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.

Design, synthesis and characterization of hydroxyapatite-chitosan nanocomposite radiolabelled with 153Sm as radiopharmaceutical for use in radiosynovectomy

2019 ◽  
Vol 108 (1) ◽  
pp. 57-65
Author(s):  
Sima Attar Nosrati ◽  
Robabeh Alizadeh ◽  
Seyed Javad Ahmadi ◽  
Mostafa Erfani
Keyword(s):  
Chemical Structure ◽  
Therapeutic Agent ◽  
Radiochemical Purity ◽  
Saline Solution ◽  
Wild Type ◽  
Design Synthesis ◽  
Physiochemical Properties

Abstract The aim of the present study was to introduction of hydroxyapatite/chitosan nanocomposite as a new radiosynovectomy agent with excellent properties. In this work, the nanocomposite was prepared through a reliable method and characterized using different techniques to elucidate its chemical structure and physiochemical properties. The prepared nanocomposite was successfully radiolabeled with 153Sm under optimal conditions and with high radiolabelling yield (99 %). The radiochemical purity of the prepared radiopharmaceutical was found to be >99 % as determined by ITLC technique. In vitro stability studies in saline solution and in human serum showed that the radiolabeled nanocomposite retained its stability for at least 6 days. The biodistribution and imaging studies in wild-type rats revealed high retention of the agent into the synovial joints of the knee even at 96 h post-injection, thereby indicating excellent in vivo stability of 153Sm labeled hydroxyapatite-chitosan nanocomposite. Therefore, the prepared radiopharmaceutical would be a potential therapeutic agent for use in radiosynovectomy procedure.

scholarly journals Engineering nucleosomes for generating diverse chromatin assemblies

2021 ◽  
Author(s):  
Zenita Adhireksan ◽  
Deepti Sharma ◽  
Phoi Leng Lee ◽  
Qiuye Bao ◽  
Sivaraman Padavattan ◽  
...  
Keyword(s):  
Dynamic Properties ◽  
Dna Nanostructures ◽  
Macromolecular Assemblies ◽  
Maximum Resolution ◽  
Different Types ◽  
Chromatin Structural ◽  
Dna Fragment

Abstract Structural characterization of chromatin is challenging due to conformational and compositional heterogeneity in vivo and dynamic properties that limit achievable resolution in vitro. Although the maximum resolution for solving structures of large macromolecular assemblies by electron microscopy has recently undergone profound increases, X-ray crystallographic approaches may still offer advantages for certain systems. One such system is compact chromatin, wherein the crystalline state recapitulates the crowded molecular environment within the nucleus. Here we show that nucleosomal constructs with cohesive-ended DNA can be designed that assemble into different types of circular configurations or continuous fibers extending throughout crystals. We demonstrate the utility of the method for characterizing nucleosome compaction and linker histone binding at near-atomic resolution but also advance its application for tackling further problems in chromatin structural biology and for generating novel types of DNA nanostructures. We provide a library of cohesive-ended DNA fragment expression constructs and a strategy for engineering DNA-based nanomaterials with a seemingly vast potential variety of architectures and histone chemistries.

scholarly journals B-1 cell: the precursor of a novel mononuclear phagocyte with immuno-regulatory properties

2009 ◽  
Vol 81 (3) ◽  
pp. 489-496 ◽  
Author(s):  
José Daniel Lopes ◽  
Mario Mariano
Keyword(s):  
Mammalian Cells ◽  
Giant Cells ◽  
Mononuclear Phagocyte ◽  
Different Types ◽  
Series Of Experiments ◽  
B1 Cells ◽  
Regulatory Properties

Characterization of the origin, properties, functions and fate of cells is a fundamental task for the understanding of physiological and pathological phenomena. Despite the bulk of knowledge concerning the diverse characteristics of mammalian cells, some of them, such as B-1 cells, are still poorly understood. Here we report the results obtained in our laboratory on these cells in the last 10 years. After showing that B-1 cells could be cultured and amplified in vitro, a series of experiments were performed with these cells. They showed that B1 cells reside mostly in the peritoneal and pleural cavities, migrate to distant inflammatory foci, coalesce to form giant cells and participate in granuloma formation, both in vitro and in vivo. They are also able to present antigens to immunologically responsive cells and are endowed with regulatory properties. Further, we have also shown that these cells facilitate different types of infection as well as tumor growth and spreading. These data are presently reviewed pointing to a pivotal role that these cells may play in innate and acquired immunity.

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.

Development, in-vitro and in-vivo characterization of gelatin nanoparticles for delivery of an anti-inflammatory drug

2016 ◽  
Vol 36 ◽  
pp. 55-61 ◽  
Author(s):  
Alok Mahor ◽  
Sunil Kumar Prajapati ◽  
Amita Verma ◽  
Rishikesh Gupta ◽  
Thakur Raghu Raj Singh ◽  
...  
Keyword(s):  
Gelatin Nanoparticles ◽  
Inflammatory Drug ◽  
Anti Inflammatory ◽  
Development In Vitro ◽  
In Vivo Characterization
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