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Acta Pharmaceutica, Vol. 58 No. 4, 2008.

Izvorni znanstveni članak
https://doi.org/10.2478/v10007-008-0024-1

Sinteza i vrednovanje analgetskog, protuupalnog i ulcerogenog djelovanja nekih triazolo- i 2-pirazolil-pirido[2,3-d]-pirimidina

HEND N. HAFEZ ; National Research Centre, Photochemistry Department (Heterocyclic Unit), Dokki, 12622 Cairo, Egypt
HEBAT-ALLAH S. ABBAS ; National Research Centre, Photochemistry Department (Heterocyclic Unit), Dokki, 12622 Cairo, Egypt
ABDEL-RAHMAN B. A. EL-GAZZAR ; National Research Centre, Photochemistry Department (Heterocyclic Unit), Dokki, 12622 Cairo, Egypt

Puni tekst: engleski, pdf (131 KB) str. 359-378 preuzimanja: 689* citiraj
APA 6th Edition
HAFEZ, H.N., ABBAS, H.S. i EL-GAZZAR, A.B.A. (2008). Synthesis and evaluation of analgesic, anti-inflammatory and ulcerogenic activities of some triazolo- and 2-pyrazolyl-pyrido[2,3-d]-pyrimidines. Acta Pharmaceutica, 58 (4), 359-378. https://doi.org/10.2478/v10007-008-0024-1
MLA 8th Edition
HAFEZ, HEND N., et al. "Synthesis and evaluation of analgesic, anti-inflammatory and ulcerogenic activities of some triazolo- and 2-pyrazolyl-pyrido[2,3-d]-pyrimidines." Acta Pharmaceutica, vol. 58, br. 4, 2008, str. 359-378. https://doi.org/10.2478/v10007-008-0024-1. Citirano 22.05.2019.
Chicago 17th Edition
HAFEZ, HEND N., HEBAT-ALLAH S. ABBAS i ABDEL-RAHMAN B. A. EL-GAZZAR. "Synthesis and evaluation of analgesic, anti-inflammatory and ulcerogenic activities of some triazolo- and 2-pyrazolyl-pyrido[2,3-d]-pyrimidines." Acta Pharmaceutica 58, br. 4 (2008): 359-378. https://doi.org/10.2478/v10007-008-0024-1
Harvard
HAFEZ, H.N., ABBAS, H.S., i EL-GAZZAR, A.B.A. (2008). 'Synthesis and evaluation of analgesic, anti-inflammatory and ulcerogenic activities of some triazolo- and 2-pyrazolyl-pyrido[2,3-d]-pyrimidines', Acta Pharmaceutica, 58(4), str. 359-378. doi: https://doi.org/10.2478/v10007-008-0024-1
Vancouver
HAFEZ HN, ABBAS HS, EL-GAZZAR ABA. Synthesis and evaluation of analgesic, anti-inflammatory and ulcerogenic activities of some triazolo- and 2-pyrazolyl-pyrido[2,3-d]-pyrimidines. Acta Pharm. [Internet]. 2008 [pristupljeno 22.05.2019.];58(4):359-378. doi: https://doi.org/10.2478/v10007-008-0024-1
IEEE
H.N. HAFEZ, H.S. ABBAS i A.B.A. EL-GAZZAR, "Synthesis and evaluation of analgesic, anti-inflammatory and ulcerogenic activities of some triazolo- and 2-pyrazolyl-pyrido[2,3-d]-pyrimidines", Acta Pharmaceutica, vol.58, br. 4, str. 359-378, 2008. [Online]. doi: https://doi.org/10.2478/v10007-008-0024-1

Sažetak
U radu je opisana sinteza serije 2-hidrazino-7,8-dihidro-6H-ciklopenta[5,6]pirido[2,3-d]pirimidina i njihovih 1,7,8,9-tetrahidrociklopenta[5,6]pirido[2,3-d][1,2,4]triazolo[4,3-a]pirimidinskih, 1,7,8,9-tetrahidrociklopenta[5,6]pirido[2,3-d][1,2,3,4]tetrazolo[4,5-a]pirimidinskih, 8,9-dihidro-7H-ciklopenta[5,6]pirido[2,3-d]imidazolo[1,2-a]pirimidinskih i 2-(pirazol-1-il)-7,8-dihidro-6H-ciklopenta[5,6]pirido[2,3-d]pirimidinskih derivata s potencijalnim protuupalnim i analgetskim te manjim ulcerogenim djelovanjem. Spojevima s izraženim protuupalnim djelovanjem testirano je analgetsko i ulcerogeno djelovanje. Spojevi 3-amino-6-(4-aril)-9-(4-arilmetilen)-ciklopenta[5,6]pirido[2,3-d][1,2,4]triazolo[4,3-a]pirimidin-5(H)-on (4c), 1-amino-2-metil-6-(4-aril)-9-(4-aril-metilen)-ciklopenta[5,6]pirido[2,3-d]imidazolo[1,2-a]pirimidin-5(H)-on (6a), 2-amino-5-(4-aril)-8-(4-arilmetilen)-ciklopenta[5,6]pirido[2,3-d]pirimidin-4(H)-on (9), 2-(3-amino-5-hidroksipirazol-1-il)-5-(4-aril)-8-(4-arilmetilen)- ciklopenta[5,6]-pirido[2,3-d]pirimidin-4(H)-on (10a) i 3-tiokso-6-(4-aril)-9-(4-arilmetilen)-ciklopenta[5,6]pirido[2,3-d][1,2,4]triazolo[4,3-a]pirimidin-5(H)-on (13) pokazali su značajno analgetsko djelovanje. Spoj 2-(3-amino-5-hidroksipirazol-1-il)-5-(4-aril)-8-(4-arilmetilen)-ciklopenta[5,6]pirido[2,3-d]pirimidin-4(H)-on (10a) je vodeći spoj s jačim protuupalnim djelovanjem (82,8%) od ibuprofena (79,5%), a slabijim ulcerogenim djelovanjem.

Ključne riječi
pirido[2,3-d]pirimidini; [1,2,4]triazol anelacija; protuupalno djelovanje; analgetsko djelovanje

Hrčak ID: 26776

URI
https://hrcak.srce.hr/26776

[engleski]

Posjeta: 977 *