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In this study, we have explored the prevention of gastric side effects such as gastric lesions and bleeding while maintaining the high analgesic and anti-inflammatory activities by the derivatization of the carboxylate moiety into amides in [5-chloro-6-(2-chloro/fluorobenzoyl)-2-benzoxazolinone-3-yl]acetic acids. We have tested the analgesic and anti-inflammatory activities of the synthesized compounds in vivo by using p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. Compounds 3a, 3d, 3e, 3j and 3k potent analgesic and anti-inflammatory activities without gastric lesions in the tested animals. Therefore, conversion of the carboxylate moiety into certain amide derivatives generated potent analgesic and anti-inflammatory compounds while eliminating the gastrointestinal side effects. Cyclooxygenase (COX)-selectivity of the active compounds was also investigated by using in vitro human whole blood assay. Compounds 3a, 3e, 3h and 3k selective inhibition of COX-2 to some extent although the inhibitory activity was not very potent.
A series of 6-substituted-3(2H)-pyridazi-none derivatives were synthesized and evaluated for analgesic and anti-inflammatory activities. The structures of these new pyridazinone derivatives were confirmed by their IR, 1H-NMR spectra and elementary analysis. Analgesic and anti-inflammatory activities of the title compounds have been evaluated. Four of the ten tested compounds possessed significant analgesic effects in the phenylbenzoquinone-in-duced writhing test (PBQ test). The most active derivatives 8a, 8b, 8d, 8e were void of gastric ulcerogenic effect or acute toxicity at the maximal dose (200 mg/kg p.o.). In the carrageenan-induced paw edema model, compound 8d (6- [ 4- (2-fluoro-phenyl) piperazin-1 -yl] - 3 (2H) -pyridazinone) showed anti-inflammatory activity similar to that of the standard drug Indometacin (CAS 53-86-1). A significant dependence of the anti-inflammatory effect on the substituents was observed. The pharmacological study of these compounds confirms that modification of the chemical group at position 6 of the 3(2H)-pyridazinone ring influences analgesic and anti-inflammatory activities.
A series of 6-(a-amino-4-chlorobenzyl)-thiazolo[3,2-b]-1, 2, 4-triazol-5-ols (2a-j) were synthesized from 6-(4-chlorobenzyl idene) thiazolo [3,2-b]-1, 2, 4-triazolo-5(6H)-one (2) by applying Michael addition reaction. All the compounds were characterized by their melting points, ele mentary analysis, IR and 1H-NMR spectra and screened for their anti-inflamma tory and analgesic activities. Among the derivatives compound 2i bearing 4-(4-acetylphenyl)piperazine showed the highest and dose-dependent analgesic and anti-inflammatory activity without inducing any gastric lesion.
A field survey of traditional medicine in Turkey, specifically medicinal plants in East-Anatolia (Van-Bitlis Provinces), is discussed. Interviews with inhabitants, elder people, traditional practitioners and eyh (semi-religious persons) were conducted to determine the vernacular names of plants used as medicine. The plants were all taxonomically identified, and their medicinal uses and administration routes are listed. The use of medicinal plants is usually the first choice of treatment among the rural people in this region.
Abstract In this study, a series of (7‐acyl‐5‐chloro‐2‐oxo‐3 H ‐benzoxazol‐3‐yl)alkanoic acid derivatives were synthesized and evaluated for their analgesic and anti‐inflammatory activities by using the p‐benzoquinone‐induced writhing test and the carrageenan hind paw edema model, respectively. Acetic acid‐induced peritoneal capillary permeability test and serotonin‐induced hind paw edema test were also employed for the most active compounds. The test results indicated that (7‐acyl‐2‐oxo‐3 H ‐benzoxazol‐3‐yl)alkanoic acids (Compounds 6 a—c , 8 a—c , 10 a—c ) were equally or more potent analgesic and anti‐inflammatory agents than aspirin and indomethacin respectively. The compounds 8a and 8c , but not 8b have the longest carbon chain on alkanoic acid moiety did not induce gastric lesion in mice.
The root of Paeonia daurica was investigated for its antiinflammatory activity with the carrageenan-induced hind paw edema method in mice. For the determination of active antiinflammaroty principle, the EtOH extract of the root was subjected to a series of successive fractionations, leading to paeonoside and paeonol as the active principles.
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