- 6-Benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones substituted with ibuprofen: Synthesis, characterization and evaluation of anti-inflammatory activity
-
In this study, the synthesis of 3-[1-(4-(2-methylpropyl)phenyl)ethyl]- 1,2,4-triazole-5-thione (2) and its condensed derivatives 6- benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones (2a-u) are described. The structures of the compounds were elucidated by spectral and elemental analysis. In the pharmacological studies, anti-inflammatory activities of these compounds have been screened. Among the compounds examined, the compounds 2 and 2g possessed the most prominent and consistent activity. In gastric ulceration studies the synthesized compounds were generally found to be safe at a 200 mg/kg dose level. (C) 2000 Edition scientifique et medicales Elsevier SAS.
- Tozkoparan, Birsen,Goekhan, Nesrin,Aktay, Goeknur,Yesilada, Erdem,Ertan, Mevluet
-
-
Read Online
- Identification of an isoform catalyzing the CoA conjugation of nonsteroidal anti-inflammatory drugs and the evaluation of the expression levels of acyl-CoA synthetases in the human liver
-
Nonsteroidal anti-inflammatory drugs (NSAIDs) containing carboxylic acid are conjugated with coenzyme A (CoA) or glucuronic acid in the body. It has been suggested that these conjugates are associated with toxicities, such as liver injury and anaphylaxis,
- Hashizume, Hiroki,Fukami, Tatsuki,Mishima, Kanji,Arakawa, Hiroshi,Mishiro, Kenji,Zhang, Yongjie,Nakano, Masataka,Nakajima, Miki
-
-
Read Online
- PROGRAMMABLE DENDRITIC DRUGS
-
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, L, L1, L2, L3/sup
- -
-
Page/Page column 103
(2019/04/27)
-
- PROGRAMMABLE POLYMERIC DRUGS
-
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, L, L1, L2, L3/su
- -
-
Page/Page column 132
(2019/04/27)
-
- PROGRAMMABLE POLYMERIC DRUGS
-
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, L, L1, L2, L3, L4, M, m and n are as defined herein. Methods associated w
- -
-
Page/Page column 72
(2019/06/09)
-
- POLYMERS WITH RIGID SPACING GROUPS COMPRISING BIOLOGICALLY ACTIVE COMPOUNDS
-
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein A, R1, R2, R3, R4, R5, L, L1
- -
-
Page/Page column 76; 77
(2019/07/30)
-
- PHOSPHOALKYL POLYMERS COMPRISING BIOLOGICALLY ACTIVE COMPOUNDS
-
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, L, L1/sup
- -
-
Page/Page column 113
(2019/07/30)
-
- Design and Synthesis of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Treatment of Rheumatoid Arthritis
-
We report the synthesis of a series of hybrid compounds incorporating 6- and 7-substituted coumarins (carbonic anhydrase, CA inhibitors) derivatized with clinically used NSAIDs (indomethacin, sulindac, ketoprofen, ibuprofen, diclofenac, ketorolac, etc., cyclooxygenase inhibitors) as agents for the management of rheumatoid arthritis (RA). Most compounds were effective in inhibiting the RA overexpressed hCA IX and XII, with KI values in the low nanomolar-subnanomolar ranges. The antihyperalgesic activity of such compounds was assessed by means of the paw-pressure and incapacitance tests using an in vivo RA model. Among all tested compounds, the 7-coumarine hybrid with ibuprofen showed potent and persistent antihyperalgesic effect up to 60 min after administration.
- Bua, Silvia,Di Cesare Mannelli, Lorenzo,Vullo, Daniela,Ghelardini, Carla,Bartolucci, Gianluca,Scozzafava, Andrea,Supuran, Claudiu T.,Carta, Fabrizio
-
p. 1159 - 1170
(2017/02/19)
-
- Synthesis and evaluation of anti-inflammatory, analgesic, ulcerogenicity and nitric oxide-releasing studies of novel ibuprofen analogs as nonulcerogenic derivatives
-
Since the last 41 years, Ibuprofen has been one of the most widely used Non-Steroidal Anti-Inflammatory Drug (NSAID) due to its anti-inflammatory actions. As all the NSAIDs are suffering from the deadlier GI toxicities, Ibuprofen also is no exception to these toxicities. The free -COOH group is thought to be responsible for the Gastrointestinal (GI) tract toxicity associated with all the traditional NSAIDs. Therefore, the main aim of this study was to develop new chemical entities as potential anti-inflammatory agents with less GI toxicities. In this article, synthesis of a series of Hybrid molecules containing important pharmacophore of Ibuprofen and substituted diaryl rings on 5-membered heterocycle similar to coxibs and Nitric oxidereleasing moiety are described. All the synthesized compounds were tested in vivo for their anti-inflammatory, analgesic, ulcerogenic properties, and histopathological studies and in vitro for their nitric oxide-releasing properties. Out of the six synthesized compounds, four compounds showed significant anti-inflammatory and analgesic activity which was compared with standard. All the synthesized compounds exhibited significant nitric oxide-releasing and reduced GI ulcerogenic activity. Springer Science+Business Media, LLC 2010.
- Sarkate, Aniket P.,Lokwani, Deepak K.,Patil, Ajit A.,Bhandari, Shashikant V.,Bothara, Kailash G.
-
scheme or table
p. 795 - 808
(2012/05/31)
-
- Therapeutic compound-fatty acid conjugates
-
The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non-steroidal anti-infiammatory agents which include a carboxylic acid group. The compounds involve the use of tromethamine or ethanolamine derivative to link the acyl groups derived from fatty acids to the therapeutic compounds.
- -
-
Page column 9
(2010/01/30)
-