Tryptanthrin derivatives as Toxoplasma gondii inhibitors--structure-activity-relationship of the 6-position.

A panel of derivatives of the natural product tryptanthrin was synthesized and screened for its in vitro activity against the intracellular parasite Toxoplasma gondii. We concentrated on the modification of the 6-keto group of tryptanthrin and prepared a series of oximes, hydrazones and alcohols based on tryptanthrin. We evaluated parasite growth inhibition and host cell cytotoxicity.

Structure-activity studies of some berberine analogs as inhibitors of Toxoplasma gondii.

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.

7,9-Dichloro-6H,12H-indolo[2,1-b]quinazoline-6,12-dione.

There are two independent mol-ecules in the asymmetric unit of the title compound, C(15)H(6)Cl(2)N(2)O(2). The conjugated four-ring system is essentially planar in each mol-ecule [maximum deviation = 0.089 (2) Å].