The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Methoxypiperidine( cas:4045-24-3 ) is researched.Electric Literature of C6H13NO.Du, Lifei; Wang, Xiaoyu; Cui, Guonan; Xu, Bailing published the article 《Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors》 about this compound( cas:4045-24-3 ) in Bioorganic & Medicinal Chemistry. Keywords: thiazole based derivative human Pin1 inhibitors; PPIase; Pin1; Pin1 inhibitor; Thiazole derivatives. Let’s learn more about this compound (cas:4045-24-3).
Pin1 is a peptidyl prolyl cis-trans isomerase (PPIase) and inhibiting Pin1 is a potential way for discovering anti-tumor agents. With an aim to find potent Pin1 inhibitors with a novel scaffold, a series of thiazole derivatives with an alicyclic heterocycles on the 2-position were designed, synthesized and tested against human Pin1. Compound 9p bearing a 2-oxa-6-azaspiro [3,3] heptane moiety on the thiazole scaffold was identified as the most potent Pin1 inhibitor of this series with an IC50 value of 0.95 μM. The structure-activity relationship (SAR) and mol. modeling study indicated that introducing an alicyclic ring with an H-bond acceptor would be a viable way to improve the binding affinity.
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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem