23-nor-23-thia avermectin analogs are active anthelmintic agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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549 14, 514 30, 536 71, A61K 3139, C07D41114

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active

051623633

ABSTRACT:
Avermectin analogs are prepared where the 23-position ring carbon atom is deleted and replaced by a sulfur atom. The compounds are prepared by opening the outer spiroketal ring to gain access to the 23-position atom, substituting the ring-opened compounds with a substituent containing the sulfur atom in the appropriate position and closing the ring to prepare the desired compounds. The compounds are potent anthelmintic agents and methods and compositions including such 23-nor-23-thia compounds are also disclosed.

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