Chunjian Liu, Wei Wang, Jianxin Feng, Brett Beno, Thiruvenkadam Raja, Jacob Swidorski, Raju K V L P Manepalli, Muthalagu Vetrichelvan, Prasada Rao Jalagam, Satheesh K Nair, Anuradha Gupta, Manoranjan Panda, Kaushik Ghosh, Jinal Kaushikkumar Shukla, Harinath Sale, Devang Shah, Shashyendra Singh Gautam, Dipal Patel, Arvind Mathur, Bruce A Ellsworth, Dong Cheng, Alicia Regueiro-Ren
As a result of our continued efforts to pursue Gal-3 inhibitors that could be used to fully evaluate the potential of Gal-3 as a therapeutic target, two novel series of benzothiazole derived monosaccharides as potent (against both human and mouse Gal-3) and orally bioavailable Gal-3 inhibitors, represented by 4 and 5, respectively, were identified. These discoveries were made based on proposals that the benzothiazole sulfur atom could interact with the carbonyl oxygen of G182/G196 in h/mGal-3, and that the anomeric triazole moiety could be modified into an N-methyl carboxamide functionality...
March 1, 2024: Bioorganic & Medicinal Chemistry