Synthesis and Biological Evaluation of New Antiinflammatory 1-Benzothiophene-2-carboxanilides

2000 ◽  
Vol 65 (7) ◽  
pp. 1082-1092 ◽  
Author(s):  
Jiří Svoboda ◽  
Michal Štádler ◽  
Antonín Jandera ◽  
Vladimíra Panajotová ◽  
Miroslav Kuchař
Keyword(s):  
Biological Evaluation ◽  
Antiinflammatory Effect ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1 ◽  
Carrageenin Edema

3-Substituted 1-benzothiophene-2-carboxanilides 2-5 and their corresponding sulfones 6-8 were synthesized. The antiinflammatory effect of compounds 2-8 was evaluated in tests of LTB4 biosynthesis, carrageenin edema and ear inflammation. With the exception of 3-hydroxyamides 5a-5c, low inhibitory activities against COX and LT biosynthesis were observed.

scholarly journals Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position

MedChemComm ◽  
2018 ◽  
Vol 9 (3) ◽  
pp. 545-553 ◽  
Author(s):  
David Cousin ◽  
Marc G. Hummersone ◽  
Tracey D. Bradshaw ◽  
Jihong Zhang ◽  
Christopher J. Moody ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Growth Inhibitory ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

The synthesis and biological evaluation of imidazotetrazines substituted at N-3 is described.

Facile Synthesis and Biological Evaluation of Cyclopropyl-Pyrazole Hybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents

2019 ◽  
Vol 4 (3) ◽  
pp. 152-158
Author(s):  
P.C. Burde ◽  
A.M. Rahatgaonkar
Keyword(s):  
Ionic Liquid ◽  
Ambient Temperature ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Biphasic System ◽  
Facile Synthesis ◽  
Convenient Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from corresponding chalcones were synthesized and evaluated for their biological activities. A convenient synthesis of a library of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic system at ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which are immiscible, has been easily recycled and reused after separation of the products without any noticeable diminution in its activity.

Synthesis and biological evaluation of oleanolic acid derivative–chalcone conjugates as α-glucosidase inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (21) ◽  
pp. 10862-10874 ◽  
Author(s):  
Chu Tang ◽  
Linhui Zhu ◽  
Yu Chen ◽  
Rui Qin ◽  
ZhiNan Mei ◽  
...  
Keyword(s):  
Acid Derivative ◽  
Oleanolic Acid ◽  
Biological Evaluation ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation ◽  
Oleanolic Acid Derivative

Series of oleanolic acid derivative–chalcone conjugates were designed, synthesized and their α-glucosidase inhibitory activities were investigatedin vitro.

scholarly journals Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-N-substituted-hydrazinecarbothioamides

2012 ◽  
Vol 22 (4) ◽  
pp. 2014-2022 ◽  
Author(s):  
Subhas S. Karki ◽  
Amol A. Kulkarni ◽  
Sujeet Kumar ◽  
Suresh Kumar Veliyath ◽  
Erik De Clercq ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL THIAZOLE-PYRAZOLE INTEGRATED CHALCONES AS ANTIOXIDANT AND ANTI-INFLAMMATORY AGENTS

2019 ◽  
pp. 311-315
Author(s):  
DNYANESHWAR SIRSAT ◽  
PRADEEP KATE ◽  
MADHUSUDAN BACHUTE
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
Schmidt Reaction ◽  
Chemical Structures ◽  
1H Nuclear Magnetic Resonance ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

Objective: The objective of the present study was to synthesize the thiazole-pyrazole integrated chalcones and their in vitro antioxidant and anti- inflammatory evaluation. Methods: The designed hybrid thiazole-pyrazole integrated chalcones (3a-j) were synthesized by Claisen–Schmidt reaction of substituted 1-(4-methyl-2-phenylthiazol-5-yl) ethanone and substituted pyrazole aldehyde in the presence of 10% NaOH in ethanol solvent under reflux condition. The chemical structures of synthesized compounds were confirmed by IR, 1H nuclear magnetic resonance (NMR), 13C NMR, and high- resolution mass spectra. Results: All the title compounds were screened for their in vitro antioxidant and anti-inflammatory activity. The screening data indicated that tested compounds showed potent antioxidant activity with moderate anti-inflammatory potential. Conclusion: Antioxidant screening data reveal that most of the synthesized compounds possess excellent 1,1-diphenyl-2-picrylhydrazyl and NO radical scavenging activity. Most of the compounds found to possess marked anti-inflammatory potential by effectively inhibiting the heat-induced albumin denaturation.

Synthesis and Biological Evaluation of 2, 3-Diaryl substituted-1, 3-thiazolidin-4-ones as Anti-HIV Agents

2007 ◽  
Vol 3 (4) ◽  
pp. 355-363 ◽  
Author(s):  
Ravindra K. Rawal ◽  
Raj Kamal Tripathi ◽  
S.B. Katti ◽  
Christophe Pannecouque ◽  
Erik De Clercq
Keyword(s):  
Biological Evaluation ◽  
Anti Hiv Agents ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1 ◽  
Anti Hiv

ChemInform Abstract: Synthesis and Biological Evaluation of Some 4-Substituted 1-[1-(4-Hydroxybutyl)-1,2,3-triazol-(4 and 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.

ChemInform ◽  
2010 ◽  
Vol 33 (9) ◽  
pp. no-no
Author(s):  
O. Moukha-Chafiq ◽  
M. L. Taha ◽  
H. B. Lazrek ◽  
J. J. Vasseur ◽  
C. Pannecouque ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

scholarly journals Correction: Synthesis and biological evaluation of hybrids from farnesylthiosalicylic acid and hydroxylcinnamic acid with dual inhibitory activities of Ras-related signaling and phosphorylated NF-κB

2021 ◽  
Author(s):  
Yong Ling ◽  
Zhiqiang Wang ◽  
Xuemin Wang ◽  
Ying Zhao ◽  
Wei Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Correction for ‘Synthesis and biological evaluation of hybrids from farnesylthiosalicylic acid and hydroxylcinnamic acid with dual inhibitory activities of Ras-related signaling and phosphorylated NF-κB’ by Yong Ling et al., Org. Biomol. Chem., 2014, 12, 4517–4530, DOI: 10.1039/C4OB00023D.

Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates

MedChemComm ◽  
2016 ◽  
Vol 7 (6) ◽  
pp. 1146-1150 ◽  
Author(s):  
Mateusz Daśko ◽  
Maciej Masłyk ◽  
Konrad Kubiński ◽  
Justyna Aszyk ◽  
Janusz Rachon ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Steroid Sulfatase ◽  
Coumarin 7 ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

In the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors.

Solution-phase synthesis and biological evaluation of triostin A and its analogues

2016 ◽  
Vol 14 (6) ◽  
pp. 2090-2111 ◽  
Author(s):  
Kozo Hattori ◽  
Kota Koike ◽  
Kensuke Okuda ◽  
Tasuku Hirayama ◽  
Masahiro Ebihara ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Biological Evaluation ◽  
Solution Phase ◽  
Phase Synthesis ◽  
Total Syntheses ◽  
Solution Phase Synthesis ◽  
Triostin A ◽  
Inhibitory Activities ◽  
High Yields ◽  
Synthesis And Biological Evaluation

We have accomplished preparative solution-phase total syntheses of triostin A (17.5% in 13 steps) and its analogues with high yields to demonstrate their significant inhibitory activities on HIF-1 activation and cell proliferation.

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