title: Hemoglobin S antigelation agents based on 5-bromotryptophan with potential for sickle cell anemia.
abstract: 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.
authors: Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois, Chicago 60680.
authors: P Z
authors: PZ
authors: De Croos
authors: P
authors: P
authors: Sangdee
authors: B L
authors: BL
authors: Stockwell
authors: L
authors: L
authors: Kar
authors: E B
authors: EB
authors: Thompson
authors: M E
authors: ME
authors: Johnson
authors: B L
authors: BL
authors: Currie
mesh_terms: D000755:Anemia, Sickle Cell / Q000097:blood* / Q000188:drug therapy; D000818:Animals; D004151:Dipeptides / Q000138:chemical synthesis / Q000494:pharmacology; D005782:Gels; D006451:Hemoglobin, Sickle / Q000737:chemistry*; D006801:Humans; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D013329:Structure-Activity Relationship; D014364:Tryptophan / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D004151:Dipeptides; D005782:Gels; D006451:Hemoglobin, Sickle; C066614:5-bromotryptophan; D014364:Tryptophan