Synthesis and biological activity of endomorphin-2 analogs incorporating piperidine-2-, 3- or 4-carboxylic acids instead of proline in position 2 was written by Staniszewska, Renata;Fichna, Jakub;Gach, Katarzyna;Toth, Geza;Poels, Jeroen;Vanden Broeck, Jozef;Janecka, Anna. And the article was included in Chemical Biology & Drug Design in 2008.Reference of 86069-86-5 The following contents are mentioned in the article:
Novel endomorphin-2 (EM-2) analogs have been synthesized, incorporating unnatural amino acids with six-membered heterocyclic rings, such as piperidine-2-, 3- and 4-carboxylic acids (Pip, Nip and Inp, resp.) instead of Pro in position 2. [(R)-Nip2]EM-2 displayed an extremely high affinity for the μ-opioid receptor with IC50 = 0.04 ± 0.01 nM in comparison with IC50 = 0.69 ± 0.03 nM for EM-2. This analog was also very potent in the aequorin luminescence-based functional calcium assay and showed significantly enhanced stability in rat brain homogenate. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Reference of 86069-86-5).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Reference of 86069-86-5
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem