Oxa-spirocycles: synthesis, properties and applications.

ABSTRACT: A general approach to a new generation of spirocyclic molecules - oxa-spirocycles - was developed. The key synthetic step was iodocyclization. More than 150 oxa-spirocyclic compounds were prepared. Incorporation of an oxygen atom into the spirocyclic unit dramatically improved water solubility (by up to 40 times) and lowered lipophilicity. More potent oxa-spirocyclic analogues of antihypertensive drug terazosin were synthesized and studied in vivo.

SUBMITTER: Fominova K 

PROVIDER: S-EPMC8447932 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature