Fourteen phenanthroindolizidine alkaloids which differ in number, nature, and distribution of oxygen-bearing substitucnts, in the presence of unsaturation in ring E or in the presence of an angular (methyl or hydroxyl) function or in the cleaved phenanthrene portion were isolated from two species of Tylophora plant. These along with the synthesized unsubstituted molecule and its intermediates were examined for their amoebicidal activity in vitro and all had been found active with varying MIC's. Structure-activity relationships were deduced and common sti-octural-determinants of this activity with emctine were found. The acute toxicity of tylophorine hydrochloride was determined and the same was found to be equally effective in intestinal as well as hepatic amoebiasis in test animals.

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The N-Acyl-alpha-aminosuccinimides and N-Acyl-alpha-aminoglutarimides were reported to exhibit moderate anticonvulsant activities. These compounds were 5-membered or 6-membered alpha-amino cyclic imides and have N-CO-C-N moiety in their structures. Based on these structural characteristics, a series of 6-amino-1,4-oxazepine-3,5-dione derivatives 1, having a heterocyclic 7-memberd alpha-amino cyclic imide and N-CO-C-N moiety in their structures were designed and synthesized. These syntheses were in view to develop novel anticonvulsant compounds. The 6-amino-1, 4-oxazepine-3,5-dione derivatives were prepared from (S)-N-Cbz-serine by usual synthetic procedures and their anticonvulsant activities were examined by the MES and PTZ tests. The N-H (1a), N-methyl (1b), and N-n-butyl (1e) derivatives showed moderate anticonvulsant activities in the MES test. In the case of PTZ test, all the tested compounds except N-n-propyl compound(1c) also showed moderate anticonvulsant activities. Moreover, N-H (1a), N-methyl (1b), and N-n-butyl (1e) derivatives showed anticonvulsant activities in both the MES and PTZ test. From these studies, it was concluded that the 6-amino-1,4-oxazepane-3,5-dione derivatives were novel compounds enough to be recommended as new anticonvulsants.

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