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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
chemistry
Synthesis of substituted pyrimidines as corticotropin releasing factor (CRF) receptor ligands
European Journal of Medicinal Chemistry, Volume 78, Year 2014
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Description
Corticotropin releasing factor (CRF) is a neuropeptide hormone produced from the hypothalamus that controls the secretion of corticotropin (ACTH) from the anterior pituitary gland that, in turn, prompts the adrenal glands to secrete glucocorticoids. This involvement in the hypothalamic-pituitary-adrenal axis (HPA) in response to stress and also playing a key role in behavioral, cardiovascular, immune and gastrointestinal systems made CRF binding to its receptors an important target in drug discovery aiming to develop lead compounds with the potential to treat various stress-related disorders including depression, anxiety and addictive disorders. Several non-peptide CRF1 receptor antagonists were developed by pharmaceutical companies and are currently in clinical trials with the aim of improving the health consequences of chronic stress and for use in the clinical management of anxiety and stress. Many showed promising results not only in treatment of anxiety and depression but also in treatment of CRF-induced hypertension, as well as in treatment of arthritis, irritable bowel syndrome and peptic ulcers. In this manuscript, we describe the synthesis of substituted pyrimidines with close structural similarities to reported lead compounds with promising CRF1 receptor affinities and carrying groups known to be associated with optimum affinity to CRF1 receptors. The affinity of the newly prepared compounds in comparison to antalarmin, a potent CRF1 receptor antagonist in clinical trials as a standard, is also described. Four compounds from the new series showed promising CRF1 receptor affinity. © 2014 Elsevier B.V. All rights reserved.
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
Fahmy, Hesham Tawfik Youssef
United States, Brookings
South Dakota State University
Statistics
Citations: 11
Authors: 4
Affiliations: 2
Identifiers
Doi:
10.1016/j.ejmech.2014.03.040
ISSN:
02235234
Research Areas
Mental Health
Noncommunicable Diseases