Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

Zapytanie: PARUSZEWSKI
Liczba odnalezionych rekordów: 2



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Tytuł oryginału: New renin inhibitors with pseudodipeptidic units in P1-P1' and P2'-P3' positions.
Autorzy: Paruszewski Ryszard, Jaworski Paweł, Winiecka Iwona, Tautt Jadwiga, Dudkiewicz Jadwiga
Źródło: Chem. Pharm. Bull. (Tokyo) 2002: 50 (6) s.850-853, tab., bibliogr. 21 poz.
Sygnatura GBL: 304,601

Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • praca opublikowana za granicą
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • in vitro

    Streszczenie angielskie: A series of four new potential renin inhibitors has been synthesized. The structure of the compounds was designed in such a way as to produce agents resistant to enzymatic degradation, metabolically stable, possibly potent and with improved oral absorption. All positions of the 8-13 fragment of the human angiotensinogen were occupied by unnatural units (two unnatural amino acids in position P3 and P2 and two pseudodipeptides in positions P1-P1, and P2-P3,). Both N- and C-terminal functions of the inhibitors were blocked with tert-Boc and ethyl ester groups. Their hydrophobicity evaluated as a log P value, calculated by a computer method, was 6.57 and 6.08 respectively. All peptides were obtained by the carbodiimide method in solution and purified by chromatography on the SiO2 column. Their resistance to enzymatic degradation was assayed by determination of stability against chymotrypsin activity. The potency was measured in vitro by a spectrofluorimetric method (assay of Leu-Val-Tyr-Ser released from the N-acetyltreadecapeptide substrate by renin in the presence of the inhibitor). All inhibitors were stable to chymotrypsin. Their IC50 (M/I) values were: 9.6 x 10**-4 (12), 1.6 x 10**-5 (17), 1.0 X 10**-5 (22) and 1.0 x 10**-5 (23) respectively.

    2/2

    Tytuł oryginału: Analytical studies on two amino acid derivatives of anticonvulsant activity.
    Autorzy: Pirianowicz-Chaber Elżbieta, Paruszewski Ryszard
    Źródło: Acta Pol. Pharm. 2002: 59 (4) s.239-241, il., tab., bibliogr. 5 poz.
    Sygnatura GBL: 301,378

    Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • tytuł obcojęzyczny

    Streszczenie angielskie: Qualitative and quantitative methods of analysis of two new amino acid derivatives, potential anticolvulsants of low neurotoxicity: N-acetyl-ç-aminobutyric acid benzylamide (1) and N-methyl-ç-aminobutyric acid benzylamide (2) were developed. Qualitative analysis includes characteristic colour reactions, chromatographic (TLC) investigations, IR and UV spectra interpretation and quantitative analysis involves spectrophotometric, chromatographic (HPLC), acidimetric and argentometric methods.

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