The original synthesis of a CCR6 antagonist and subsequent enablement for kilogram manufacture is presented. Highlighted improvements made in the preparation for the scale-up campaign include (1) a re...

Amides of squaric acid are new drug candidates with activity against mycobacteria. Like the approved drug bedaquiline, these compounds achieve efficacy by inhibiting mycobacterial ATP synthase. Howeve...

A potent squaramide-based anion transporter was used to evaluate how vesicles prepared with tailored lipid compositions, which mimic organelle membranes, can impact transmembrane transport. Using HPTS...

A potent squaramide-based anion transporter was used to evaluate how vesicles prepared with tailored lipid compositions, which mimic organelle membranes, can impact transmembrane transport. Using…

Capillary-driven flow distributes reagents evenly

A potent squaramide-based anion transporter was used to evaluate how vesicles prepared with tailored lipid compositions, which mimic organelle membranes, can impact transmembrane transport. Using…

Read the full paper: Lysosome-Targeted Squaramide Anion Transporters

CCR6 is a chemokine receptor that mediates the migration of pathogenic inflammatory leukocytes to sites of inflammation in response to its ligand, CCL20. Herein we report the design of a potent CCR6 antagonist capable of inhibiting the chemotactic migration of CCR6+ T cells in vitro. Key to this finding was the discovery of a remarkable methyl substituent effect on antagonist potency. A 365-fold improvement in potency was observed for the cis-2-methylcyclohexanamine analogue compared to the unsubstituted cyclohexanamine derivative. Evidence generated through the characterization of conformationally restricted analogues supports the conclusion that the large potency enhancement is the result of the methyl substituent biasing the cyclohexane ring ground state conformation to favor that of the bound ligand and thus decreasing the ligand strain energy.

Capillary-driven flow distributes reagents evenly

CCR6 is a chemokine receptor that mediates the migration of pathogenic inflammatory leukocytes to sites of inflammation in response to its ligand, CCL20. Herein we report the design of a potent CCR6 antagonist capable of inhibiting the chemotactic migration of CCR6+ T cells in vitro. Key to this finding was the discovery of a remarkable methyl substituent effect on antagonist potency. A 365-fold improvement in potency was observed for the cis-2-methylcyclohexanamine analogue compared to the unsubstituted cyclohexanamine derivative. Evidence generated through the characterization of conformationally restricted analogues supports the conclusion that the large potency enhancement is the result of the methyl substituent biasing the cyclohexane ring ground state conformation to favor that of the bound ligand and thus decreasing the ligand strain energy.

Complexation of radiometals by chelators allows for convenient radiolabeling of molecules of interest for the preparation of radiopharmaceuticals. In the chelator family, triazacyclononane (TACN)-base...

3-[(Benzo-1,3-dioxol-5-yl)amino]-4-meth­oxy­cyclo­but-3-ene-1,2-dione forms concomitant polymorphs, namely, block-shaped crystals of a monoclinic form I (space group P21/c, Z = 8, Z′ = 2) and needle-shaped crystals of a triclinic form II (space group P\overline{1}, Z = 4, Z′ = 2), the latter of which exhibits twinning by pseudomerohedry.