Syntheses, Structures, and Antimicrobial Activity of New Remarkably Light-Stable and Water-Soluble Tris(pyrazolyl)methanesulfonate Silver(I) Derivatives of N-Methyl-1,3,5-triaza-7-phosphaadamantane Salt - [mPTA]BF4

2014 ◽  
Vol 54 (2) ◽  
pp. 434-440 ◽  
Author(s):  
Piotr Smoleński ◽  
Claudio Pettinari ◽  
Fabio Marchetti ◽  
M. Fátima C. Guedes da Silva ◽  
Giulio Lupidi ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Water Soluble ◽  
Derivatives Of

scholarly journals Quaternary Salts of Chitosan: History, Antimicrobial Features, and Prospects

2011 ◽  
Vol 2011 ◽  
pp. 1-12 ◽  
Author(s):  
Douglas de Britto ◽  
Rejane Celi Goy ◽  
Sergio Paulo Campana Filho ◽  
Odilio B. G. Assis
Keyword(s):  
Physical Chemistry ◽  
Antimicrobial Activity ◽  
Drug Delivery Systems ◽  
Antimicrobial Properties ◽  
Water Soluble ◽  
Chemical Characteristics ◽  
Packaging Materials ◽  
Inhibitory Effects ◽  
Quaternary Salts ◽  
Derivatives Of

Recently, increasing attention has been paid to water-soluble derivatives of chitosan at its applications. The chemical characteristics and the antimicrobial properties of these salts can play significant role in pharmacological and food areas mainly as carriers for drug delivery systems and as antimicrobial packaging materials. In the current paper, a historical sequence of the main preparative methods, physical chemistry aspects, and antimicrobial activity of chitosan quaternized derivatives are presented and briefly discussed. In general, the results indicated that the quaternary derivatives had better inhibitory effects than the unmodified chitosan.

QSAR Analysis of Selected Antimicrobial Structures Belonging to Nitro-derivatives of Heterocyclic Compounds

2020 ◽  
Vol 17 (2) ◽  
pp. 214-225 ◽  
Author(s):  
Piotr Kawczak ◽  
Leszek Bober ◽  
Tomasz Bączek
Keyword(s):  
Antimicrobial Activity ◽  
Heterocyclic Compounds ◽  
Molecular Descriptors ◽  
Microbiological Activity ◽  
Activity Data ◽  
Qsar Analysis ◽  
Qsar Models ◽  
Nitro Derivatives ◽  
Semi Empirical ◽  
Derivatives Of

Background: Nitro-derivatives of heterocyclic compounds were used as active agents against pathogenic microorganisms. A set of 4- and 5-nitroimidazole derivatives exhibiting antimicrobial activity was analyzed with the use of Quantitative Structure-Activity Relationships (QSAR) method. The study included compounds used both in documented treatment and those described as experimental. Objective: The purpose of this study was to demonstrate the common and differentiating characteristics of the above-mentioned chemical compounds alike physicochemically as well as pharmacologically based on the quantum chemical calculations and microbiological activity data. Methods: During the study PCA and MLR analysis were performed, as the types of proposed chemometric approach. The semi-empirical and ab initio level of in silico molecular modeling was performed for calculations of molecular descriptors. Results: QSAR models were proposed based on chosen descriptors. The relationship between the nitro-derivatives structure and microbiological activity data was able to class and describe the antimicrobial activity with the use of statistically significant molecular descriptors. Conclusion: The applied chemometric approaches revealed the influential features of the tested structures responsible for the antimicrobial activity of studied nitro-derivatives.

Potential anticonvulsants: Substituted N-benzylidene derivatives of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins

1983 ◽  
Vol 48 (4) ◽  
pp. 1173-1186 ◽  
Author(s):  
Václav Bártl ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Marie Bartošová ◽  
Miroslav Protiva
Keyword(s):  
Acute Toxicity ◽  
Water Soluble ◽  
Hypotensive Activity ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Soluble Salts ◽  
Sleeping Time ◽  
Central Depression ◽  
Derivatives Of ◽  
Electroshock Seizures

Reactions of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins XIVa-XIVd with benzaldehyde, 3,4-dimethoxybenzaldehyde, 4-dimethylaminobenzaldehyde, salicylaldehyde, 3-ethoxy-4-hydroxybenzaldehyde, 2-(2-dimethylaminoethoxy)benzaldehyde, 3-(2-dimethylaminoethoxy)benzaldehyde and 3-ethoxy-4-(2-dimethylaminoethoxy)benzaldehyde afforded a series of 19 hydrazones IIIa-Xc. Some of them showed the expected anticonvulsant effect but only towards pentetrazole; antagonism of maximal electroshock seizures was not observed. In general, the products have a character of tranquillizers: in higher does they produce central depression, potentiate the thiopental sleeping time, have hypothermic action; in single cases antiamphetamine, antireserpine, antihistamine and cataleptic effects were observed. The water-soluble salts of the basic hydrazones VIIIa, VIIIc, IXc and Xc, administered parenterally, showed a rather high acute toxicity and revealed also adrenolytic and hypotensive activity.

scholarly journals Antioxidant Network Based on Sulfonated Polyhydroxyalkanoate and Tannic Acid Derivative

2021 ◽  
Vol 8 (1) ◽  
pp. 9
Author(s):  
Laura Brelle ◽  
Estelle Renard ◽  
Valerie Langlois
Keyword(s):  
Gallic Acid ◽  
Tannic Acid ◽  
Water Soluble ◽  
Gel Formation ◽  
Ene Reaction ◽  
Inorganic Cations ◽  
Medium Chain Length ◽  
Physically Crosslinked ◽  
The Stability ◽  
Derivatives Of

A novel generation of gels based on medium chain length poly(3-hydroxyalkanoate)s, mcl-PHAs, were developed by using ionic interactions. First, water soluble mcl-PHAs containing sulfonate groups were obtained by thiol-ene reaction in the presence of sodium-3-mercapto-1-ethanesulfonate. Anionic PHAs were physically crosslinked by divalent inorganic cations Ca2+, Ba2+, Mg2+ or by ammonium derivatives of gallic acid GA-N(CH3)3+ or tannic acid TA-N(CH3)3+. The ammonium derivatives were designed through the chemical modification of gallic acid GA or tannic acid TA with glycidyl trimethyl ammonium chloride (GTMA). The results clearly demonstrated that the formation of the networks depends on the nature of the cations. A low viscoelastic network having an elastic around 40 Pa is formed in the presence of Ca2+. Although the gel formation is not possible in the presence of GA-N(CH3)3+, the mechanical properties increased in the presence of TA-N(CH3)3+ with an elastic modulus G’ around 4200 Pa. The PHOSO3−/TA-N(CH3)3+ gels having antioxidant activity, due to the presence of tannic acid, remained stable for at least 5 months. Thus, the stability of these novel networks based on PHA encourage their use in the development of active biomaterials.

scholarly journals Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

2021 ◽  
Vol 11 (3) ◽  
pp. 1180
Author(s):  
Kinga Paruch ◽  
Łukasz Popiołek ◽  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Malm ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acid ◽  
Bacterial Infections ◽  
Acid Hydrazide ◽  
Antimicrobial Effect ◽  
In Vitro Antimicrobial Activity ◽  
Research Goal ◽  
New Compounds ◽  
Derivatives Of

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

Antimicrobial activity of piperazine derivatives of chitosan

2008 ◽  
Vol 74 (3) ◽  
pp. 566-571 ◽  
Author(s):  
Már Másson ◽  
Jukka Holappa ◽  
Martha Hjálmarsdóttir ◽  
Ögmundur V. Rúnarsson ◽  
Tapio Nevalainen ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Piperazine Derivatives ◽  
Derivatives Of

scholarly journals Synthesis and biological activity of 4-thiazolidinone derivatives of phenothiazine

2012 ◽  
Vol 77 (1) ◽  
pp. 17-26 ◽  
Author(s):  
Ritu Sharma ◽  
Pushkal Samadhiya ◽  
Savitri Srivastava ◽  
Santosh Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Heterocyclic Compounds ◽  
Thioglycolic Acid ◽  
Cycloaddition Reaction ◽  
Aromatic Aldehydes ◽  
Knoevenagel Reaction ◽  
Antituberculosis Activity ◽  
Bacteria And Fungi ◽  
Derivatives Of ◽  
Anhydrous Zncl2

A new series of N-[3-(10H-phenothiazinyl)-propyl]-2-(substituted phenyl)-4-oxo-5-( substituted benzylidene)-1,3-thiazolidine-carboxamide, 5(as) have been synthesized. The cycloaddition reaction of thioglycolic acid with N-[3-(10H-phenothiazinyl)-propyl]-N?-[(substituted phenyl)-methylidene]- urea, 3(a-s) in the presence of anhydrous ZnCl2 afforded new heterocyclic compounds N-[3-(10H-phenothiazinyl)-propyl]-2-(substituted phenyl)-4-oxo- 1,3-thiazolidine-carboxamide, 4(a-s). The later product on treatment with several selected substituted aromatic aldehydes in the presence of C2H5ONa undergoes Knoevenagel reaction to yield 5(a-s). The structure of compounds 1, 2, 3(a-s), 4(a-s) and 5(a-s) were confirmed by IR, 1H NMR, 13C NMR, Fmass and chemical analysis. All above compounds were screened for their antimicrobial activity against some selected bacteria and fungi and for antituberculosis activity compounds have been screened against the bacterium M. tuberculosis.

1,3-dipolar cycloaddition in the synthesis of glycoconjugates of natural chlorins and bacteriochlorins

2009 ◽  
Vol 13 (03) ◽  
pp. 336-345 ◽  
Author(s):  
Mikhail A. Grin ◽  
Ivan S. Lonin ◽  
Anna A. Lakhina ◽  
Elena S. Ol'shanskaya ◽  
Alexey I. Makarov ◽  
...  
Keyword(s):  
Triple Bond ◽  
Tautomeric Form ◽  
Click Reaction ◽  
Copper Cation ◽  
Water Soluble ◽  
Dipolar Cycloaddition ◽  
Nmr Studies ◽  
Metal Free ◽  
Cu Complex ◽  
Derivatives Of

Glucose-, galactose- and lactose-containing photosensitizers based on derivatives of chlorophyll a and bacteriochlorophyll a were synthesized with the use of [3+2] cycloaddition between sugar azides and triple bond derivatives of chlorins and bacteriochlorins. Unlike bacteriochlorin cycloimide, chlorin was detected to form a Cu -complex during the click reaction. An approach to the synthesis of metal-free glycosylated chlorins was developed with the use of "protection" by Zn 2+ cation and subsequent demetalation. It is based on the action of alkynyl chlorin e6 derivative Zn -complex, which is resistant to the substitution by copper cation. Bacteriochlorin p cycloimide conjugate with per-acetylated β-D-lactose was obtained and shown to become water-soluble after unblocking of the lactose hydroxy functions. NMR studies allowed for the elucidation of structure, tautomeric form and conformation of the obtained compounds.

Synthesis and antimicrobial activity of certain derivatives of N-substituted pyrrolidones and pyrrolidines

1982 ◽  
Vol 16 (1) ◽  
pp. 44-47 ◽  
Author(s):  
V. A. Sedavkina ◽  
N. A. Morozova ◽  
V. F. Chulkov ◽  
L. K. Kulikova
Keyword(s):  
Antimicrobial Activity ◽  
Derivatives Of

Esters, amides and substituted derivatives of cinnamic acid: synthesis, antimicrobial activity and QSAR investigations

2004 ◽  
Vol 39 (10) ◽  
pp. 827-834 ◽  
Author(s):  
Balasubramanian Narasimhan ◽  
Deepak Belsare ◽  
Devayani Pharande ◽  
Vishnukant Mourya ◽  
Avinash Dhake
Keyword(s):  
Antimicrobial Activity ◽  
Cinnamic Acid ◽  
Acid Synthesis ◽  
Derivatives Of
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