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Synthesis and Myorelaxant activity of fused 1,4-Dihydropyridines on isolated rabbit gastric fundus


Şafak, Cihat; Gündüz, Miyase Gözde; İlhan, Sevil Özger; Şimşek, Rahime; İşli, Fatma; Yıldırım, Şeniz; Fincan, Gökçe Sevim Öztürk; Sarıoğlu, Yusuf; Linden, Anthony (2012). Synthesis and Myorelaxant activity of fused 1,4-Dihydropyridines on isolated rabbit gastric fundus. Drug Development Research, 73(6):332-342.

Abstract

In the present study, 25 novel condensed 1,4-dihydropyridine (DHP) derivatives bearing cyclopentane, cyclohexane, or tetrahydrothiopene ring with a bulky and lipophilic moiety (3-pyridylmethyl) in the ester group were synthesized via a modified Hantzsch reaction, and their calcium channel modulator activities were assayed on isolated rabbit gastric fundus smooth muscle strips. To evaluate the myorelaxant effects of the compounds, the maximum relaxant response (Emax) and pD 2 values were calculated. The results indicated that all compounds produced concentration-dependent relaxation and the introduction of five- or six-membered rings to the DHP nucleus and 3-pyridiylmethyl moiety to the ester group led to potent calcium antagonists.

In the present study, 25 novel condensed 1,4-dihydropyridine (DHP) derivatives bearing cyclopentane, cyclohexane, or tetrahydrothiopene ring with a bulky and lipophilic moiety (3-pyridylmethyl) in the ester group were synthesized via a modified Hantzsch reaction, and their calcium channel modulator activities were assayed on isolated rabbit gastric fundus smooth muscle strips. To evaluate the myorelaxant effects of the compounds, the maximum relaxant response (Emax) and pD 2 values were calculated. The results indicated that all compounds produced concentration-dependent relaxation and the introduction of five- or six-membered rings to the DHP nucleus and 3-pyridiylmethyl moiety to the ester group led to potent calcium antagonists.

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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Language:English
Date:2012
Deposited On:19 Oct 2012 11:39
Last Modified:05 Apr 2016 16:00
Publisher:Wiley-Blackwell
ISSN:0272-4391
Funders:Hacettepe University Scientific Research and Development Office (Project No: 5222)
Publisher DOI:https://doi.org/10.1002/ddr.21024
Permanent URL: https://doi.org/10.5167/uzh-65497

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