23921-67-7

Upstream product

• 13037-60-0 1-bromo-2-isothiocyanatobenzene 
• 118-92-3 anthranilic acid 
• 134-20-3 2-carbomethoxyaniline 

Downstream Products

• 105362-94-5 3-Amino-2-(2-bromo-phenylamino)-3H-quinazolin-4-one 

Relevant academic research and scientific papers

Energy barriers to rotation in axially chiral quinazoline-4-ones

Axially chiral 2-thioxo-3-(o-aryl)-quinazolin-4-ones and 2-(benzylthio)-3-(o-aryl)-quinazolin-4-ones were synthesized and their energy barriers to rotation about the N3-Caryl bond were determined by thermal racemization of the separa

Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model

A simple and efficient synthetic method for the preparation of quinazoline type phosphodiesterase 7 (PDE7) inhibitors, based on microwave irradiation, has been developed. The use of this methodology improved yields and reaction times, providing a scalable procedure. These compounds are pharmacologically interesting because of their in vivo efficacy both in spinal cord injury and Parkinson's disease models, as shown in previous studies from our group. Herein we describe for the first time that administration of one of the PDE7 inhibitors here optimized, 3-phenyl-2,4-dithioxo-1,2,3,4-tetrahydroquinazoline (compound 5), ameliorated brain damage and improved behavioral outcome in a permanent middle cerebral artery occlusion (pMCAO) stroke model. Furthermore, we demonstrate that these PDE7 inhibitors are potent anti-inflammatory as well as neuroprotective agents in primary cultures of neural cells. These results led us to propose PDE7 inhibitors as a new class of therapeutic agents for neuroprotection.

CODES, a novel procedure for ligand-based virtual screening: PDE7 inhibitors as an application example

Phosphodiesterase (PDE) 7 is a high affinity cAMP-specific PDE whose functional role in T-cells has been the subject of some controversy. Recent findings on tissue distribution, however, support the hypothesis that PDE7 could be a good target for the treatment of airway diseases, T-cell related diseases or central nervous system (CNS) disorders. Therefore, the identification of selective inhibitors targeted against PDE7 enzyme has become an attractive area of research. We report here the first use of the descriptors generated by the CODES program for ligand-based virtual screening. This program codifies molecules from a topological point of view and the generated descriptors are related to the chemical nature of the atoms, the atomic bonds and the connectivity with the rest of the molecule. They are also able to distinguish among stereoisomers. By using this approach, 173 compounds were codified, and their similarity with the reference compound was analysed. Based on the analysis, new potential PDE7 inhibitors have been identified, synthesized and biologically evaluated confirming that CODES descriptors are valid for ligand-based virtual screening and provided new lead compounds for further optimization as potent and selective PDE7 inhibitors.

A facile photochemical synthesis of 12H-benzothiazolo[2,3-b]quinazolin-12-ones

The photochemical synthesis of 12H-benzothiazolo[2,3-b]quinazolin-12-ones (4) by the irradiation of 2-thioquinazolinediones 1 and disulphide 5 are described.