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

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

Sinteza i cAMP-ovisna inhibicija fosfodiesteraze novih derivata tiazolokinazolina

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 20.02.2019.
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 20.02.2019.];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
U radu je opisana sinteza serije 6,7,8,9-tetrahidro-5H-5-(2'-hidroksifenil)-2-(4'-supstituiranih benzilidin)tiazolo(2,3-b)kinazolin-3(2H)-ona (4a-j) i 6,7,8,9-tetrahidro-5H-5-(2'-hidroksifenil)-2-(4'-supstituiranih benzilidin)-3-(4-nitrofenilamino)tiazolokinazolina (5a-j) prema objavljenoj metodi te ispitano njihovo inhibitorno djelovanje na fosfodiesterazu. Svi testirani spojevi pokazuju dobro djelovanje. Proučavan je i odnos strukture i djelovanja. U obje serije spojeva, elektron-odvlačeći supstituenti doprinose jačem djelovanju. Među ispitivanim spojevima pronađeno je da 6,7,8,9-tetrahidro-5H-5-(2'-hidroksifenil)-2-(4'-fluorobenzilidine)-3-(4-nitrofenilamino)tiazolokinazolin (5e), 6,7,8,9-tetrahidro-5H-5-(2'-hidroksifenil)-2-(4'-nitrobenzilidine)-3-(4-nitrofenilamino)tiazolokinazolin (5j) i 6,7,8,9-tetrahidro-5H-5-(2'-hidroksifenil)-2-(4'-klorobenzilidin)-3-(4-nitrofenilamino)tiazolokinazolin (5f) imaju jače djelovanje od teofilina (IC50 u mmol L–1 1,34 ± 0,09 za 5f, 1,44 ± 0,02 za 5e, 1,52 ± 0,05 za 5j nasuprot 1,72 ± 0,09 za teofilin).

Ključne riječi
tiazolokinazolin; benzilidinetiazolokinazolin; nitrofenilaminotiazolokinazolin; inhibicija fosfodiesteraze; SAR

Hrčak ID: 63380

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

[engleski]

Posjeta: 522 *