These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Synthesis of novel sulfamides incorporating phenethylamines and determination of their inhibition profiles against some metabolic enzymes.
    Author: Aksu K, Akıncıoğlu H, Akıncıoğlu A, Göksu S, Tümer F, Gülçin İ.
    Journal: Arch Pharm (Weinheim); 2018 Sep; 351(9):e1800150. PubMed ID: 30074266.
    Abstract:
    A series of sulfamides were synthesized and evaluated for their acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and carbonic anhydrase inhibition properties. The synthesis of sulfamides was achieved by the reactions of phenethylamines with N,N-dimethylsulfamoyl chloride in the presence of Et3 N. The methoxylated sulfamides were converted into their phenolic derivatives with BBr3 for structure-activity relationships. The synthesized sulfamide/phenolic sulfamide derivatives were investigated as cholinesterase inhibitors and their relative role in AChE versus BChE inhibition was defined. Sulfamide/phenolic sulfamide derivatives are known as important carbonic anhydrase inhibitors; therefore, the synthesized compounds were investigated for inhibitory effects on both carbonic anhydrase isoenzymes. Additionally, we evaluated four different enzymes, which were inhibited in the low nanomolar range by these compounds. According to the present studies, for AChE, BChE, and carbonic anhydrase I and II, the ranges of results are recorded as 0.027-0.076 nM, 0.075-0.327 nM, 0.123-0.678 nM, and 0.024-0.688 nM, respectively.
    [Abstract] [Full Text] [Related] [New Search]