Search of new anti-inflammatory drugs among the derivatives of thiazolidine

1996 ◽  
Vol 4 ◽  
pp. S107
Author(s):  
V.J. Horishny ◽  
O.V. Vladzimirska ◽  
B.S. Zimenkovsky ◽  
R.B. Lesyk ◽  
O.M. Roman ◽  
...  
Keyword(s):  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

Cytostatic and Antiviral Activity Evaluations of Hydroxamic Derivatives of Some Non-steroidal Anti-inflammatory Drugs

2009 ◽  
Vol 73 (3) ◽  
pp. 328-338 ◽  
Author(s):  
Zrinka Rajic ◽  
Ivan Butula ◽  
Branka Zorc ◽  
Sandra Kraljevic Pavelic ◽  
Karlo Hock ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals Active Anti-Inflammatory and Hypolipidemic Derivatives of Lorazepam

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3277
Author(s):  
Panagiotis Theodosis-Nobelos ◽  
Georgios Papagiouvannis ◽  
Panos N. Kourounakis ◽  
Eleni A. Rekka
Keyword(s):  
Acute Inflammation ◽  
Current Knowledge ◽  
Rat Plasma ◽  
Straightforward Method ◽  
Inflammatory Drugs ◽  
Multifunctional Agents ◽  
Anti Inflammatory ◽  
High Yields ◽  
Derivatives Of ◽  
And Oxidative Stress

Novel derivatives of some non steroidal anti-inflammatory drugs, as well as of the antioxidants α-lipoic acid, trolox and (E)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid with lorazepam were synthesised by a straightforward method at satisfactory to high yields (40%–93%). All the tested derivatives strongly decreased lipidemic indices in rat plasma after Triton induced hyperlipidaemia. They also reduced acute inflammation and a number of them demonstrated lipoxygenase inhibitory activity. Those compounds acquiring antioxidant moiety were inhibitors of lipid peroxidation and radical scavengers. Therefore, the synthesised compounds may add to the current knowledge about multifunctional agents acting against various disorders implicating inflammation, dyslipidaemia and oxidative stress.

Synthesis and pharmacological evaluation of amide derivatives of non-steroidal anti-inflammatory drugs

1992 ◽  
Vol 1 (3) ◽  
pp. 201-212 ◽  
Author(s):  
M. -F. Otis ◽  
L. Levesque ◽  
F. Marceau ◽  
J. Lacroix ◽  
R. C. Gaudreault
Keyword(s):  
Pharmacological Evaluation ◽  
Amide Derivatives ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals Nitroxide derivatives of non-steroidal anti-inflammatory drugs exert anti-inflammatory and superoxide dismutase scavenging properties in A459 cells

2012 ◽  
Vol 165 (4b) ◽  
pp. 1058-1067 ◽  
Author(s):  
Wilmarie Flores-Santana ◽  
Terry Moody ◽  
Weibin Chen ◽  
Michael J Gorczynski ◽  
Mai E Shoman ◽  
...  
Keyword(s):  
Superoxide Dismutase ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals Analgesic and anti-inflammatory activity of 5,7-diacyl-3-H(alkіl)-6- aryl-5H-[1,2,4]triazol[3,4-b][1,3,4]tіadiazin derivaties

2015 ◽  
Vol 17 (2) ◽  
Author(s):  
O. Ye. Yadlovskyi ◽  
А. Ya. Koval ◽  
N. M. Seredynska ◽  
T. A. Bukhtiarova ◽  
T. A. Bershova ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Specific Activity ◽  
Reference Product ◽  
Antinociceptive Effect ◽  
Antinociceptive Activity ◽  
Hot Plate ◽  
Carrageenan Edema ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

The search for new analgesic and anti-inflammatory drugs, exceeding by efficacy and/or safety the existing<br />analogues is very important and relevant. The nitrogenous heterocycles are promising in this respect, in particular,<br />the compounds containing an imidazole triazol and tіadiazin moiety. The aim of the current study was to investigate<br />the antiexudative and antinociceptive activity of new derivatives of 5,7-diacyl-3-H(alkyl)-6-aryl-5H[1,2,4]triazol[3,4-b]<br />[1,3,4]thiadiazine.<br />The antinociceptive and antiexudative activity studies were carried out on the white nonlinear mice. The<br />experimental evaluation of specific activity was carried out on the models “Hot plate”, acetic acid induced writhing<br />(antinociceptive action) and carrageenan edema (antiexudative action). The substance was used in a single oral rout<br />administration in a dose of 25 mg/kg. Ketorolac was used as a reference product in the dose of 25 mg/kg (models<br />“Hot plate”, acetic acid induced writhing). Diclofenac was used as a reference product in the dose of 25 mg/kg on<br />the model carrageenan edema. The experimental study showed the antinociceptive and antiexudative effects of the<br />derivatives. The antinociceptive activity of 5,7-diacyl-3-H(alkіl)-6-aryl-5H[1,2,4]triazol[3,4-b][1,3,4]tіadiazin derivaties<br />related to the modification structure in the para position of benzene ring. The antiexudative activity is associated with<br />acetyl groups thiadiazine ring. The most promising compound IFT_247 showed a significant antinociceptive effect,<br />which is comparable to an active comparator ketorolac: “Hot plate” +232.46 % and +112.71 %; acetic acid induced<br />writhing -66.67 % and -61.02 %, respectively.

scholarly journals Synthesis of 1,2,3-triazole derivatives based on propargyl ester of a saturated single-basic carbonic acid and para-azidobenzoic acid

2021 ◽  
Vol 12 (1) ◽  
pp. 13-17
Author(s):  
Ibragimdjan Аbdugafurov Azizovich ◽  
Fazliddin Qirgizov Bakhtiyarovich ◽  
Ilhom Оrtikov Sobirovich
Keyword(s):  
Carbonic Acid ◽  
Effect Of Temperature ◽  
Reaction Yield ◽  
Factors Affecting ◽  
Low Toxicity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
First Time ◽  
Derivatives Of ◽  
Membered Heterocycle

The development of highly effective and low-toxicity nonsteroidal anti-inflammatory drugs (NSAIDs) is one of the important challenges facing modern pharmacology. To overcome this problem, many studies have been conducted on compounds containing a five-membered heterocycle containing three nitrogen atoms. The pharmacodynamics of these compounds are mainly due to their anti-inflammatory effect. Therefore, it is important to synthesize new derivatives of 1,2,3-triazoles, to determine their structure and to look for substances with anti-inflammatory activity on their basis. For the first time, the corresponding derivatives of 4-(4-(exchangeable)-1H-1,2,3-triazole-1-yl)-benzoic acid were synthesized by cycloaddition of propargyl esters of saturated carboxylic acids and para-azidobenzoic acid in the presence of copper (I) iodide. The structure of the obtained substances was analyzed by IR, 1H NMR, and MS techniques. It is proved that under the action of the catalyst in the reaction, only 1,4-isomers are formed. Factors affecting the course of the reaction were identified. Only one isomer is formed in the reaction of cyclic addition under the action of a catalyst and the effect of temperature, duration of time, and nature of the solvent on the reaction yield was studied.

scholarly journals Synthesis, anti-inflammatory, molecular docking and ADME studies of new derivatives of ketoprofen as cyclooxygenases inhibitor

2019 ◽  
pp. 125-139
Keyword(s):  
Molecular Docking ◽  
Side Effects ◽  
Nmr Spectra ◽  
Ft Ir ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Derivatives Of

The synthesis of new selective COX-2 enzyme is an approach for obtaining potent, anti-inflammatory drugs that have fewer side effects. Ketoprofen has a very low selectivity toward COX-2 enzyme and has a serious GIT side effects because it induces gastric ulcer. A new series of 4-thiazolidinones bearing ketoprofen moiety was designed, synthesized, and then evaluated as a new inhibitor of cyclooxygenase-2 (COX-2). Characterization and identification of the synthesized compounds were established by determination of 1H-NMR spectra,13C-NMR spectra, FT-IR spectroscopy, and physical properties. These newly synthesized compounds have been evaluated in vivo for their anti-inflammatory efficiency and in silico selectivity toward COX-2 throughout molecular docking by using GOLD.suite.v.5.6.2. All the tested. compounds via molecular. docking showed significant. activities when compared. With ketoprofen and diclofenac as references drugs, the results were consistent with the study of in in vivo acute. anti-inflammatory activity. Also, ADME studies had been accomplished in order to predict the absorption sites, bioavailability, topological polar surface Area (TPSA), and also drug-likeness. The ADME results reported that. All the synthesized. compounds can be absorbed by the GIT.

Synthetic strategies towards safer NSAIDs through prodrug approach: A review

2020 ◽  
Vol 21 ◽  
Author(s):  
Komal Gupta ◽  
Pooja A Chawla ◽  
Deepika Sharma
Keyword(s):  
Side Effects ◽  
Parent Compound ◽  
Docking Studies ◽  
Antipyretic Activity ◽  
Structure Activity ◽  
Carboxylic Groups ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Relationship Of ◽  
Derivatives Of

: Non-steroidal anti-inflammatory drugs (NSAIDs) are agents that are used for various properties such as analgesic activity, anti-inflammatory activity, antipyretic activity, etc. But this class of drugs is associated with different side effects such as dyspepsia, gastroduodenal ulcers, gastrointestinal (GI) bleeding and perforation, etc. The prodrug approach is quite beneficial to curb these side effects. Prodrugs are the inactive compounds that on metabolism get converted into an active metabolite exhibiting desired activities. Commonly used approaches for synthesizing prodrugs are amide, esters, and mutual prodrugs by suppressing the free carboxylic groups that are mainly responsible for these side effects. In this review, different schemes reported for the synthesis of NSAIDs that are devoid of undesired side effects such as irritation to gastric mucosa, gastrotoxicity, and ulcerogenicity have been compiled. Docking studies and the structure-activity relationship of some compounds are also discussed. The paper shall help the researchers to understand the methods to expedite the synthesis by carrying out substitutions of various groups of the parent compound and establish the mechanism of action of these derivatives of masking the unwanted side effects.

Sign in / Sign up

Export Citation Format

Share Document