Synthesis, analgesic, anti-inflammatory, ulcerogenic index and antibacterial activities of novel 2-methylthio-3-substituted-5,6,7,8-tetrahydrobenzo (b) thieno[2,3-d]pyrimidin-4(3H)-ones

2006 ◽  
Vol 41 (11) ◽  
pp. 1293-1300 ◽  
Author(s):  
V. Alagarsamy ◽  
S. Meena ◽  
K.V. Ramseshu ◽  
V.R. Solomon ◽  
K. Thirumurugan ◽  
...  
2017 ◽  
Vol 17 (43) ◽  
pp. 28-33 ◽  
Author(s):  
M Asif

A series of substituted triazin-pyridazine compounds were exhibited diverse types of biological activities and synthesized by different methods. These compounds were mainly tested for their anti-inflammatory, anticancer, antifungal and antibacterial activities. These substituted triazin-pyridazine compounds have mild to potent activities on compare with their appropriate reference standards.


2003 ◽  
Vol 69 (3) ◽  
pp. 448-449 ◽  
Author(s):  
E.E. Elgorashi ◽  
S. Zschocke ◽  
J. van Staden ◽  
J.N. Eloff

2012 ◽  
Vol 19 (11) ◽  
pp. 1784-1791 ◽  
Author(s):  
Abhigyan Som ◽  
Nicolás Navasa ◽  
Avital Percher ◽  
Richard W. Scott ◽  
Gregory N. Tew ◽  
...  

ABSTRACTA group of synthetic antimicrobial oligomers, inspired by naturally occurring antimicrobial peptides, were analyzed for the ability to modulate innate immune responses to Toll-like receptor (TLR) ligands. These synthetic mimics of antimicrobial peptides (SMAMPs) specifically reduced cytokine production in response toStaphylococcus aureusand theS. aureuscomponent lipoteichoic acid (LTA), a TLR2 agonist. Anti-inflammatory SMAMPs prevented the induction of tumor necrosis factor (TNF), interleukin 6 (IL-6), and IL-10 in response toS. aureusor LTA, but no other TLR2 ligands. We show that these SMAMPs bind specifically to LTAin vitroand prevent its interaction with TLR2. Importantly, the SMAMP greatly reduced the induction of TNF and IL-6in vivoin mice acutely infected withS. aureuswhile simultaneously reducing bacterial loads dramatically (4 log10). Thus, these SMAMPs can eliminate the damage induced by pathogen-associated molecular patterns (PAMPs) while simultaneously eliminating infectionin vivo. They are the first known SMAMPs to demonstrate anti-inflammatory and antibacterial activitiesin vivo.


2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Leila Maria Leal Parente ◽  
Ruy de Souza Lino Júnior ◽  
Leonice Manrique Faustino Tresvenzol ◽  
Marina Clare Vinaud ◽  
José Realino de Paula ◽  
...  

Calendula officinalisis an annual herb from Mediterranean origin which is popularly used in wound healing and as an anti-inflammatory agent. In this study, the ethanolic extract, the dichloromethane, and hexanic fractions of the flowers from plants growing in Brazil were produced. The angiogenic activity of the extract and fractions was evaluated through the chorioallantoic membrane and cutaneous wounds in rat models. The healing activity of the extract was evaluated by the same cutaneous wounds model through macroscopic, morphometric, histopathologic, and immunohistochemical analysis. The antibacterial activity of the extract and fractions was also evaluated. This experimental study revealed thatC. officinalispresented anti-inflammatory and antibacterial activities as well as angiogenic and fibroplastic properties acting in a positive way on the inflammatory and proliferative phases of the healing process.


2011 ◽  
Vol 76 (12) ◽  
pp. 1617-1626 ◽  
Author(s):  
Mohammad Alam ◽  
Priya Sarkar ◽  
Asif Husain ◽  
Akranth Marella ◽  
M.S. Zaman ◽  
...  

A series of 3-[2-chloroquinolin-3-yl)methylene]-5-aryl-furan-2(3H)-ones {3(a-p)} were synthesized. The required 3-(substitutedbenzoyl) propionic acids {2(a-d)} were prepared under Friedal Craft acylation reaction conditions. The substituted 2-chloroquinoline-3-carbaldehydes {1(a-d)} were synthesized by reaction of substitutedphenylethanone-oxime with phosphorus oxychloride in presence of dimethyl formamide using the Vilsmeir Haack reaction method. These compounds were screened for their anti-inflammatory and antibacterial activities along with their ulcerogenic and lipid peroxidation potentials. The compounds that showed significant anti-inflammatory activity were further screened for their analgesic activity. The compounds were less toxic in terms of ulcerogenicity as compared to a standard, which was also supported by lipid peroxidation studies. The antibacterial activities were performed against Staphylococcus aureus and Escherichia coli. Compounds 3f, 3n and 3o showed significant activity against both S. aureus and E. coli having an MIC value of 6.25?g mL-1.


Molecules ◽  
2019 ◽  
Vol 24 (5) ◽  
pp. 856 ◽  
Author(s):  
Wansha Yu ◽  
Hu Chen ◽  
Zhonghuai Xiang ◽  
Ningjia He

The extraction of Ramulus mori polysaccharides (RMPs) was optimized using response surface methodology (RSM). The optimal process conditions, which gave the highest yield of RMPs (6.25%) were 80 °C, 50 min, and a solid–liquid ratio of 1:40 (g/mL), with the extraction performed twice. The RMPs contained seven monosaccharides, namely, mannose, rhamnose; glucuronic acid, glucose, xylose, galactose, and arabinose, in a 1.36:2.68:0.46:328.17:1.53:21.80:6.16 molar ratio. The glass transition and melting temperatures of RMPs were 83 and 473 °C, respectively. RMPs were α-polysaccharides and had surfaces that resembled a porous sponge, as observed by scanning electron microscopy. RMPs inhibited the proliferation of Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa and showed antioxidant activity (assessed by three different methods), although it was generally weaker than that of vitamin C. RMPs showed anti-inflammatory activity in a concentration-dependent manner. This study provides a basis for exploring the potential uses of RMPs.


2014 ◽  
Vol 13 (2) ◽  
pp. 104 ◽  
Author(s):  
Anupama Singh ◽  
Anil Bhandari ◽  
Abhishek Khatri ◽  
IndarC Kumawat ◽  
VikasA Saharan

2009 ◽  
Vol 74 (2) ◽  
pp. 103-115 ◽  
Author(s):  
Asif Husain ◽  
Mumtaz Alam ◽  
Nadeem Siddiqui

3-Arylidene-5-(4-methylphenyl)-2(3H)-furanones 2a-m were prepared from 3-(4-methyl-benzoyl)propanoic acid 1 and several aromatic aldehydes. Some of the selected furanones were reacted with ammonia gas and benzylamine to give corresponding 3-arylidene-1,3-dihydro-5-(4-methylphenyl)-2H-pyrrol- 2-ones 3a-h and 3-arylidene-1-benzyl-1,3-dihydro-5-(4-methylphenyl)-2H- -pyrrol-2-ones 4a-f, respectively, which were characterized on the basis of IR, 1H-NMR, mass spectral data and elemental analysis results. These compounds were tested for their anti-inflammatory and antibacterial activities. The compounds, which showed significant anti-inflammatory activity, were further screened for their analgesic and ulcerogenic activities. Three new compounds (2e, 2h and 4d), out of twenty-seven showed very good anti-inflammatory activity in the carrageenan induced rat paw edema test, with significant analgesic activity in the acetic acid induced writhing test together with negligible ulcerogenic action. The antibacterial activity is expressed as the corresponding MIC values.


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