Synthesis of novel triplet drugs with 1, 3, 5-trioxazatriquinane skeletons and their pharmacologies. 3: Synthesis of novel triplet drugs with the bis (epoxymethano) or bis …

N Wada, H Fujii, K Koyano, S Hirayama, T Iwai… - Bioorganic & medicinal …, 2012 - Elsevier
N Wada, H Fujii, K Koyano, S Hirayama, T Iwai, T Nemoto, H Nagase
Bioorganic & medicinal chemistry letters, 2012Elsevier
Novel double-capped triplet drugs, which have one pharmacophore unit and two
epoxymethano or dimethylepoxymethano structures (termed cap or diMe-cap structures,
respectively) were synthesized. Key intermediate oxazoline 16 derived from acetone
enabled the effective synthesis of double-capped triplets. SYK-134 (7a) and SYK-135 (8a)
with N-cyclopropylmethyl substituent and cap structures showed selectivities for the κ opioid
receptor. On the other hand, the N-Me series exhibited selectivities for the μ opioid receptor …
Novel double-capped triplet drugs, which have one pharmacophore unit and two epoxymethano or dimethylepoxymethano structures (termed cap or diMe-cap structures, respectively) were synthesized. Key intermediate oxazoline 16 derived from acetone enabled the effective synthesis of double-capped triplets. SYK-134 (7a) and SYK-135 (8a) with N-cyclopropylmethyl substituent and cap structures showed selectivities for the κ opioid receptor. On the other hand, the N-Me series exhibited selectivities for the μ opioid receptor. The double-capped triplet drugs with diMe-cap structures preferred the μ receptor independently of their N-substituents. SYK-385 (19b), one of the μ-selective double-capped triplet drugs, showed the highest selectivity for the μ receptor among the reported μ-selective nonpeptide ligands.
Elsevier
以上显示的是最相近的搜索结果。 查看全部搜索结果