Journal of Medicinal Chemistry 1990-12-01

Hemoglobin S antigelation agents based on 5-bromotryptophan with potential for sickle cell anemia.

P Z De Croos, P Sangdee, B L Stockwell, L Kar, E B Thompson, M E Johnson, B L Currie

文献索引：J. Med. Chem. 33(12) , 3138-42, (1990)

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摘要

5-Bromotryptophan (5-BrTrp) is the most potent amino acid derivative reported in the literature to inhibit the gelation of hemoglobin S (from sickle cell anemia patients). Trp-Trp is also more potent than Trp as an antigelation agent. Therefore, we have prepared a series of dipeptides containing 5-BrTrp and evaluated the antigelation activity. 5-BrTrp-5-BrTrp is the most potent, i.e., 5.9 times the activity of Trp, followed by 5-BrTrp-Trp and then Trp-5-BrTrp. This improved antigelation potency for 5-BrTrp-5-BrTrp and 5-BrTrp-Trp is very significant and will be pursued further as lead compounds with potential for sickle cell anemia.