- ADENOSINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
-
Disclosed here is an adenosine derivative prodrug that can have reverse transcriptase inhibitor activity in vivo. This disclosure is also directed to a pharmaceutical composition comprising the adenosine derivative that can be used for the treatment of HIV infection or RNA virus infection.
- -
-
Paragraph 000221
(2021/02/05)
-
- 4-methylamino butyric acid hydrochloride synthesis process
-
The invention discloses a 4-methylamino butyric acid hydrochloride synthesis process, which comprises: adding N-methyl-2-pyrrolidone and concentrated hydrochloric acid into a reaction kettle, carryingout stirring reflux for 5-10 h under an external bath of 130-170 DEG C, supplementing concentrated hydrochloric acid, carrying out stirring reflux for 4-7 h, carrying out pressure reducing distillation to remove hydrochloric acid, adding cold acetone to the remaining solid, stirring, cooling to make the solid form a crystal, freezing to completely precipitate, filtering, washing twice with cold acetone, draining, and drying to obtain the product. According to the present invention, the yield is more than 80%.
- -
-
Paragraph 0009; 0010; 0011
(2018/06/16)
-
- Synthesis and evaluation of xanomeline analogs-Probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor
-
A series of xanomeline analogs were synthesized and evaluated for binding at the M1 muscarinic acetylcholine receptor (M1 receptor). Specifically, compounds that substitute the O-hexyl chain of xanomeline with polar, ionizable, or conformationally restricted moieties were assessed for their ability to bind to the M1 receptor in a wash-resistant manner (persistent binding). From our screen, several novel ligands that persistently bind to the M1 receptor with greater affinity than xanomeline were discovered. Results indicate that persistent binding may arise not only from hydrophobic interactions but also from ionic interactions with a secondary M1 receptor binding site. Herein, a qualitative model that accounts for both binding scenarios is proposed and applied to understand the structural basis to wash-resistant binding and long-acting effects of xanomeline-based compounds.
- Kane, Brian E.,Grant, Marianne K.O.,El-Fakahany, Esam E.,Ferguson, David M.
-
p. 1376 - 1392
(2008/09/18)
-