Institute of Organic Chemistry and Biochemistry of the CAS

Partnership with Alzheon to develop first Alzheimer’s diagnostic assay for measuring neurotoxic…

6 May 2021

IOCB Prague entered into a collaboration and license agreement with Alzheon, Inc., a clinical-stage biopharmaceutical company focused on developing new medicines for patients suffering from Alzheimer’s disease (AD) and other…

New fund supports collaboration between researchers from the Czech Republic and MIT

27 April 2021

The establishment of collaboration between researchers from the Czech Republic and world-renowned Massachusetts Institute of Technology (MIT) is being made easier thanks to a new program called the MIT-Czech Republic Seed Fund, a joint…

Junior Group Leader position in organic synthesis – Call for applications extended

30 April 2021

IOCB Prague invites applications for a Junior Group Leader position in synthetic organic chemistry with a strong emphasis on synthetic approaches to complex target molecules at…

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Junior Group Leader position in organic synthesis

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Nucleotide analogues containing a pyrrolidine, piperidine or piperazine ring: Synthesis and evaluation of inhibition of plasmodial and human 6-oxopurine phosphoribosyltransferases and in vitro antimalarial activity

J. Frydrych D. T. Keough M. Chavchich J. Travis M. Dračínský M. D. Edstein L. W. Guddat D. Hocková Z. Janeba

European Journal of Medicinal Chemistry 219: 113416 (2021)

Parasites of the Plasmodium genus are unable to produce purine nucleotides de novo and depend completely on the salvage pathway. This fact makes plasmodial hypoxanthine-guanine-(xanthine) phosphoribosyltransferase [HG(X)PRT] a valuable target for development of antimalarial agents. A series of nucleotide analogues was designed, synthesized and evaluated as potential inhibitors of Plasmodium falciparum HGXPRT, P. vivax HGPRT and human HGPRT. These novel nucleoside phosphonates have a pyrrolidine, piperidine or piperazine ring incorporated into the linker connecting the purine base to a phosphonate group(s) and exhibited a broad range of K_i values between 0.15 and 72 μM. The corresponding phosphoramidate prodrugs, able to cross cell membranes, have been synthesized and evaluated in a P. falciparum infected human erythrocyte assay. Of the eight prodrugs evaluated seven exhibited in vitro antimalarial activity with IC₅₀values within the range of 2.5–12.1 μM. The bis-phosphoramidate…

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Structural determinants for subnanomolar inhibition of the secreted aspartic protease Sapp1p from Candida parapsilosis

J. Dostál J. Brynda L. Vaňková S. R. Zia O. Heidingsfeld M. Lepšík

Journal of Enzyme Inhibition and Medicinal Chemistry 36 (1): 914-921 (2021)

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Tuning the P–C dative/covalent bond formation in R₃P–C₆₀ complexes by changing the R group

R. Lo D. Manna P. Hobza

Chemical Communications 57 (21): 3363-3366 (2021)

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α,γ-Dioxygenated amides via tandem Brook rearrangement/radical oxygenation reactions and their application to syntheses of γ-lactams

M. Klychnikov R. Pohl I. Císařová U. Jahn

Beilstein Journal of Organic Chemistry 17: 688–704 (2021)

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Institute of Organic Chemistry
and Biochemistry of the CAS

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