Synthesis, anticancer, and anti-inflammatory activity evaluation of methanesulfonamide and amidine derivatives of 3,4-diaryl-2-imino-4-thiazolines

2009 ◽  
Vol 13 (3) ◽  
pp. 357-366 ◽  
Author(s):  
Sham M. Sondhi ◽  
Reshma Rani ◽  
P. P. Gupta ◽  
S. K. Agrawal ◽  
A. K. Saxena
Author(s):  
Monther F. Mahdi ◽  
Noor H. Naser ◽  
Nethal H. Hammud

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.


2021 ◽  
Vol 7 (12) ◽  
pp. 25-33
Author(s):  
A. Chiriapkin ◽  
I. Kodonidi ◽  
A. Ivchenko ◽  
L. Smirnova

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.


2008 ◽  
Vol 43 (7) ◽  
pp. 1432-1437 ◽  
Author(s):  
Federico Martínez-Ramos ◽  
Hector Salgado-Zamora ◽  
Maria Elena Campos-Aldrete ◽  
Estela Melendez-Camargo ◽  
Yazmín Márquez-Flores ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1701
Author(s):  
Jinjie Li ◽  
Xiuting Li ◽  
Xin Wang ◽  
Xiangjian Zhong ◽  
Linlin Ji ◽  
...  

Four new sesquiterpenoids (1–4) and six known sesquiterpenoids (5–10), were isolated from the EtOAc phase of the ethanolic extract of Ainsliaea yunnanensis. Their structures were established by spectroscopic methods, including 1-D, 2-D NMR and HPLC-MS. All compounds were tested for their anti-inflammatory effect by the inhibition of the activity of NLRP3 inflammasome by blocking the self-slicing of pro-caspase-1, which is induced by nigericin, then the secretion of mature IL-1β, mediated by caspase-1, was suppressed. Unfortunately none of the compounds showed an anti-inflammatory effect.


Author(s):  
Muralidharan V. ◽  
Asha Deepti C. ◽  
Raja S.

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.


2016 ◽  
Vol 31 (6) ◽  
pp. 1520-1526 ◽  
Author(s):  
Pramod K. Sharma ◽  
Sakshi Balwani ◽  
Divya Mathur ◽  
Shashwat Malhotra ◽  
Brajendra K. Singh ◽  
...  

2020 ◽  
Vol 56 (4) ◽  
pp. 473-481 ◽  
Author(s):  
Nail S. Akhmadiev ◽  
Ekaterina S. Mescheryakova ◽  
Veronika R. Khairullina ◽  
Vnira R. Akhmetova ◽  
Askhat G. Ibragimov

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

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