Abstract:
:A series of 3,4-bis-chalcone-N-arylpyrazoles 3a-k was prepared from diacetyl pyrazoles 2a-e. The reaction of 2d and 2e with hydrazine hydrate gave pyrazolo[3,4-d]pyridazine derivatives 4a-b. Furthermore, the reaction of 2a-e with thiosemicarbazide afforded pyrazolo[3,4-d]pyridazine thiocyanate salts 5a-e. The synthesized compounds were subjected to in vivo anti-inflammatory and ulcerogenic activity measurements, in addition to determination of their in vitro COX selectivity, to give a full profile about their anti-inflammatory activities. Compounds 3c, 3f, 3i, and 3e showed significant anti-inflammatory activity among the synthesized compounds. Moreover, docking studies were performed to give an explanation for their anti-inflammatory activity through COX selectivity.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
El-Sabbagh OI,Mostafa S,Abdel-Aziz HA,Ibrahim HS,Elaasser MMdoi
10.1002/ardp.201300193subject
Has Abstractpub_date
2013-09-01 00:00:00pages
688-98issue
9eissn
0365-6233issn
1521-4184journal_volume
346pub_type
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