There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.
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.