Palladium-catalyzed N-arylation of 2-aminobenzothiazole-4-carboxylates/carboxamides: facile synthesis of PARP14 inhibitors

We have developed a palladium-catalyzed N-arylation of the biologically interesting, but synthetically rather challenging 2-arylaminobenzothiazoles bearing multiple functionalities. This protocol was successfully used to readily synthesize our initial PARP14 inhibitor followed by a limited structural optimization. A more potent PARP14 inhibitor with an IC₅₀ value of 1.69 μM was identified, and the interaction was ascertained by the X-ray co-crystal structure of the catalytic domain of PARP14 in complex with compound 8.     

Jacobi elliptic function solutions to (1 + 1) dimensional nonlinear Schrödinger equation in management system

A new kind of solutions namely elliptic function solutions to the (1 + 1) dimensional nonlinear Schrödinger equation (NLSE) in dispersion, nonlinearity and gain management system are obtained. The solutions are the generalization of analytical solutions to one-dimensional NLSE. The properties of the amplitudes and the phases of the solutions are investigated.