Author(s):
Hiroyuki Ushio, Seigo Ishibuchi, Kunitomo Adachi, Kouichi Oshita and Kenji ChibaPages 292-296 (5)
Abstract:
Through the optimization of the active metabolite 2 of the piperidine derivative 1, we discovered a potent new drug candidate for the treatment of RA, Y-320 that inhibits T cell activation induced by IL-15 and shows a therapeutic...
Wednesday, August 17, 2016
Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
Author(s):
Kuiying Xu, Marie Wetzel, Rolf W. Hartmann and Sandrine Marchais-OberwinklerPages 406-421 (16)
Abstract:
17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the...
Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
Author(s):
Muhammad Yar, Marek Bajda, Rana Atif Mehmood, Lala Rukh Sidra, Nisar Ullah, Lubna Shahzadi, Muhammad Ashraf, Tayaba Ismail, Sohail Anjum Shahzad, Zulfiqar Ali Khan, Syed Ali Raza Naqvi and Nasir MahmoodPages 331-338 (8)
Abstract:
Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of...
4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls
Author(s):
Maria Antonietta Dettori, Davide Fabbri, Marina Pisano, Carla Rozzo, Giuseppe Palmieri, Alessandro Dessi, Roberto Dallocchio and Giovanna DeloguPages 131-139 (9)
Abstract:
A small collection of eugenol- and curcumin-analog hydroxylated biphenyls was prepared by...
Potent and Orally Bioavailable Antiplatelet Agent, PLD-301, with the Potential of Overcoming Clopidogrel Resistance
Author(s):
Jingyu Chen and Michael Zhiyan WangPages 250-254 (5)
Abstract:
PLD-301, a phosphate prodrug of clopidogrel thiolactone discovered by Prelude Pharmaceuticals with the aim to overcome clopidogrel resistance, was evaluated for its in vivo inhibitory effect on ADP-induced...
