and 1-Deoxy-1-fluoro-scyllo-inositol for Use in Studies of the Phosphoinositide Cycle
-
2-Deoxy-2-fluoro-myo-inositol and 1-deoxy-1-fluoro-scyllo-inositol have been synthesized in their unlabelled and tritiated forms in order to study their potential as inhibitors of the phosphoinositide cycle.
- Lowe, Gordon,McPhee, Fiona
-
p. 1249 - 1253
(2007/10/02)
-
- MICROBIAL OXIDATION IN SYNTHESIS: PREPARATION OF MYO-INOSITOL PHOSPHATES AND RELATED CYCLITOL DERIVATIVES FROM BENZENE.
-
Pseudomonas putida oxidation of benzene affords cis-3,5-cyclohexadiene-1,2-diol (2) which is used as a novel precursor for the synthesis of D- and L-myo-inositol 1,4,5-triphosphates, (-)-(1) and (+)-(1).The versatility of this approach to functionalised cyclitols is illustrated in the synthesis of myo-inositol 1-phosphate (19), 6-deoxy, 6-deoxy-6-fluoro, and 6-deoxy-6-methyl myo-inositols (31), (37) and (43), and their 1,4,5-trisphosphate derivatives (33), (39) and (45).
- Ley, Steven V.,Parra, Margarita,Redgrave, Alison J.,Sternfeld, Francine
-
p. 4994 - 5026
(2007/10/02)
-
- SYNTHESIS OF FLUORODEOXYSCYLLOINOSITOL AND PHOSPHATIDYLFLUORODEOXYSCYLLOINOSITOL
-
Synthesis of 1-fluoro-1-deoxyscylloinositol and 2-fluoro-2-deoxy-1-phosphatidylscylloinositol from myoinositol is described.
- Yang, Shu Shu,Beattie, Thomas R.,Shen, T. Y.
-
p. 5517 - 5520
(2007/10/02)
-