Cover image for Vol. 12 Issue 20

Editorial Board Chairs: Karl-Heinz Altmann, Antonello Mai, Rainer Metternich. Editor: David Peralta

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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October 04, 2017

Call for Nominations: 2018 IUPAC–Richter Prize

Call for Nominations: 2018 IUPAC–Richter PrizeThe 2018 IUPAC–Richter Prize will be presented at the 36th National Medicinal Chemistry Symposium (ACS-MEDI NMCS: April 29th to May 2nd, 2018 in Nashville, Tennessee, USA) as well as the XXV International Symposium on Medicinal Chemistry (EFMC-ISMC: September 2nd–6th, 2018 in Ljubljana, Slovenia), where the recipient will also give plenary lectures on the subject of his or her research.

The prize, accompanied by US$10,000, is to be awarded to an internationally recognized scientist, preferably a medicinal chemist, whose activities have made an outstanding contribution to the field of medicinal chemistry.

See the IUPAC website for detailed information, along with an electronic nomination form. The submission deadline for awardee nominations is December 15th, 2017. We hope to see you at these conferences next year!

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    Prof. Jon E. Hawkinson, Dr. Rondedrick Sinville, Deepti Mudaliar, Dr. Jagathpala Shetty, Dr. Timothy Ward, Prof. John C. Herr and Prof. Gunda I. Georg

    Version of Record online: 20 OCT 2017 | DOI: 10.1002/cmdc.201700503

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    Sperm beware! Testis-specific serine/threonine kinase 2 (TSSK2) plays an important role in spermiogenesis and fertilization. A robust mobility shift assay high-throughput screen identified a pyrrolopyrimidine and a pyrimidine series of TSSK2 ATP site inhibitors. A pyrimidine analogue lacking metabolic liability was identified as a potent dual inhibitor of TSSK2 and TSSK1, demonstrating the potential to identify inhibitors of multiple TSSKs for male contraception.

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    Martina Bigatti, Dr. Alberto Dal Corso, Sara Vanetti, Samuele Cazzamalli, Dr. Ulrike Rieder, Dr. Jörg Scheuermann, Prof. Dr. Dario Neri and Dr. Filippo Sladojevich

    Version of Record online: 20 OCT 2017 | DOI: 10.1002/cmdc.201700569

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    The missing link: The screening of encoded self-assembling chemical libraries allows the identification of fragment pairs that bind to adjacent pockets on target proteins of interest. For practical application, these ligand pairs must be linked into discrete organic molecules, devoid of any nucleic acid component. Here we describe the discovery of a synergistic binding pair for acid alpha-1 glycoprotein and a chemical strategy for the identification of optimal linkers, connecting the two fragments.

  3. Synthesis, determination of the lipophilicity, anticonvulsant activity and preliminary safety of new derivatives of N-[(4-arylpiperazin-1-yl)-alkyl]-pyrrolidine-2,5-dione

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    Version of Record online: 18 OCT 2017 | DOI: 10.1002/cmdc.201700512

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    Let there be light: We designed a photo-sensing DNA microcapsule. This DNA microcapsule was formed by assembly of the Y-shaped DNA-building blocks in which azobenzenes were located within the connecting regions. Upon irradiation with light, the microcapsules were found to rapidly collapse, thus releasing doped compounds through the cis isomerization of azobenzene units positioned at connecting regions between the building blocks.

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