Exploring positions 6 and 7 of a quinazoline-based scaffold leads to changes in selectivity and potency towards RIPK2/3 kinases

Publication date: 15 November 2023

Source: European Journal of Medicinal Chemistry, Volume 260

Author(s): Mbilo Misehe, Marika Matoušová, Alexandra Dvořáková, Kamil Hercík, Kryštof Škach, Dominika Chalupská, Milan Dejmek, Michal Šála, Miroslav Hájek, Evzen Boura, Helena Mertlíková-Kaiserová, Radim Nencka

Cantharidin analogue alleviates dextran sulfate sodium-induced colitis in mice by inhibiting the activation of NF-κB signaling

Publication date: 15 November 2023

Source: European Journal of Medicinal Chemistry, Volume 260

Author(s): Yihang Wu, Zixiu Liu, Zhenxiu He, Jumei Yi, Xingfang Qiao, Chunbin Tan, Yajing Xing, Yaobo Zeng, Dajian Yang, Junlin Yin, Baomin Fan, Guangzhi Zeng

Design of phenothiazine-based cationic amphiphilic derivatives incorporating arginine residues: Potential membrane-active broad-spectrum antimicrobials combating pathogenic bacteria in vitro and in vivo

Publication date: 15 November 2023

Source: European Journal of Medicinal Chemistry, Volume 260

Author(s): Qian Yu, Qiongna Cai, Wanxin Liang, Kewen Zhong, Jiayong Liu, Haizhou Li, Yongzhi Chen, Hongxia Li, Shanfang Fang, Rongcui Zhong, Shouping Liu, Shuimu Lin

Lead generation from <em>N</em>-[benzyl(4-phenylbutyl)carbamoyl]amino acid as a novel LPA<sub>1</sub> antagonist for the treatment of systemic sclerosis

Publication date: 15 November 2023

Source: European Journal of Medicinal Chemistry, Volume 260

Author(s): Yuki Kobayashi, Fumito Uneuchi, Takumi Naruse, Daisuke Matsuda, Lisa Okumura-Kitajima, Hiromitsu Kajiyama, Reiko Wada, Yuki Yonemoto, Koichiro Nakano, Hidetoh Toki, Shunsuke Kamigaso, Jyunya Yamagishi, Seiken Tokura, Hiroyuki Kakinuma, Shoichi Kuroda

Magic shotgun approach to anti-inflammatory pharmacotherapy: Synthesis of novel thienopyrimidine monomers/heterodimer as dual COX-2 and 15-LOX inhibitors endowed with potent antioxidant activity

Publication date: 15 November 2023

Source: European Journal of Medicinal Chemistry, Volume 260

Author(s): Sara Elsayed, Ahmed S. Abdelkhalek, Samar Rezq, Mansour E. Abu Kull, Damian G. Romero, Hend Kothayer

Design, synthesis and evaluation of 2-pyrimidinylindole derivatives as anti-obesity agents by regulating lipid metabolism

Publication date: 15 November 2023

Source: European Journal of Medicinal Chemistry, Volume 260

Author(s): Shi-Yao Guo, Li-Yuan Wei, Bing-Bing Song, Yu-Tao Hu, Zhi Jiang, Dan-Dan Zhao, Yao-Hao Xu, Yu-Wei Lin, Shu-Min Xu, Shuo-Bin Chen, Zhi-Shu Huang