The synthesis of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as potent CRTh 2 antagonists
| Autor: | Ravi P. Nargund, Li-Kang Zhang, Xiaoxin Yang, Hongchen Qiu, Anandan Palani, Xianhai Huang, Craig C. Correll, Robert G. Aslanian, Wei Zhou, Ashwin U. Rao, Alexei V. Buevich, Charles G. Garlisi |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
010405 organic chemistry
Stereochemistry Chemistry Organic Chemistry Clinical Biochemistry Intramolecular cyclization Pharmaceutical Science 010402 general chemistry 01 natural sciences Biochemistry Combinatorial chemistry 0104 chemical sciences Catalysis Drug Discovery Molecular Medicine Structure–activity relationship Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 27:5344-5348 |
| ISSN: | 0960-894X |
| Popis: | New synthetic methods were developed for the preparation of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as CRTh2 antagonists. The isoquinolinone core could be constructed before the introduction of substitution groups or synthesized through a catalytic intramolecular cyclization reaction with desired substitution groups properly installed. These synthetic strategies have helped to accelerate the SAR development of this series, and potent lead compounds were identified in both the CRTh2 receptor binding assay and the CD11b biomarker assay. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect