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Literature DB >> 26113188

BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.

Alexandru Vlasceanu¹, Mikkel Jessing², John Paul Kilburn³.

Abstract

The application of BN/CC isosterism is explored as a method of expanding the scope of core scaffolds in biologically active compounds. The viability of potential drug candidates incorporating BN-heteroaromatic moieties was investigated through the synthesis of BN-substituted analogs to known phosphodiesterase (PDE10A) inhibitors, namely MP10 and a selection of N-methylanilide analogs. These in some cases revealed unexpectedly potent and relatively stable derivatives, providing further support for the potential of BN-incorporation in medicinal chemistry.

Entities: Chemical Gene

Keywords: Antipsychotics; Borazaronaphthalenes; PDE10A inhibitors

Mesh：

Substances：

Year: 2015 PMID： 26113188 DOI： 10.1016/j.bmc.2015.06.019

Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641

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Cited

19 in total

9. Exploring the strength of a hydrogen bond as a function of steric environment using 1,2-azaborine ligands and engineered T4 lysozyme receptors.

Authors: Yao Liu; Shih-Yuan Liu
Journal: Org Biomol Chem Date: 2019-07-16 Impact factor: 3.876

10. Site-Selective and Stereoselective trans-Hydroboration of 1,3-Enynes Catalyzed by 1,4-Azaborine-Based Phosphine-Pd Complex.

Authors: Senmiao Xu; Yuanzhe Zhang; Bo Li; Shih-Yuan Liu
Journal: J Am Chem Soc Date: 2016-11-01 Impact factor: 15.419

BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.

Review 1. The State of the Art in Azaborine Chemistry: New Synthetic Methods and Applications.

2. Synthesis of 1,2-Azaborines and the Preparation of Their Protein Complexes with T4 Lysozyme Mutants.

3. Medicinal Chemistry Profiling of Monocyclic 1,2-Azaborines.

4. Hydrogen Bonding of 1,2-Azaborines in the Binding Cavity of T4 Lysozyme Mutants: Structures and Thermodynamics.

5. Accessing Elaborated 2,1-Borazaronaphthalene Cores Using Photoredox/Nickel Dual-Catalytic Functionalization.

6. 3-Boryl-2,1-borazaronaphthalene: Umpolung Reagents for Diversifying Naphthalene Isosteres.

7. Cation-π binding ability of BN indole.

8. 1,2-Azaborine's Distinct Electronic Structure Unlocks Two New Regioisomeric Building Blocks via Resolution Chemistry.

9. Exploring the strength of a hydrogen bond as a function of steric environment using 1,2-azaborine ligands and engineered T4 lysozyme receptors.

10. Site-Selective and Stereoselective trans-Hydroboration of 1,3-Enynes Catalyzed by 1,4-Azaborine-Based Phosphine-Pd Complex.