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Hemoglobin S antigelation agents based on 5-bromotryptophan with potential for sickle cell anemia
P Z De Croos1, P Sangdee, B L Stockwell
1Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois, Chicago 60680.
Journal of Medicinal Chemistry
|December 1, 1990
Summary
Researchers synthesized novel dipeptides containing 5-Bromotryptophan (5-BrTrp) to inhibit hemoglobin S gelation. The dipeptide 5-BrTrp-5-BrTrp demonstrated significantly enhanced antigelation activity, showing promise for sickle cell anemia treatment.
Area of Science:
- Biochemistry
- Medicinal Chemistry
Background:
- Sickle cell anemia involves the gelation of hemoglobin S.
- Amino acid derivatives, such as tryptophan (Trp), show potential in inhibiting this process.
- 5-Bromotryptophan (5-BrTrp) is a known potent inhibitor of hemoglobin S gelation.
Purpose of the Study:
- To synthesize and evaluate the antigelation activity of dipeptides containing 5-Bromotryptophan.
- To identify novel compounds with improved efficacy for sickle cell anemia.
Main Methods:
- Synthesis of dipeptides incorporating 5-Bromotryptophan.
- Evaluation of the antigelation activity of these synthesized dipeptides.
Main Results:
- The dipeptide 5-Bromotryptophan-5-Bromotryptophan (5-BrTrp-5-BrTrp) exhibited the highest antigelation potency, 5.9 times that of tryptophan.
- Other synthesized dipeptides, including 5-BrTrp-Trp and Trp-5-BrTrp, also showed significant antigelation activity.
- The potency order observed was 5-BrTrp-5-BrTrp > 5-BrTrp-Trp > Trp-5-BrTrp.
Conclusions:
- Dipeptides containing 5-Bromotryptophan demonstrate enhanced antigelation activity compared to single amino acids.
- 5-BrTrp-5-BrTrp and 5-BrTrp-Trp are identified as lead compounds for further investigation in sickle cell anemia therapeutics.