scholarly journals Optimized Synthesis of New Thiosemicarbazide Derivatives with Tuberculostatic Activity

2021 ◽  
Vol 22 (22) ◽  
pp. 12139
Author(s):  
Corina Popovici ◽  
Cristina-Maria Pavel ◽  
Valeriu Sunel ◽  
Corina Cheptea ◽  
Dan Gheorghe Dimitriu ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Spectral Analysis ◽  
Elemental Analysis ◽  
Tuberculostatic Activity ◽  
Medical Applications ◽  
Wide Range ◽  
Biological Tests ◽  
Ft Ir ◽  
Thiosemicarbazide Derivatives

Original results are presented in the field of research that addresses the extension of the reaction of residue of acyl-thiosemicarbazide fixation on the structure of 5-nitrobenzimidazole by a sulphonic group. The aim of the study is the increase of new thiosemicarbazide derivatives’ applicative potential in the field of biochemistry, with a wide range of medical applications. The newly obtained compounds were characterized by using elemental analysis and spectral analysis (FT-IR and 1H NMR). A study regarding the optimization of the chemical reactions was made. The performed in vitro biological tests confirmed the tuberculostatic activity of three newly obtained compounds against Mycobacterium tuberculosis.

scholarly journals Advanced Functional Materials Based on Nanocellulose for Pharmaceutical/Medical Applications

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1125
Author(s):  
Raluca Nicu ◽  
Florin Ciolacu ◽  
Diana E. Ciolacu
Keyword(s):  
Rapid Development ◽  
Cellulose Nanofibrils ◽  
Functional Materials ◽  
Medical Applications ◽  
Bacterial Nanocellulose ◽  
Green Materials ◽  
Wide Range ◽  
In Vivo Cytotoxicity

Nanocelluloses (NCs), with their remarkable characteristics, have proven to be one of the most promising “green” materials of our times and have received special attention from researchers in nanomaterials. A diversity of new functional materials with a wide range of biomedical applications has been designed based on the most desirable properties of NCs, such as biocompatibility, biodegradability, and their special physicochemical properties. In this context and under the pressure of rapid development of this field, it is imperative to synthesize the successes and the new requirements in a comprehensive review. The first part of this work provides a brief review of the characteristics of the NCs (cellulose nanocrystals—CNC, cellulose nanofibrils—CNF, and bacterial nanocellulose—BNC), as well as of the main functional materials based on NCs (hydrogels, nanogels, and nanocomposites). The second part presents an extensive review of research over the past five years on promising pharmaceutical and medical applications of nanocellulose-based materials, which have been discussed in three important areas: drug-delivery systems, materials for wound-healing applications, as well as tissue engineering. Finally, an in-depth assessment of the in vitro and in vivo cytotoxicity of NCs-based materials, as well as the challenges related to their biodegradability, is performed.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

scholarly journals Synthesis of Optically Active Bicyclic Derivatives of Nitroimidazoles

Compounds ◽  
2021 ◽  
Vol 1 (3) ◽  
pp. 145-153
Author(s):  
Justyna Żwawiak ◽  
Lucjusz Zaprutko
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Biological Activity ◽  
Optically Active ◽  
Tuberculostatic Activity ◽  
Wide Range ◽  
Derivatives Of

Nitroimidazoles are characterized by a wide range of biological activity and many of them are used as therapeutics. Moreover, some bicyclic nitroimidazooxazoles show considerable potency against Mycobacterium tuberculosis. Some authors noticed that in the case of chiral derivatives of nitroimidazodihydrooxazoles, the (R) form shows a greater tuberculostatic activity than the (S) enantiomer. This work describes the procurement of new 12 enantiomeric bicyclic derivatives of nitroimidazole.

scholarly journals Insulin-Loaded Barium Salt Particles Facilitate Oral Delivery of Insulin in Diabetic Rats

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 710
Author(s):  
Rahela Zaman ◽  
Md. Emranul Karim ◽  
Iekhsan Othman ◽  
Anuar Zaini ◽  
Ezharul Hoque Chowdhury
Keyword(s):  
Blood Glucose ◽  
Blood Glucose Level ◽  
Glucose Level ◽  
Insulin Aspart ◽  
Oral Delivery ◽  
Diabetic Rats ◽  
Duration Of Action ◽  
Wide Range ◽  
Ft Ir

Oral delivery is considered as the most preferred and yet most challenging mode of drug administration; especially a fragile and sensitive peptide like insulin that shows extremely low bioavailability through the gastro-intestinal (GIT) route. To address this problem, we have designed a novel drug delivery system (DDS) using precipitation-induced Barium (Ba) salt particles. The DDS can load insulin molecules and transport them through the GIT route. There were several in vitro simulation tests carried out to prove the efficiency of Ba salt particles as oral delivery candidates. All three Ba salt particles (BaSO4, BaSO3, and BaCO3) showed very good loading of insulin (>70% in all formulations) and a degree of resistance throughout a wide range of pHs from basic to acidic conditions when assessed by spectrophotometry. Particles and insulin-associated particles were morphologically assessed and characterized using FE-SEM and FT-IR. A set of tests were designed and carried out with mucin to predict whether the particles are potentially capable of overcoming one of the barriers for crossing intestinal epithelium. The mucin binding experiment demonstrated 60–100% of mucin adhesion to the three different particles. FT-IR identifies the characteristic peaks for mucin protein, particles, and particle-mucin complex re-confirming mucin adhesion to the particles. Finally, the effectiveness of nano-insulin was tested on streptozotocin (STZ) induced diabetic rats. A short acting human insulin analog, insulin aspart, was loaded into Ba salt particles at a dose of 100 IU/Kg prior to oral administration. Among the three formulations, insulin aspart-loaded BaSO4 and BaCO3 particles dramatically reduced the existing hyperglycemia. BaSO4 with loaded Insulin showed an onset of glucose-lowering action within 1 hr, with blood glucose level measured significantly lower compared to the 2nd and 3rd h (p < 0.05). Insulin-loaded BaCO3 particles showed a significant decrease in blood glucose level at 1–2 h, although the glucose level started to show a slight rise at 3rd h and by 4th h, it was back to baseline level. However, although BaSO3 particles with loaded insulin showed a trend of reduction in blood glucose level, the reduction was not found to be significant (p < 0.05) at any point in time. Therefore, oral formulations of insulin/BaSO4 and insulin/BaCO3 particles were observed as effective as native insulin aspart subcutaneous formulation in terms of onset and duration of action. Further investigation will be needed to reveal bioavailability and mechanism of action of this novel Nano-Insulin formulations.

scholarly journals Haemocompatibility Of Non-Functionalized And Plasmachemical Functionalized Detonation Nanodiamond Particles

2015 ◽  
Vol 60 (3) ◽  
pp. 2183-2189 ◽  
Author(s):  
K. Mitura ◽  
M. Jedrzejewska-Szczerska ◽  
P. Ceynowa ◽  
M. Dudek ◽  
M. Cicha ◽  
...  
Keyword(s):  
Microwave Plasma ◽  
Chemical Vapour ◽  
Detonation Nanodiamond ◽  
Innovative Design ◽  
Materials Research ◽  
Detonation Method ◽  
Biological Tests ◽  
Ft Ir ◽  
Rotary Reactor

AbstractThe purpose of this paper is to present the innovative design of microwave plasma system for modification of detonation nanodiamond particles (DNP) using a special rotating drum placed inside the reactor. Nanodiamond particles manufactured by detonation method reveal the biological activity depending on surface functionalization. Plasmachemical modification of detonation nanodiamond particles gives the possibility of controlling surface of nanodiamonds particles in biological tests. In this paper we would like to compare detonation nanodiamond (the grain sizes from 2 to 5 nm) with modified detonation nanodiamond in rotary reactor chamber, by microwave plasma activated chemical vapour deposition (MW PACVD) method in materials research (Raman and FT-IR spectroscopy) and in vitro examinations with full of human blood. The results indicate haemocompatibility of non-modified detonation nanodiamond and modified nanodiamond by MW PACVD method in rotary reactor chamber (modifiedND-3) and the presence of haemolysis in commercial detonation nanodiamond.

scholarly journals Preparation, Characterization, and Antimicrobial Activities of Bimetallic Complexes of Sarcosine with Zn(II) and Sn(IV)

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Yasir Arafat ◽  
Saqib Ali ◽  
Saira Shahzadi ◽  
Muhammad Shahid
Keyword(s):  
Elemental Analysis ◽  
Zinc Acetate ◽  
Room Temperature ◽  
Antimicrobial Activities ◽  
Molar Ratio ◽  
Heterobimetallic Complexes ◽  
Nmr Data ◽  
Ft Ir ◽  
Coordinate Geometry

Heterobimetallic complexes of Zn(II) and Sn(IV) with sarcosine have been synthesized at room temperature under stirring conditions by the reaction of sarcosine and zinc acetate in 2 : 1 molar ratio followed by the stepwise addition of CS2and organotin(IV) halides, where R = Me,n-Bu, and Ph. The complexes were characterized by elemental analysis, FT-IR and NMR (1H,13C) spectroscopy. IR data showed that the ligand acts in a bidentate manner. NMR data revealed the four coordinate geometry in solution state.In vitroantimicrobial activities data showed that complexes (3) and (4) were effective against bacterial and fungal strains with few exceptions.

scholarly journals Imidazole-Thiosemicarbazide Derivatives as Potent Anti-Mycobacterium tuberculosis Compounds with Antibiofilm Activity

Cells ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 3476
Author(s):  
Adrian Bekier ◽  
Malwina Kawka ◽  
Jakub Lach ◽  
Jarosław Dziadek ◽  
Agata Paneth ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Biofilm Formation ◽  
Bacterial Infections ◽  
Effective Vaccine ◽  
Antibiofilm Activity ◽  
Intracellular Growth ◽  
Expensive Drug ◽  
Cytotoxicity Studies ◽  
Thiosemicarbazide Derivatives

Mycobacterium tuberculosis (Mtb) is an intracellular pathogenic bacterium and the causative agent of tuberculosis. This disease is one of the most ancient and deadliest bacterial infections, as it poses major health, social and economic challenges at a global level, primarily in low- and middle-income countries. The lack of an effective vaccine, the long and expensive drug therapy, and the rapid spread of drug-resistant strains of Mtb have led to the re-emergence of tuberculosis as a global pandemic. Here, we assessed the in vitro activity of new imidazole-thiosemicarbazide derivatives (ITDs) against Mtb infection and their effects on mycobacterial biofilm formation. Cytotoxicity studies of the new compounds in cell lines and human monocyte-derived macrophages (MDMs) were performed. The anti-Mtb activity of ITDs was evaluated by determining minimal inhibitory concentrations of resazurin, time-kill curves, bacterial intracellular growth and the effect on biofilm formation. Mutation frequency and whole-genome sequencing of mutants that were resistant to ITDs were performed. The antimycobacterial potential of ITDs with the ability to penetrate Mtb-infected human macrophages and significantly inhibit the intracellular growth of tubercle bacilli and suppress Mtb biofilm formation was observed.

Synthesis and Antituberculotic Activity of 5-Alkyl-6-chloro-2-pyrazinecarboxamides and Corresponding Thioamides

1996 ◽  
Vol 61 (7) ◽  
pp. 1109-1114 ◽  
Author(s):  
Jiří Hartl ◽  
Martin Doležal ◽  
Jana Krinková ◽  
Antonín Lyčka ◽  
Želmíra Odlerová
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Elemental Analysis ◽  
Nmr Spectra ◽  
Antimycobacterial Activity ◽  
Partial Hydrolysis ◽  
Alkanoic Acid ◽  
H Nmr ◽  
Homolytic Alkylation ◽  
Lawesson's Reagent

Homolytic alkylation of 6-chloro-2-pyrazinecarbonitrile by alkanoic acid and subsequent partial hydrolysis afforded 5-alkyl-6-chloro-2-pyrazinecarboxamides 1a-1e. Reaction of amides 1a-1e by Lawesson's reagent afforded corresponding thioamides 2a-2e. The structure of compounds was confirmed by elemental analysis, IR and 1H NMR spectra. The assessment of in vitro antimycobacterial activity of the compounds was carried out. The highest antituberculotic activity against Mycobacterium tuberculosis and other mycobacterial strains in this series was shown by 5-(1,1-dimethylethyl)-6-chloro-2-pyrazinecarbothioamide (2e).

scholarly journals Biosynthesized silver nanoparticles using Ulva lactuca as a safe synthetic pesticide (in vitro)

2020 ◽  
Vol 5 (1) ◽  
pp. 291-299
Author(s):  
Hadear Hanie Amin
Keyword(s):  
Silver Nanoparticles ◽  
Ulva Lactuca ◽  
Biological Synthesis ◽  
Agricultural Crops ◽  
Ag Nps ◽  
Wide Range ◽  
Synthetic Pesticide ◽  
Ft Ir ◽  
Bacteria And Fungi

AbstractIn this era, we must synthesize safe pesticides from inexpensive sources to avoid the diseases caused by most of the previously used pesticides. Therefore, nanotechnology was used to produce biologically synthesis pesticides from very cheap sources such as seaweed, especially green algae, as it is safe to synthesize a pesticide against various pests such as bacteria and fungi that affect various agricultural crops. Ulva lactuca is used for the biosynthesis of silver nanoparticles by a bottom-up bioreduction reaction of silver nitrate to silver nanoparticles (Ag-NPs) observed by the formation of brown color. The biosynthesis reaction has been proven by using UV-VIS, FT-IR, EDAX, SEM, TEM, and DSC-TGA and has been tested against a wide range of bacteria and fungi that affect plants, poultry, fish, rabbits, animals, and humans. Antioxidant activity was also determined. Silver nanoparticles (Ag-NPs) have proven to be good and safe synthetic pesticides. The results of the spectroscopy demonstrated the success of the biological synthesis of the pesticide. Also, the results of the antimicrobial activity demonstrated the success of the pesticide that was biologically synthesized to fight bacteria and fungi that cause different diseases of different agricultural crops and should be used as a safe synthetic pesticide.

scholarly journals Synthesis and Characterization of New Selenonitrone Derivative and Its Effect on Breast Cancer Cell Line Viability in Vitro

2019 ◽  
Vol 16 (3(Suppl.)) ◽  
pp. 0754
Author(s):  
Haddad Et al.
Keyword(s):  
Breast Cancer ◽  
Elemental Analysis ◽  
Carbonyl Compounds ◽  
Spectroscopic Data ◽  
Breast Cancer Cells ◽  
Cancer Cell Line ◽  
Ft Ir ◽  
The Times

          New nitrone and selenonitrone compounds were synthesized. The condensation method between N-(2-hydroxyethyl) hydroxylamine and substituted carbonyl compounds such as [benzil, 4, 4́-dichlorobenzil and  2,2́ -dinitrobenzil] afforded a variety of new nitrone compounds while the condensation between N-benzylhydroxylamine and substituted selenocarbonyl compounds such as [di(4-fluorobenzoyl) diselenide and (4-chlorobenzoyl selenonitrile] obtained selenonitrone compounds. The condensation of N-4-chlorophenylhydroxylamine with dibenzoyl diselenide obtained another type of selenonitrone compounds. The structures of the synthesized compounds were assigned based on spectroscopic data (FT-IR, 1H-NMR, 13C-NMR, MS and elemental analysis. The result spectra and the result of elemental analysis were verified the expected structure. The results of new selenonitron derivative (N1) effect on the MDA-MB-231 breast cancer cells in vitro revealed that is an increase in the proliferation of cells with increased concentrations of selenonitron at all periods of the times.

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