2. Academic Validation
  3. Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production

Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production

  • Bioorg Med Chem Lett. 2007 Oct 15;17(20):5693-7. doi: 10.1016/j.bmcl.2007.07.059.
Lain-Yen Hu 1,  Huangshu John Lei,  Daniel Du,  Theodore R Johnson,  Victor Fedij,  Catherine Kostlan,  Wen Song Yue,  Mark Lovdahl,  Jie Jack Li,  Mathew Carroll,  Danielle Dettling,  Jeffrey Asbill,  Conglin Fan,  Kimberly Wade,  David Pocalyko,  Kimberly Lapham,  Radhika Yalamanchili,  Brian Samas,  Derek Vrieze,  Susan Ciotti,  Teresa Krieger-Burke,  Drago Sliskovic,  Howard Welgus
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. [email protected]
PMID: 17766112 DOI: 10.1016/j.bmcl.2007.07.059
Abstract

A series of amino-pyridines were synthesized and evaluated for androgen antagonist activities. Among these compounds, (R)-(+)-6-[methyl-(1-phenyl-ethyl)-amino]-4-trifluoromethyl-nicotinonitrile was the most active example of this class. This compound displayed potent Androgen Receptor antagonist activity as well as favorable pharmacokinetic characteristics for a potential topical agent. It also demonstrated remarkable potency for stimulating hair growth in a male C3H mouse model as well as reducing sebum production in the male Syrian hamster ear model.

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