1237750-37-6Relevant academic research and scientific papers
Esters of levonorgestrel and etonogestrel intended as single, subcutaneous-injection, long-lasting contraceptives
Meece, Frederick A.,Ahmed, Gulzar,Nair, Hareesh,Santhamma, Bindu,Tekmal, Rajeshwar R.,Zhao, Chumang,Pollok, Nicole E.,Lara, Julia,Shaked, Ze'ev,Nickisch, Klaus
, p. 47 - 56 (2018)
An effort with the goal of discovering single-dose, long-lasting (>6 months) injectable contraceptives began using levonorgestrel (LNG)-17-β esters linked to a sulfonamide function purposed as human carbonic anhydrase II (hCA 2) ligands. One single analog from this first series showed noticeably superior anti-ovulatory activity in murine models, and a subsequent structure-activity relationship (SAR, the relationship between a compound's molecular structure and its biological activity) study based on this compound identified a LNG-phenoxyacetic acid ester analog exhibiting longer anti-ovulatory properties using the murine model at 2 and 4 mg dose than medroxyprogesterone acetate (MPA). The same ester function linked to etonogestrel (ENG) furnished a compound which inhibited ovulation at 2 mg for 60 days, the longest duration of all compounds tested at these doses. By comparison, MPA at the same dose inhibited ovulation for 32 days.
Design and synthesis of C60-benzenesulfonamide conjugates
Zakharian, Tatiana Y.,Christianson, David W.
supporting information; experimental part, p. 3645 - 3648 (2010/08/19)
Synthesis of C60-benzenesulfonamide conjugates is reported. The strategies for improving their water solubility, as required for binding to human carbonic anhydrase II, are discussed.
