Diphenyl Ethers as Androgen Receptor Antagonists for the Topical Suppression of Sebum Production

In 2009, Pfizer Global Research and Development conducted a study on the use of diphenyl ethers as androgen receptor antagonists to suppress sebum production, which is linked to conditions like acne and alopecia. The research found that diphenyl ethers, when applied topically, could bind to the androgen receptor and reduce sebum production. The study prepared and evaluated a series of diphenyl ethers for their androgen receptor antagonist activity. Several compounds, particularly 1, 2, and 6i, showed over 80% reduction of wax esters, a component of sebum, in a Golden Syrian Hamster ear model when applied as a 3% topical formulation. The study concluded that diphenyl ethers could potentially be used as topical treatments for conditions related to excess sebum production.