Literature DB >> 9873487

Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.

D J Wustrow1, T Capiris, R Rubin, J A Knobelsdorf, H Akunne, M D Davis, R MacKenzie, T A Pugsley, K T Zoski, T G Heffner, L D Wise.   

Abstract

A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series, 10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.

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Year:  1998        PMID： 9873487     DOI： 10.1016/s0960-894x(98)00372-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Synthesis, F-18 radiolabeling, and microPET evaluation of 3-(2,4-dichlorophenyl)-N-alkyl-N-fluoroalkyl-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-amines as ligands of the corticotropin-releasing factor type-1 (CRF1) receptor.

Authors:  Jeffrey S Stehouwer; Matthew S Birnbaum; Ronald J Voll; Michael J Owens; Susan J Plott; Chase H Bourke; Michael A Wassef; Clinton D Kilts; Mark M Goodman
Journal:  Bioorg Med Chem       Date:  2015-06-19       Impact factor: 3.641

2.  (E)-3,5-Dimethyl-1-p-tolyl-4-(p-tolyl-diazen-yl)-1H-pyrazole.

Authors:  Carlos Bustos; Marcia Pérez-Cerda; Luis Alvarez-Thon; Enrique Barrales-Salcedo; Maria Teresa Garland
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-01-11

3.  Synthesis of new pyrazolyl-2, 4-thiazolidinediones as antibacterial and antifungal agents.

Authors:  Deepak K Aneja; Poonam Lohan; Sanjiv Arora; Chetan Sharma; Kamal R Aneja; Om Prakash
Journal:  Org Med Chem Lett       Date:  2011-11-08

4.  Synthesis of pyrazolopyrimidinones using a "one-pot" approach under microwave irradiation.

Authors:  Mark Kelada; John M D Walsh; Robert W Devine; Patrick McArdle; John C Stephens
Journal:  Beilstein J Org Chem       Date:  2018-05-28       Impact factor: 2.883

5.  Consecutive three-component synthesis of 3-(hetero)aryl-1H-pyrazoles with propynal diethylacetal as a three-carbon building block.

Authors:  Lucilla Levi; Christina Boersch; Charlotte F Gers; Eugen Merkul; Thomas J J Müller
Journal:  Molecules       Date:  2011-11-07       Impact factor: 4.411

6.  Synthesis, crystal structure, DFT studies and biological activity of (Z)-3-(3-bromophenyl)-1-(1,5-dimethyl-1H-pyrazol-3-yl)-3-hydroxyprop-2-en-1-one.

Authors:  Said Tighadouini; Redouane Benabbes; Monique Tillard; Driss Eddike; Khadija Haboubi; Khalid Karrouchi; Smaail Radi
Journal:  Chem Cent J       Date:  2018-11-26       Impact factor: 4.215
  6 in total

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