| Autor: |
Frederick A, Meece, Gulzar, Ahmed, Hareesh, Nair, Bindu, Santhamma, Rajeshwar R, Tekmal, Chumang, Zhao, Nicole E, Pollok, Julia, Lara, Ze'ev, Shaked, Klaus, Nickisch |
| Rok vydání: |
2018 |
| Předmět: |
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| Zdroj: |
Steroids. 137 |
| ISSN: |
1878-5867 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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Full Text from ScienceDirect