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Acta Pharmaceutica, Vol. 61 No. 1, 2011.

Kratko priopćenje
https://doi.org/10.2478/v10007-011-0009-3

Synthesis and cAMP-dependent phosphodiesterase inhibition activity of novel thiazoloquinazoline derivatives

THEIVENDREN PANNEER SELVAM   ORCID icon orcid.org/0000-0002-8197-4688 ; Department of Biotechnology, Acharya Nagarjuna University, Guntur-522510, India
PALANIRAJAN VIJAYARAJ KUMAR ; Department of Pharmacy, College Sadaya, International University, Jalan Menara Gading 56000 Cheras, Kuala Lumpur, Malaysia

Puni tekst: engleski, pdf (93 KB) str. 103-113 preuzimanja: 296* citiraj
APA 6th Edition
SELVAM, T.P. i KUMAR, P.V. (2011). Synthesis and cAMP-dependent phosphodiesterase inhibition activity of novel thiazoloquinazoline derivatives. Acta Pharmaceutica, 61 (1), 103-113. https://doi.org/10.2478/v10007-011-0009-3
MLA 8th Edition
SELVAM, THEIVENDREN PANNEER i PALANIRAJAN VIJAYARAJ KUMAR. "Synthesis and cAMP-dependent phosphodiesterase inhibition activity of novel thiazoloquinazoline derivatives." Acta Pharmaceutica, vol. 61, br. 1, 2011, str. 103-113. https://doi.org/10.2478/v10007-011-0009-3. Citirano 17.02.2019.
Chicago 17th Edition
SELVAM, THEIVENDREN PANNEER i PALANIRAJAN VIJAYARAJ KUMAR. "Synthesis and cAMP-dependent phosphodiesterase inhibition activity of novel thiazoloquinazoline derivatives." Acta Pharmaceutica 61, br. 1 (2011): 103-113. https://doi.org/10.2478/v10007-011-0009-3
Harvard
SELVAM, T.P., i KUMAR, P.V. (2011). 'Synthesis and cAMP-dependent phosphodiesterase inhibition activity of novel thiazoloquinazoline derivatives', Acta Pharmaceutica, 61(1), str. 103-113. doi: https://doi.org/10.2478/v10007-011-0009-3
Vancouver
SELVAM TP, KUMAR PV. Synthesis and cAMP-dependent phosphodiesterase inhibition activity of novel thiazoloquinazoline derivatives. Acta Pharm. [Internet]. 2011 [pristupljeno 17.02.2019.];61(1):103-113. doi: https://doi.org/10.2478/v10007-011-0009-3
IEEE
T.P. SELVAM i P.V. KUMAR, "Synthesis and cAMP-dependent phosphodiesterase inhibition activity of novel thiazoloquinazoline derivatives", Acta Pharmaceutica, vol.61, br. 1, str. 103-113, 2011. [Online]. doi: https://doi.org/10.2478/v10007-011-0009-3

Sažetak
The series of 6,7,8,9-tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(4'-substituted benzylidine) thiazolo(2,3-b)quinazolin-3(2H)-ones (4a-j) and 6,7,8,9-tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(4'-substituted benzylidine)-3-(4-nitrophenylamino)thiazoloquinazolines (5a-j) were synthesized by the reported method and evaluated for their phosphodiesterase inhibitory activity. All test compounds exhibited good activity. The structure-activity relationships were also studied. In both series of compounds, electron-withdrawing substitutions showed higher activity. Among the tested compounds, 6,7,8,9-tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(4'-fluorobenzylidine)-3-(4-nitrophenylamino)thiazoloquinazoline (5e), 6,7,8,9-tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(4'-nitrobenzylidine)-3-(4-nitrophenylamino)thiazoloquinazoline (5j) and 6,7,8,9-tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(4'-chlorobenzylidine)-3-(4-nitrophenylamino)thiazoloquinazoline (5f) were found to be more potent than theophylline (IC50 in mmol L–1 of 1.34 ± 0.09 for 5f, 1.44 ± 0.02 for 5e, 1.52 ± 0.05 for 5j vs. 1.72 ± 0.09 for theophylline).

Ključne riječi
thiazoloquinazoline; benzylidinethiazoloquinazoline; nitrophenylaminothiazolo quinazoline; phosphodiesterase inhibition; SAR

Hrčak ID: 63380

URI
https://hrcak.srce.hr/63380

[hrvatski]

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