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A kind of small molecule oxathiazide derivative and its application
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A technology of oxathiazine and small molecules, which is applied in the field of small molecule oxthiazide derivatives, and can solve problems in the preclinical research stage or clinical trial stage
Active Publication Date: 2021-03-09
WEST CHINA HOSPITAL SICHUAN UNIV
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Existing research results have pointed out the direction for the design of AMPA receptor positive allosteric modulators, but most of them are in the preclinical research stage or clinical trial stage
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Embodiment 1
[0050] Compound disclosed in this example: LT-1,8-(4-methoxyphenyl)-3,4-dihydrobenzo[e][1,2,3]oxathiazine 2,2-dioxide (LT -1)
[0054] The specific preparation method is as follows:
[0055] At 0°C, 3-bromo-2-hydroxybenzaldehyde (A01a) (5.6g, 28mmol) was dispersed in 60ml of dimethylacetamide DMA, and then aminosulfonyl chloride (10g, 86.5 mmol). The reaction system was stirred and slowly raised to room temperature until the reaction was complete. After the reaction, add water to precipitate the solid, filter and wash the filter cake with water and ethyl acetate respectively, and obtain the off-white compound as 8-bromobenzo[e][1,2,3]oxathiazine 2 with a yield of 85%. 2-dioxide (A01b).
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Abstract
The invention belongs to the field of organic synthetic medicine, and specifically relates to a small-molecule oxathiazine derivative, whose general formula is as follows: the small-molecule oxthiazine derivative can be used as a positive allosteric regulator of AMPA receptors, which proves that The compound can positively regulate the AMPA receptor, and can make the conformation of the agonist (such as endogenous neurotransmitter glutamate) more stable after binding to the receptor, thereby reducing the inactivation rate of the receptor and inhibiting the desensitization of the receptor. Enhance the function of AMPA receptors.
Description
technical field [0001] The invention relates to the technical field of innovative chemical medicines, in particular to a small molecule oxathiazine derivative and its application. Background technique [0002] AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors are an important subtype of ionotropic glutamate receptors, mainly distributed in the postsynaptic membrane of the central nervous system, Composed of four core subunits G1uR1~4, it mediates the main rapid excitatory transmission in the central nervous system, promotes neural development and outstanding plasticity, and participates in various neural activity processes. Important targets related to systemic diseases. [0003] The extracellular domain of each AMPA receptor subunit contains two domains: the amino-terminal domain (amino-terminal domain, ATD) involved in subunitassembly and the ligand-binding domain (Ligand binding domain, LBD) that provides glutamate binding. Studies have shown that t...
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