An expedient and facile one-step synthesis of a biguanide library by microwave irradiation coupled with simple product filtration. Inhibitors of dihydrofolate reductase

Journal of Combinatorial Chemistry
Stanislas MayerMichael G Organ

Abstract

It has been demonstrated previously by us that guanide-containing compounds (1 and 2) can inhibit significantly dihydrofolate reductase (DHFR). In this report, we have produced an array of alkyl- and aryl-based biguanide compounds using microwave irradiation. Further, we have demonstrated the use of TMSCl for the first time as an excellent and practical catalyst for the formation of alkyl and aryl biguanides. Using these methods, we prepared a 60-compound collection, of which one compound (21g) showed approximately one-half of the inhibitory activity of the parent compound 2.

Citations

Apr 16, 2010·Expert Opinion on Therapeutic Targets·Thomas D Lockwood
Oct 8, 2015·Organic & Biomolecular Chemistry·Chen ZhangDong-Mei Cui
May 3, 2019·Biometals : an International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine·Thomas D Lockwood
Aug 20, 2009·Inorganic Chemistry·Alexander G TskhovrebovVadim Yu Kukushkin
May 25, 2021·Beilstein Journal of Organic Chemistry·Oleksandr GrytsaiRachid Benhida
Dec 13, 2019·The Journal of Organic Chemistry·Rosaura Padilla-SalinasHang Yin
Aug 3, 2017·Biochemistry·Scott A GabelRobert E London
Nov 15, 2005·Journal of Combinatorial Chemistry·Roland E Dolle

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