1225477-99-5Relevant academic research and scientific papers
Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1)
Ye, Xiang-Yang,Chen, Stephanie Y.,Nayeem, Akbar,Golla, Rajasree,Seethala, Ramakrishna,Wang, Mengmeng,Harper, Timothy,Sleczka, Bogdan G.,Li, Yi-Xin,He, Bin,Kirby, Mark,Gordon, David A.,Robl, Jeffrey A.
supporting information; experimental part, p. 6699 - 6704 (2011/12/21)
Starting from high throughput screening hit 2-adamantyl acetic acid 3, a series of polycyclic acids have been designed and synthesized as novel, potent, and selective inhibitors of human 11β-HSD-1. Structure-activity relationships of two different regions
Synthesis and pharmacological evaluation of 1-alkyl-N-[2-ethyl-2-(4- fluorophenyl)butyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents
Watanuki, Susumu,Matsuura, Keisuke,Tomura, Yuichi,Okada, Minoru,Okazaki, Toshio,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
, p. 5628 - 5638 (2011/10/12)
We synthesized and evaluated inhibitory activity against T-type Ca 2+ channels for a series of 1-alkyl-N-[2-ethyl-2-(4-fluorophenyl) butyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that dialkyl substituents at the benzylic position play an important role in increasing inhibitory activity. Oral administration of N-[2-ethyl-2-(4-fluorophenyl)butyl]-1-(2-phenylethyl)piperidine-4-carboxamide (20d) lowered blood pressure in spontaneously hypertensive rats without inducing reflex tachycardia, which is often caused by traditional L-type Ca2+ channel blockers.
