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1.
Org Biomol Chem ; 11(43): 7455-7, 2013 Nov 21.
Article in English | MEDLINE | ID: mdl-24089031

ABSTRACT

A recent report has indicated that the oxidizing agent Oxone does not possess the ability to cleave the 2,3-carbon-carbon bond of indole. Work in our laboratory shows that this is not the case. Indole and a variety of aryl ring substituted derivatives readily react to form synthetically important isatoic anhydrides.

2.
Bioorg Med Chem Lett ; 22(8): 2980-2, 2012 Apr 15.
Article in English | MEDLINE | ID: mdl-22425568

ABSTRACT

The shortfalls of the current treatment options against infections with the parasite Toxoplasma gondii (T. gondii) necessitates the development of non-toxic and well-tolerated alternatives. To address this problem a structurally diverse panel of berberine alkaloids was synthesized and evaluated for in vitro inhibition of T. gondii tachyzoites. Inhibitory doses (ID(50)) of less than 50 nM and therapeutic indices (TI) up to 4000 were observed.


Subject(s)
Antiparasitic Agents/chemistry , Antiparasitic Agents/pharmacology , Berberine/chemistry , Berberine/pharmacology , Toxoplasma/drug effects , Antiparasitic Agents/chemical synthesis , Berberine/chemical synthesis , Cells, Cultured , Inhibitory Concentration 50
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