Synthesis of Novel Derivatives of NMDARs Allosteric Modulators
     
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Synthesis of Novel Derivatives of NMDARs Allosteric Modulators

Syntheses of novel allosteric modulators of NMDARsN-methyl-D-aspartate receptors (NMDARs) are ligand-gated ion channels wich is activated by L-glutamate (the brain’s primary excitatory neurotransmitter). They have many critical roles in CNS function and in various neurological and psychiatric disorders.

We offer the chemical optimization service - synthesis of NMDARs targeted-specific sets of novel sulfonamides, quinazoline-4-ones, pyrazolines, iminothiazolidinones, N-arylbenzamides, coumarin-3-carboxylic acids, benzenesulfonamides, thiazoles and tetrahydroisoquinolines for your biological projects. These novel compounds will be selected from a sets of 1,000 - 2,000+ unique virtual derivatives for each chemical class using our company’s proprietary molecular modeling platform.

These target-specific sets of novel derivatives will be synthesized exclusively upon your request.

This is referred to a paper from Journal of Medicinal Chemistry* which showed that significant progress has been made in the development of selective positive and negative allosteric modulators (PAMs and NAMs) of NMDARs:

Syntheses of novel allosteric modulators of NMDARs

Novel derivatives of NAMs and PAMs provide a perfect basis for drug discovery projects related with pain, stroke, epilepsy, schizophrenia, post-traumatic stress disorder, depression and various neurodegenerative diseases such as Alzheimer’s and Parkinson’s.

* Erica S. Burnell, Mark Irvine, Guangyu Fang, Kiran Sapkota, David E. Jane, Daniel T. Monaghan. Positive and Negative Allosteric Modulators of N‑Methyl‑D‑aspartate (NMDA) Receptors: Structure − Activity Relationships and Mechanisms of Action. J. Med. Chem. 2019, Vol. 62, pp. 3−23, DOI: 10.1021/acs.jmedchem.7b01640.


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