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Sulfamates in drug design and discovery: Pre-clinical and clinical investigations.
- Source :
-
European Journal of Medicinal Chemistry . Oct2019, Vol. 179, p257-271. 15p. - Publication Year :
- 2019
-
Abstract
- In the present article, we reviewed the sulfamate-containing compounds reported as bioactive molecules. The possible molecular targets of sulfamate derivatives include steroid sulfatase enzyme, carbonic anhydrases, acyl transferase, and others. Sulfamate derivatives can help treat hormone-dependent tumors including breast, prostate, and endometrial cancers, Binge eating disorder, migraine, glaucoma, weight loss, and epilepsy. Sulfamate derivatives can act also as calcium sensing receptor agonists and can aid in osteoporosis. Furthermore, acyl sulfamate derivatives can act as antibacterial agents against Gram-positive bacteria. A recent study revealed a new side effect of topiramate, a sulfamate-containing compound, which is sialolithiasis. The structural and biological characteristics of the reviewed compounds are presented in detail. Image 1 • The recently reported biologically active sulfamate derivatives have been reviewed. • Sulfamates have been reported as inhibitors of STS, aromatase, carbonic anhydrases (CAs), and 17β-HSD. • Irosustat (7) is an STS inhibitor with no estrogenic side effects and currently in clinical trials. • Compound 33 is DASI, it inhibits both STS and aromatase enzymes. • Topiramate (46) inhibits CA and when combined with phentermine can treat epilepsy and cause weight loss. [ABSTRACT FROM AUTHOR]
- Subjects :
- *DRUG design
*SULFAMATES
*BIOACTIVE compounds
*COMPULSIVE eating
*WEIGHT loss
Subjects
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 179
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 138342234
- Full Text :
- https://doi.org/10.1016/j.ejmech.2019.06.052