Design, Synthesis, and Preliminary Pharmacological Evaluation ofN-Acyl-3-aminoglutarimides as Broad-Spectrum Chemokine Inhibitors in Vitro and Anti-inflammatory Agents in Vivo

2002 ◽  
Vol 45 (2) ◽  
pp. 360-370 ◽  
Author(s):  
David J. Fox ◽  
Jill Reckless ◽  
Stuart G. Warren ◽  
David J. Grainger
Keyword(s):  
Broad Spectrum ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
Anti Inflammatory

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents

2020 ◽  
Vol 186 ◽  
pp. 111863 ◽  
Author(s):  
Muhammad Saeed Jan ◽  
Sajjad Ahmad ◽  
Fida Hussain ◽  
Ashfaq Ahmad ◽  
Fawad Mahmood ◽  
...  
Keyword(s):  
In Silico ◽  
Design Synthesis ◽  
In Silico Studies ◽  
Anti Inflammatory

scholarly journals (E)-2-Cyano-3-(1H-Indol-3-yl)-N-Phenylacrylamide, a Hybrid Compound Derived from Indomethacin and Paracetamol: Design, Synthesis and Evaluation of the Anti-Inflammatory Potential

2020 ◽  
Vol 21 (7) ◽  
pp. 2591
Author(s):  
Pablo Silva ◽  
Maria de Almeida ◽  
Jamire Silva ◽  
Sonaly Albino ◽  
Renan Espírito-Santo ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Significant Inhibition ◽  
In Vitro Assays ◽  
Paw Edema ◽  
Substituted Anilines ◽  
Hybrid Compound ◽  
Design Synthesis ◽  
Anti Inflammatory

The compound (E)-2-cyano-3-(1H-indol-3-yl)-N-phenylacrylamide (ICMD-01) was designed and developed based on the structures of clinically relevant drugs indomethacin and paracetamol through the molecular hybridization strategy. This derivative was obtained by an amidation reaction between substituted anilines and ethyl 2-cyanoacetate followed by a Knoevenagel-type condensation reaction with indole aldehyde that resulted in both a viable synthesis and satisfactory yield. In order to assess the immunomodulatory and anti-inflammatory activity, in vitro assays were performed in J774 macrophages, and significant inhibitions (p < 0.05) of the production of nitrite and the production of cytokines (IL-1β and TNFα) in noncytotoxic concentrations were observed. The anti-inflammatory effect was also studied via CFA-induced paw edema in vivo tests and zymosan-induced peritonitis. In the paw edema assay, ICMD01 (50 mg kg−1) showed satisfactory activity, as did the group treated with dexamethasone, reducing edema in 2–6 h. In addition, there was no significant inhibition of PGE2, IL-1β or TNFα in vivo. Moreover, in the peritonitis assay that assesses leukocyte migration, ICMD-01 exhibited promising results. Therefore, these preliminary studies demonstrate this compound to be a strong candidate for an anti-inflammatory drug together with an improved gastrointestinal safety profile when compared to the conventional anti-inflammatory drugs.

Design, synthesis, and preliminary in vitro and in vivo pharmacological evaluation of 4-{4-[2-(4-(2-substitutedquinoxalin-3-yl)piperazin-1-yl)ethyl]phenyl}thiazoles as atypical antipsychotic agents

2012 ◽  
Vol 22 (4) ◽  
pp. 1660-1673 ◽  
Author(s):  
Kondapalli Venkata Gowri Chandra Sekhar ◽  
Vajja Sambasiva Rao ◽  
Winnie Deuther-Conrad ◽  
Divya Sridhar ◽  
Hunsur Nagendra Nagesh ◽  
...  
Keyword(s):  
Atypical Antipsychotic ◽  
Antipsychotic Agents ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
Atypical Antipsychotic Agents

scholarly journals Design, Synthesis and Characterization of Some Novel benzamide derivatives and it's Pharmacological Screening

2020 ◽  
pp. 68-74 ◽  
Author(s):  
Akshay R. Yadav ◽  
Shrinivas K. Mohite
Keyword(s):  
Chemical Structure ◽  
Design Synthesis ◽  
Different Types ◽  
Anti Inflammatory ◽  
Benzoyl Isothiocyanate ◽  
Pharmacological Screening ◽  
Benzamide Derivatives

The new series of substituted N-(phenylcarbamothioyl)benzamide derivatives (2a-2f) was designed, development and synthesized by using conventional and microwave method. In present work 6 different N-(phenylcarbamothioyl)benzamide were synthesized. Substituted benzoyl chloride is converted into benzoyl isothiocyanate by esterification. Benzoyl isothiocyanate is converted into Substituted (phenylcarbamothioyl)benzamide by treating with different types of substituted aniline. Confirmation of the chemical structure of the synthesized was substantiated by TLC, IR, 1H NMR, MS spectroscopy.Novel synthesized compounds screened for their in vivo and in-vitro anti-inflammatory studies and compound 2f shows promising anti-inflammatory activity.

scholarly journals In Vitro Antiviral Activity of Doxycycline against SARS-CoV-2

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5064 ◽  
Author(s):  
Mathieu Gendrot ◽  
Julien Andreani ◽  
Priscilla Jardot ◽  
Sébastien Hutter ◽  
Océane Delandre ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Broad Spectrum ◽  
In Vitro Study ◽  
Experimental Models ◽  
In Vivo Evaluation ◽  
Study Results ◽  
Anti Inflammatory ◽  
Approved Drugs

In December 2019, a new severe acute respiratory syndrome coronavirus (SARS-CoV-2), causing coronavirus disease 2019 (COVID-19), emerged in Wuhan, China. Despite containment measures, SARS-CoV-2 spread in Asia, Southern Europe, then in America and currently in Africa. Identifying effective antiviral drugs is urgently needed. An efficient approach to drug discovery is to evaluate whether existing approved drugs can be efficient against SARS-CoV-2. Doxycycline, which is a second-generation tetracycline with broad-spectrum antimicrobial, antimalarial and anti-inflammatory activities, showed in vitro activity on Vero E6 cells infected with a clinically isolated SARS-CoV-2 strain (IHUMI-3) with median effective concentration (EC50) of 4.5 ± 2.9 µM, compatible with oral uptake and intravenous administrations. Doxycycline interacted both on SARS-CoV-2 entry and in replication after virus entry. Besides its in vitro antiviral activity against SARS-CoV-2, doxycycline has anti-inflammatory effects by decreasing the expression of various pro-inflammatory cytokines and could prevent co-infections and superinfections due to broad-spectrum antimicrobial activity. Therefore, doxycycline could be a potential partner of COVID-19 therapies. However, these results must be taken with caution regarding the potential use in SARS-CoV-2-infected patients: it is difficult to translate in vitro study results to actual clinical treatment in patients. In vivo evaluation in animal experimental models is required to confirm the antiviral effects of doxycycline on SARS-CoV-2 and more trials of high-risk patients with moderate to severe COVID-19 infections must be initiated.

scholarly journals Design and Synthesis of 2-Mercapto Benzoxazole coupled Benzyl Triazoles as Anti-inflammatory Agents Targeting COX-2 Enzyme

2020 ◽  
Vol 32 (12) ◽  
pp. 3209-3218
Author(s):  
K. Praveen Kumar ◽  
Y. Prashanthi ◽  
G. Rambabu ◽  
Md. Ataur Rahman ◽  
J.S. Yadav
Keyword(s):  
Chemical Space ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Design Synthesis ◽  
Standard Drug ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Anti Inflammatory

In this study, we report the design, synthesis and the biological evaluation of 19 analogues of 2-mercapto benzoxazole coupled benzyl triazoles (BOTs) based on analysis of the binding site and literature of chemical space. These BOTs were evaluated both in vitro and in vivo for their anti-inflammatory activity. Eleven compounds showed less than 10 μM in vitro COX-2 enzyme activities. The most potent analogue among the BOT analogues were BOT15, BOT3 and BOT19 with IC50 3.40 μM, 4.50 μM and 4.57 μM respectively against COX-2. The in vivo anti-inflammatory activity of two BOTs has significantly higher than that of standard drug, ibuprofen. 2-Mercapto benzoxazole coupled benzyl triazoles (BOTs) were also tested for their antioxidant capacity and proved to be an as active scavenger, better than ascorbic acid.

Novel paeonol derivatives: Design, synthesis and anti-inflammatory activity in vitro and in vivo

2020 ◽  
Vol 98 ◽  
pp. 103735 ◽  
Author(s):  
Yang Sheng Hu ◽  
Xu Han ◽  
Pei Jing Yu ◽  
Ming Ming Jiao ◽  
Xin Hua Liu ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Design Synthesis ◽  
Anti Inflammatory
Sign in / Sign up

Export Citation Format

Share Document