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  • 1 Medical University of Łódź Department of Analytical Chemistry Muszyńskiego 1 90-151 Łódź Poland
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Quantitative structure-activity relationships (QSAR) between H 1 -histaminergic activity and chromatographic data have been investigated for derivatives of 2-[2-(phenylamino)thiazol-4-yl]ethanamine, 2-(2-benzyl-4-thiazolyl)ethanamine, 2-(2-benzhydrylthiazol-4-yl)ethanamine, 2-(1-piperazinyl)benzothiazole, and 2-(hexahydro-1 H -1,4-diazepin-1-yl)benzothiazole. TLC was performed on precoated silanized silica gel RP2 60F 254 plates impregnated with solutions of propionic acid, propionamide, and n -amylamine (used as amino acid analogs) and their mixtures, with two mobile phases — the systems were chosen as models of hH1R antagonistic interaction. Relationships between chromatographic and biological activity data were found by use of regression analysis. The correlations obtained for the thiazole and benzothiazole derivatives with H 1 -antihistamine activity (p A2 (H 1 )) represent their interaction with all the proposed biochromatographic models (S1–S4). Some of the correlation equations obtained can be used to predict the pharmacological activity of new drug candidates. Lipophilicity data were obtained for the compounds and used in QSAR assays. The log P values of particular compounds are an extremely important indicator of this kind of activity.

  • E. Traiffort, R. Leurs, J.M. Arrang, J. Tardivel-Lacombe, J. Diaz, J.-C. Schwartz , and M. Ruat , J. Neurochem. 62 (2) (1994) 507–518.

    Ruat M. , '' (1994 ) 62 J. Neurochem. : 507 -518.

  • R. Leurs, H. Van der Goot , and H. Timmerman , in: B. Testa (Ed.) Advances in Drug Research, Academic Press, London, 1991, Chap. 20, pp. 217–304.

    Timmerman H. , '', in Advances in Drug Research , (1991 ) -.

  • E. Traiffort, R. Leurs, J. Arrang, J. Tardivel-Lacombe, J. Diaz, J. Schwartz , and M. Ruat , J. Neurochem. 62 (1994) 507–518.

    Ruat M. , '' (1994 ) 62 J. Neurochem. : 507 -518.

  • M. Smit, H. Timmerman, J. Hijzelendoorn, H. Fukui , and R. Leurs , Br. J. Pharmacol. 117 (1996) 1071–1080.

    Leurs R. , '' (1996 ) 117 Br. J. Pharmacol. : 1071 -1080.

  • M. Smit, M. Hoffmann, H. Timmerman , and R. Leurs , Clin. Exp. Allergy Suppl. 3 (1999) 19–28.

    Leurs R. , '' (1999 ) 3 Clin. Exp. Allergy Suppl. : 19 -28.

  • G. Durant, C. Ganellin , and M. Parson , J. Med. Chem. 18 (1975) 905–909.

    Parson M. , '' (1975 ) 18 J. Med. Chem. : 905 -909.

  • S. Elz, K. Kramer, H. Pertz, H. Detert, A. der Laak, R. Kühne , and W. Schunack , J. Med. Chem. 43 (2000) 1071–1084.

    Schunack W. , '' (2000 ) 43 J. Med. Chem. : 1071 -1084.

  • A. Ter Laak, J. Venhorst, G. Donné-Op den Kelder , and H. Timmerman , J. Med. Chem. 38 (1995) 3351–3360.

    Timmerman H. , '' (1995 ) 38 J. Med. Chem. : 3351 -3360.

  • T. Takizawa, J. Matsumoto, T. Tohma, T. Kanke, Y. Wada, M. Nagao, N. Inagaki, H. Nagai, M.Q. Zhang , and H. Timmerman , Jpn J. Pharmacol. 86 (2001) 55–64.

    Timmerman H. , '' (2001 ) 86 Jpn J. Pharmacol. : 55 -64.

  • R. Kaliszan , Chemom. Intell. Lab. Systems 24 (1994) 89–97.

    Kaliszan R. , '' (1994 ) 24 Chemom. Intell. Lab. Systems : 89 -97.

  • R. Kaliszan, M. van Straten, M. Markuszewski, C. Cramers , and H. Claessens , J. Chromatogr. 855 (1999) 455–486.

    Claessens H. , '' (1999 ) 855 J. Chromatogr. : 455 -486.

  • R. Kaliszan, A. Nasal , and M. Turowski , J. Chromatogr. A 722 (1996) 25–32.

    Turowski M. , '' (1996 ) 722 J. Chromatogr. A : 25 -32.

  • T.H. Dzido , Modern TLC Chambers, in: Sz. Nyiredy (Ed.) Planar Chromatography, A Retrospective View for the Third Millennium, Springer, Budapest, 2001, pp. 68–87.

    Dzido T.H. , '', in Planar Chromatography, A Retrospective View for the Third Millennium , (2001 ) -.

  • E. Brzezińska , Acta Polon. Pharm. 53 (1996) 383–388.

    Brzezińska E. , '' (1996 ) 53 Acta Polon. Pharm. : 383 -388.

  • E. Brzezińska , Acta Polon. Pharm. 53 (1996) 389–392.

    Brzezińska E. , '' (1996 ) 53 Acta Polon. Pharm. : 389 -392.

  • E. Brzezińska, G. Kośka , and K. Walczyński , J. Chromatogr. A 1007 (2003) 145–155.

    Walczyński K. , '' (2003 ) 1007 J. Chromatogr. A : 145 -155.

  • E. Brzezińska, G. Kośka , and A. Klimczak , J. Chromatogr. A 1007 (2003) 157–164.

    Klimczak A. , '' (2003 ) 1007 J. Chromatogr. A : 157 -164.

  • I. de Esch, H. Timmerman, W. Menge , and P. Nederkoorn , Arch. Pharm. Pharm. Med. Chem. 333 (2000) 254–260.

    Nederkoorn P. , '' (2000 ) 333 Arch. Pharm. Pharm. Med. Chem. : 254 -260.

  • A. Windhorst, H. Timmerman, E. Worthington, G. Bijloo, P. Nederkoorn, W. Menge, R. Leurs , and J. Herscheid , J. Med. Chem. 43 (2000) 1754–1761.

    Herscheid J. , '' (2000 ) 43 J. Med. Chem. : 1754 -1761.

  • K. Walczyński, R. Guryn, O.P. Zuiderveld, M.Q. Zhang , and H. Timmerman , Il Farmaco 55 (2000) 569–574.

    Timmerman H. , '' (2000 ) 55 Il Farmaco : 569 -574.

  • K. Walczyński, H. Timmerman, O.P. Zuiderveld, M.Q. Zhang , and R. Glinka , Il Farmaco 54 (1999) 533–541.

    Glinka R. , '' (1999 ) 54 Il Farmaco : 533 -541.

  • K. Walczyński, R. Guryn, O.P. Zuiderveld, M.Q. Zhang , and H. Timmerman , Il Farmaco 54 (1999) 684–694.

    Timmerman H. , '' (1999 ) 54 Il Farmaco : 684 -694.

  • E.C. Bate-Smith and R.G. Westall , Biochim. Biophys. Acta 4 (1950) 427–440.

    Westall R.G. , '' (1950 ) 4 Biochim. Biophys. Acta : 427 -440.

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Journal of Planar Chromatography - Modern TLC
Language English
Size A4
Year of
Foundation
1988
Volumes
per Year
1
Issues
per Year
6
Founder Akadémiai Kiadó
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Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
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Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
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Chief Executive Officer, Akadémiai Kiadó
ISSN 0933-4173 (Print)
ISSN 1789-0993 (Online)

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