Structural analogs of leukotrienes C and D and their contractile activities.
- 1 January 1982
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 30 (7) , 2453-2462
- https://doi.org/10.1248/cpb.30.2453
Abstract
Thirteen structural analogs of leukotrienes C and D were prepared and tested for contractile activities on guinea pig pulmonary parenchymal strips. The analogs differed from the native structures in the peptide moiety, the 5-hydroxyl group, the carboxyl group and in the number and geometry of ethylenic bonds. Deamino analogs of leukotriene C4 (LTC4) and leukotriene D4 (LTD4) retained substantial contractile activities. Amide analogs of LTD4 and 5-O-methyl-LTC4 showed some activity. Modification of the peptide moiety caused a 1-3 orders of magnitude decrement. Analogs in which the various ethylenic bonds were saturated retained substantial contractile activity. However, perhydro LTD had no contractile activity.Keywords
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