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Wang W.-L.,Jiangnan University | Wang W.-L.,CAS Shanghai Institute of Materia Medica | Wang W.-L.,Jiangshu Alpha Biopharmaceuticals Inc. | Yang D.-L.,Jiangnan University | And 16 more authors.
Molecules | Year: 2014

A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.© 2014 by the authors licensee MDPI Basel Switzerland.

Wang W.-L.,Jiangnan University | Wang W.-L.,Jiangshu Alpha Biopharmaceuticals Inc. | Song L.-J.,Wuxi Institute of Technology | Chen X.,Jiangnan University | And 6 more authors.
Molecules | Year: 2013

The synthesis and structure-activity relationship (SAR) studies of praziquantel derivatives with activity against adult Schistosoma japonicum are described. Several of them showed better worm killing activity than praziquantel and could serve as leads for further optimization. © 2013 by the authors; licensee MDPI, Basel, Switzerland.

Wang W.,Jiangnan University | Wang W.,Jiangshu Alpha Biopharmaceuticals Inc. | Song L.,Jiangsu Institute of Parasitic Diseases | Wang G.,Jiangnan University | And 5 more authors.
Chinese Journal of Organic Chemistry | Year: 2013

Due to widespread and intensive use of antischistosomal drug, praziquantel (PZQ), there is serious concern that drug-resistant mutants of the parasite may emerge. To develop novel antischistosomal agents, a series of 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives were designed, synthesized, and evaluated for their antischistosomal activity against S. japonicum in vitro. The results indicated that compound 10 with chloroacetyl group showed better antischistosoaml activity than PZQ. © 2013 Chinese Chemical Society & SIOC, CAS.

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