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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
pharmacology, toxicology and pharmaceutics
Synthesis of new thiazolo[4,5-d]pyrimidines as corticotropin releasing factor modulators
Medicinal Chemistry, Volume 11, No. 1, Year 2015
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Description
Corticotropin-releasing factor (CRF) is a neurohormone that plays a crucial role in integrating the body's overall response to stress. It appears necessary and sufficient for the organism to mount functional, physiological and endocrine responses to stressors. CRF is released in response to various triggers such as chronic stress. The role of CRF and its involvement in these neurological disorders suggest that new drugs that can target the CRF function or bind to its receptors may represent a new development of neuropsychiatric medicines to treat various stress-related disorders including depression, anxiety and addictive disorders. Based on pharmacophore of the CRF1 receptor antagonists, a new series of thiazolo[4,5-d] pyrimidines were synthesized as Corticotropin-releasing factor (CRF) receptor modulators and the prepared compounds carry groups shown to produce optimum binding affinity to CRF receptors. Twenty two compounds were evaluated for their CRF1 receptor binding affinity in HEK 293 cell lines and two compounds 5o and 5s showed approximately 25% binding affinity to CRF1 receptors. Selected compounds (5c and 5f) were also evaluated for their effect on expression of genes associated with depression and anxiety disorders such as CRF1, CREB1, MAO-A, SERT, NPY, DatSLC6a3, and DBH and significant upregulation of CRF1 mRNA has been observed with compound 5c. © 2015 Bentham Science Publishers.
Authors & Co-Authors
Kuppast, Bhimanna K.
United States, Brookings
South Dakota State University
Spyridaki, Katerina
Greece, Rethymnon
University of Crete
Liapakis, George
Greece, Rethymnon
University of Crete
Davies, Gareth E.
United States, Sioux Falls
Avera Health
United States, Vermillion
University of South Dakota
United States, Brookings
South Dakota State University
Fahmy, Hesham Tawfik Youssef
United States, Brookings
South Dakota State University
Statistics
Citations: 8
Authors: 5
Affiliations: 4
Identifiers
Doi:
10.2174/1573406410666140724115627
ISSN:
15734064
Research Areas
Mental Health