Potential filaricides. 5. 3-Ethyl-8-methyl-1,3,8 ... - ACS Publications

Chem. , 1971, 14 (10), pp 929–931. DOI: 10.1021/jm00292a009. Publication Date: October 1971. ACS Legacy Archive. Cite this:J. Med. Chem. 14, 10, 929...
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Journal of Medicinal Chemistry, 29Y1, Vol. 14, N o . 10 929

STUDIES I N POTENTIAL FILARICIDES. 5

Studies in Potential Filaricides. 5. 3- Ethyl-8-methyl-l,3,8- tri azabicyclo[4.4.0]decan-2-one, a New Antifilarial Agent RANJNA SAXENA, SATYAVAN SHARMA, R. N. IYER,AND NITYAANAND* Division of Medicinal Chemistry, Central Drug Research Institute] I J u c k n m , India Received February 2, 1971 The synthesis of 3-ethy1-8-methy1-1,3,8-triazabicyc1o [4,4,0]decan-2-one possessing high microfilaricidal activity is reported.

I n earlier studies of this series, the syntheses of certain o p e n - ~ h a i nand ~ ~ ~cyclic4-* analogs of diethylcarbamazine (I) were described, but none of these compds possessed significant antifilarial activity. This communication describes the synthesis and antifilarial activity of 3-ethyl-8-methyl-l,3,S-triazabicyclo [4.4.0]decan-2-one (11),where the diethylcarbamazine molecule has been incorporated into a rigid framework.

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