title: Convenient synthesis, anti-inflammatory, analgesic and ulcerogenic activites of some new bis-hydrazones and pyrazole derivatives.
abstract: The reaction of acid hydrazides (1a-c) with 2-chloro-1-(4-chlorophenyl)ethanone (2a) or 2-bromo-1-(4-bromophenyl)ethanone (2b) afforded bis-hydrazones 6a-d, while the reaction of la-c with 2-oxo-N-arylpropanehydrazonoyl chlorides (3a,b) furnished N-(aryl)propanehydrazonoyl chlorides 8a-c. The reaction of the latter chlorides with sodium benzenesulfinate furnished sulfones 11a-c. On the other hand, treatment of benzothiazole-2-carbohydrazide (1c) with the appropriate ketones yielded the corresponding hydrazones 13a,b, while the reaction of 1c with 2-(ethoxymethylene)malononitrile (14) or with 2-[bis(methylthio)methylene]malononitrile (16) afforded pyrazole derivatives 15 and 17, respectively. In acute toxicity study, no mortalities were observed for the tested compounds. All the tested compounds showed significant anti-inflammatory activity, while some of them exhibited potent analgesic activity. In addition, all compounds exhibited lower ulcerogenic effects than the standard ketoprofen.
authors.affiliation: Applied Organic Chemistry Department, National Research Center, Dokki 12622, Cairo, Egypt. drnehalhamdy63@hotmail.com
authors.forename: Nehal A
authors.initials: NA
authors.lastname: Hamdy
authors.forename: Hatem A
authors.initials: HA
authors.lastname: Abdel-Aziz
authors.forename: Gehan M
authors.initials: GM
authors.lastname: Kamel
authors.forename: Issa M I
authors.initials: IM
authors.lastname: Fakhr
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D051379:Mice; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D006835:Hydrazones; D011720:Pyrazoles