Synthesis and structure—activity relationships of cyclopropane-containing analogs of pharmacologically active compounds

Diamides conformationally restricted with central amino acid: Design, synthesis, and biological activities

“…In the optimization of Bradykinin B 1 receptor antagonist and factor Xa inhibition [25], the replacement from phenyl ring to amino acids containing small alkyl ring has been deemed utility. The introduction of amino acid could improve several pharmaceutical properties of the molecule such as cytotoxicity, metabolic stability, and bioavailability [26,27]. In addition, those small‐ring‐containing subunits would impose conformational restriction on the compound for mimicking the bioactive conformation of the original molecule [28].…”

Recent Advances in Selected Asymmetric Reactions Promoted by Chiral Catalysts: Cyclopropanations, Friedel–Crafts, Mannich, Michael and Other Zinc-Mediated Processes—An Update

“…Some synthetic approaches with or without transition metals to achieve cyclopropyl ring have been reviewed in 2018 [13]. Moreover, some examples illustrating relationships between pharmacological activity and structure of various cyclopropyl derivatives have also been reported in 2018 [14].…”

A Remarkable Ring Opening Observed in the Reaction of Cyclopropyl Ferrocenyl Thioketone with Triiron Dodecacarbonyl Fe3(CO)12

“…Importance of the cyclopropane ring as an useful pharmacophore has been demonstrated in a series of recent original and review publications. [1] Moreover, great attention is focused on applications of 'donor-acceptor' cyclopropanes as versatile building blocks for synthesis of N-and S-heterocycles with diverse ring size. [2] Finally, the cyclopropyl ring was found as an important structural motif for studying radical mechanisms in organic reactions within so called 'radical clock approach'.…”