Assessing gastric toxicity of xanthone derivatives of anti-inflammatory activity using simulation and experimental approaches

2017 ◽  
Vol 220 ◽  
pp. 20-33 ◽  
Author(s):  
Michal Markiewicz ◽  
Tadeusz Librowski ◽  
Anna Lipkowska ◽  
Pawel Serda ◽  
Krzysztof Baczynski ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Xanthone Derivatives ◽  
Experimental Approaches ◽  
Gastric Toxicity ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF NEW NAPROXEN ANALOGUES HAVING 1, 2, 4-TRIAZOLE-3-THIOL

2017 ◽  
Vol 9 (7) ◽  
pp. 66
Author(s):  
Monther F. Mahdi ◽  
Noor H. Naser ◽  
Nethal H. Hammud
Keyword(s):  
Aromatic Aldehydes ◽  
Heterocyclic Ring ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
Dose Equivalent ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: The objective of this search was to synthesize a new naproxen analogues having a 1,2,4-triazole-3-thiol heterocyclic ring, and preliminary pharmacological assessment of the anti-inflammatory activity of the synthesized compounds. Methods: The synthesis of naproxen analogues that having 1,2,4-triazole-3-thiol heterocyclic ring occur through esterification of naproxen, and then its reaction with hydrazine hydrate, and carbon disulfide, finally different aromatic aldehydes reacted with triazole derivatives of naproxen containing amino group to produce schiff bases.Results: In vivo acute anti-inflammatory activity of the synthesize compounds (Va-Vd) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (50 mg/kg) of naproxen. All tested compounds were produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Compound Vd produced superior anti-inflammatory activity compared to naproxen.Conclusion: The results obtained in this work give evidence about the valid synthesis of 1,2,4 triazole-3-thiol derivatives of naproxen, which reacted with different aldehydes to yield several schiff bases. The incorporation of benzaldehyde possess para-electron donating group (para-hydroxyl benzaldehyde) will increase the anti-inflammatory activity of naproxen.

scholarly journals Synthesis and Prognosis of Anti-inflammatory Activity of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3h)-one

2021 ◽  
Vol 7 (12) ◽  
pp. 25-33
Author(s):  
A. Chiriapkin ◽  
I. Kodonidi ◽  
A. Ivchenko ◽  
L. Smirnova
Keyword(s):  
Acetic Acid ◽  
Biological Activity ◽  
Dimethyl Sulfoxide ◽  
In Silico ◽  
Glacial Acetic Acid ◽  
Inflammatory Activity ◽  
Modified Method ◽  
Anti Inflammatory ◽  
Catalytic Addition ◽  
Derivatives Of

The article presents a modified method for the synthesis of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one and the predict of their anti-inflammatory activity. The proposed method for obtaining tetrahydrothienopyrimidine derivatives is preparatively effective and simple. Their synthesis was carried out by heterocyclization of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in the medium of glacial acetic acid with the catalytic addition of dimethyl sulfoxide. Preliminary prognosis of anti-inflammatory activity in silico method allowed us to identify the most promising compounds. Of these, the 4b structure containing a 2-hydroxyphenyl fragment in the second position of pyrimidine-4(3H)-one may be of the greatest interest. It seems appropriate to further study the spectrum of biological activity of the studied compounds.

scholarly journals A REVIEW ON ANTI-INFLAMMATORY POTENTIAL OF SUBSTITUTED PYRAZOLINE DERIVATIVES SYNTHESISED FROM CHALCONES

2018 ◽  
Vol 10 (2) ◽  
pp. 9 ◽  
Author(s):  
Muralidharan V. ◽  
Asha Deepti C. ◽  
Raja S.
Keyword(s):  
Inflammatory Activity ◽  
Biological Behaviour ◽  
Synthetic Compounds ◽  
Pyrazoline Ring ◽  
Heterocyclic Derivatives ◽  
Anti Inflammatory ◽  
Novel Drug ◽  
Derivatives Of ◽  
Aromatic Heterocyclic ◽  
Significant Class

The pyrazoline ring is a ubiquitous structural feature of many natural and synthetic compounds with potent anti-inflammatory activity. The creation of novel pyrazoline derivatives and examination of their chemical and biological behaviour have gained additional focus in the current decade. Pyrazolines and its fused heterocyclic derivatives tested with anti-inflammatory activity constitute a significant class of compounds for novel drug evolution. Pyrazoline nucleus when linked with different substituents like alkyl, aromatic, heterocyclic rings and many other groups at different positions on the ring shows considerable to more effective anti-inflammatory activity. This article presents a comprehensive review of the anti-inflammatory activity of some novel derivatives of pyrazoline ring.

Green synthesis of new sulfanyl derivatives of ampyrone and prediction of their anti-inflammatory activity

2020 ◽  
Vol 56 (4) ◽  
pp. 473-481 ◽  
Author(s):  
Nail S. Akhmadiev ◽  
Ekaterina S. Mescheryakova ◽  
Veronika R. Khairullina ◽  
Vnira R. Akhmetova ◽  
Askhat G. Ibragimov
Keyword(s):  
Green Synthesis ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Derivatives Of

The synthesis and anti-inflammatory activity of propargylamino derivatives of naphthoquinonlevopimaric acid

2015 ◽  
Vol 41 (1) ◽  
pp. 83-86 ◽  
Author(s):  
S. F. Vasilevsky ◽  
D. S. Baranov ◽  
A. I. Govdi ◽  
I. V. Sorokina ◽  
T. G. Tolstikova
Keyword(s):  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Derivatives Of

Synthesis and preliminary anti-inflammatory evaluation of xanthone derivatives

2018 ◽  
Vol 24 (4) ◽  
pp. 231-236 ◽  
Author(s):  
Dorota Żelaszczyk ◽  
Anna Lipkowska ◽  
Natalia Szkaradek ◽  
Karolina Słoczyńska ◽  
Agnieszka Gunia-Krzyżak ◽  
...  
Keyword(s):  
Liver Microsomes ◽  
Rat Liver Microsomes ◽  
Paw Edema ◽  
Reference Compound ◽  
Xanthone Derivatives ◽  
Ulcerogenic Effect ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Derivatives Of

AbstractXanthone derivatives of acetic, propionic and 2-methylpropionic acids were synthesized and assayed for their anti-inflammatory, analgesic and ulcerogenic activities. Compound 8 causes a dose-dependent diminution of paw edema (up to 61%) in the carrageenan model and at the highest tested dose reduces mechanical hyperalgesia in the Randall-Selitto test more effectively than the reference compound (~75% and ~32%, respectively). It shows high in vitro metabolic stability (Clint=12.5 μL/mg/min, t1/2=138.6 min) in the rat liver microsomes. None of the studied xanthone derivatives are ulcerogenic. The results of the present study suggest that compound 8 can be of interest in the future for the search for antinociceptive and antiedematous agents devoid of ulcerogenic effect.

Synthesis and anti-inflammatory activity of acyl derivatives of taraxasterol

2008 ◽  
Vol 42 (6) ◽  
pp. 319-321 ◽  
Author(s):  
É. R. Shakurova ◽  
T. I. Parfenova ◽  
R. Sh. Sufiyarova ◽  
A. Z. Khalilova ◽  
V. R. Akhmetova ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Acyl Derivatives

scholarly journals Synthesis of Either C2- or C4′-Alkylated Derivatives of Honokiol and Their Biological Evaluation for Anti-inflammatory Activity

2019 ◽  
Vol 67 (9) ◽  
pp. 966-976 ◽  
Author(s):  
San-ha Lee ◽  
Xiang Fei ◽  
Chaelin Lee ◽  
Hien Thi Thu Do ◽  
Inmoo Rhee ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Derivatives Of
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