scholarly journals Synthesis of the 4’-desmethoxy analogue of RU79115

2004 ◽  
Vol 69 (11) ◽  
pp. 855-859 ◽  
Author(s):  
Branislav Musicki ◽  
Anne-Marie Periers ◽  
Nicole Tessot ◽  
Michel Klich
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Inhibitory Activity ◽  
Methoxy Group

The synthesis, and biological activity in vitro of the 4?-desmethoxy analogue (3) of RU 79115 (2) is described. Comparison of the biological activity of the two analogues clearly indicated the importance of the 4?-methoxy group in conferring good gyrase B inhibitory activity as well as antibacterial activity.

scholarly journals Studies on the .ALPHA.-glucoside hydrolase inhibitor, adiposin. III. .ALPHA.-Glucoside hydrolase inhibitory activity and antibacterial activity in vitro.

1982 ◽  
Vol 35 (9) ◽  
pp. 1160-1166 ◽  
Author(s):  
KUNIO KANGOURI ◽  
SHINJURO NAMIKI ◽  
TAKATOSHI NAGATE ◽  
HIROSHI HARA ◽  
KAZUHIKO SUGITA ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity

scholarly journals A New Monoterpenoid and a New Flavonoid Glycoside from the Peels of Clausena lansium

2016 ◽  
Vol 11 (5) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Hui-Dong Deng ◽  
Cai-Hong Cai ◽  
Shuai Liu ◽  
Yan-Bo Zeng ◽  
Wen-Li Mei ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Carboxylic Acid ◽  
Inhibitory Activity ◽  
2D Nmr ◽  
Flavonoid Glycoside ◽  
Esi Ms ◽  
Inhibition Zones

One new monoterpenoid, nerol oxide-8-carboxylic acid (1), and one new flavonoid glycoside, claulansoside A (2), together with six known compounds, clausenamide (3), quercetin (4), isorhamnetin (5), dihydromyric (6), 2′',3′'-dihydroxyanisolactone (7) and ( E,E)-8-(7-hydroxy-3,7-dimethylocta-2,5-dienyloxy)psoralen (8), have been isolated from the peels of Clausena lansium (Lour.) Skeels. Their structures were determined using a combination of 1D, and 2D NMR (HMQC, HMBC, COSY and NOESY) techniques, and HR-ESI-MS analyses. Compounds 1 and 7 exhibited antibacterial activity against Staphylococcus aureus with the diameter of inhibition zones of 11.5 mm and 14.2 mm. Compounds 3 and 6 showed α-glucosidase inhibitory activity in vitro.

Computational Druglikeness Assessment, Synthesis, Characterization and in vitro Biological Activity Evaluation of some Novel Mixed Metal Complexes of 2-(butan-2-ylidene) hydrazinecarbothioamide

2020 ◽  
Vol 23 ◽  
Author(s):  
Tahmeena Khan ◽  
Iqbal Azad ◽  
Alfred J. Lawrence ◽  
Saman Raza ◽  
Seema Joshi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Molecular Docking ◽  
Metal Complexes ◽  
Docking Studies ◽  
Mixed Metal ◽  
Ic50 Value ◽  
Mixed Metal Complexes ◽  
Mcf 7

Aims and Objectives: The heteronuclear (mixed metal) complexes of Schiff bases have been explored as part of the coordination and bioinorganic chemistry. Five novel mixed metal complexes of (E)-2-(butan-2-ylidene) hydrazinecarbothioamide (2-butanone thiosemicarbazone) were prepared and characterized by different spectroscopic techniques. Molecular docking studies were performed with three proteins for two complexes. The toxicity potential, physicochemical properties and bioactivity scores were also predicted. The complexes were tested against three cell lines and also evaluated for their antibacterial activity. Materials and Methods: The mixed metal complexes were prepared in 1:4 molar ratio of metal salt and ligand. OSIRIS 4.6.1 was used to assess the toxicity whereas Molinspiration 2016.03 was used to calculate the bioactivity scores and other physicochemical properties. Principal Component Analysis (PCA) was performed using the Osiris Property Explorer 4.5.1 for defining and visualizing multidimensional property spaces by assigning dimensions to numerical descriptors. Molecular docking studies were performed with three proteins. The anticancer activity was tested against MCF-7, MDA-MB-231, HepG2 and A549 cell lines using MTT assay whereas antibacterial activity was tested using disc diffusion method. Results and Conclusion: The melting points of the complexes were as high as >3500C, indicating high thermal stability. [CuZn(C5H11N3S)4(SO4)2] exhibited minimum energies against the selected proteins. The bioactivity scores of the complexes were between -0.50 and 0.0. All the prepared complexes showed negative Ames score predicted their non-carcinogenic nature. Against A549 [CuZn(C5H11N3S)4(SO4)2], [CoZn(C5H11N3S)4(SO4)Cl2] and [FeZn(C5H11N3S)4(SO4)2] showed potential in vitro activity. IC50 of these three complexes were 19.69, 37.73 and 38.4 respectively. Against MCF-7, [FeCu(C5H11N3S)4(SO4)2] had IC50 value 53.5. Whereas, against HepG2 [CoZn(C5H11N3S)4(SO4)Cl2] was active having IC50 value 61.8. [CoZn(C5H11N3S)4(SO4)Cl2], [FeCu(C5H11N3S)4(SO4)2] and [FeCo(C5H11N3S)4(SO4)Cl2] were active against S. aureus in the concentration range 2-20 mg/mL. The complexes showed improved biological activity as compared to the monometallic complexes of the same ligand.

Synthesis and In Vitro Biological Activity Evaluation of Novel Imidazo [2,1-B][1,3,4] Thiadiazole as Anti-Alzheimer Agents

2020 ◽  
Vol 17 (5) ◽  
pp. 610-617
Author(s):  
Sara Azimi ◽  
Omidreza Firuzi ◽  
Aida Iraji ◽  
Afsaneh Zonouzi ◽  
Mahsima Khoshneviszadeh ◽  
...  
Keyword(s):  
Biological Activity ◽  
Inhibitory Activity ◽  
Phenyl Ring ◽  
Activity Evaluation ◽  
Butyryl Cholinesterase ◽  
Thiadiazole Derivatives ◽  
Derivatives Of

Background: Considering that AD is multifactorial in nature, novel series of imidazo [2,1-b][1,3,4] thiadiazole derivatives were designed to address the basic factors responsible for the disease. <p> Methods: These compounds were investigated as inhibitors of beta-site APP cleaving enzyme 1, acetylcholinesterase and butyryl cholinesterase. <p> Results: The BACE1 inhibitory results indicated that nitro phenyl substituted derivatives of imidazo [2,1-b][1,3,4] thiadiazole scaffold (R2 = m-NO2) demonstrated superior BACE1 inhibitory activity compared to other substituted moieties. In the BuChE assay, compounds 4h and 4l carrying meta NO2 at R2 of phenyl ring turned out to be potent inhibitors. <p> Conclusion: In conclusion, these novel synthesized derivatives seem to be promising anti-Alzheimer agents.

scholarly journals Contributions of the 8-Methoxy Group of Gatifloxacin to Resistance Selectivity, Target Preference, and Antibacterial Activity against Streptococcus pneumoniae

2001 ◽  
Vol 45 (6) ◽  
pp. 1649-1653 ◽  
Author(s):  
Hideyuki Fukuda ◽  
Ryuta Kishii ◽  
Masaya Takei ◽  
Masaki Hosaka
Keyword(s):  
Antibacterial Activity ◽  
Streptococcus Pneumoniae ◽  
Type Strain ◽  
Methoxy Group ◽  
Wild Type Strain ◽  
Dna Gyrase ◽  
Wild Type ◽  
Topoisomerase Iv ◽  
Mutant Strains

ABSTRACT Gatifloxacin (8-methoxy, 7-piperazinyl-3′-methyl) at the MIC selected mutant strains that possessed gyrA mutations at a low frequency (3.7 × 10−9) from wild-type strainStreptococcus pneumoniae IID553. AM-1147 (8-methoxy, 7-piperazinyl-3′-H) at the MIC or higher concentrations selected no mutant strains. On the other hand, the respective 8-H counterparts of these two compounds, AM-1121 (8-H, 7-piperazinyl-3′-methyl) and ciprofloxacin (8-H, 7-piperazinyl-3′-H), at one and two times the MIC selected mutant strains that possessed parC mutations at a high frequency (>2.4 × 10−6). The MIC of AM-1147 increased for the gyrA mutant strains but not for theparC mutant strains compared with that for the wild-type strain. These results suggest that fluoroquinolones that harbor 8-methoxy groups select mutant strains less frequently and prefer DNA gyrase, as distinct from their 8-H counterparts. The in vitro activities of gatifloxacin and AM-1147 are twofold higher against the wild-type strain, eight- and twofold higher against the first-stepparC and gyrA mutant strains, respectively, and two- to eightfold higher against the second-step gyrA andparC double mutant strains than those of their 8-H counterparts. These results indicate that the 8-methoxy group contributes to enhancement of antibacterial activity against target-altered mutant strains as well as the wild-type strain. It is hypothesized that the 8-methoxy group of gatifloxacin increases the level of target inhibition, especially against DNA gyrase, so that it is nearly the same as that for topoisomerase IV inhibition in the bacterial cell, leading to potent antibacterial activity and a low level of resistance selectivity.

The prediction of the spectrum of biological activity and antimicrobial properties of diaminoazoles

2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Antimicrobial Properties ◽  
Biological Properties ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Wide Range ◽  
Alternative Drugs

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.

scholarly journals Correlations between the lipophilicity and the inhibitory activity of different substituted benzimidazoles

2009 ◽  
Vol 15 (3) ◽  
pp. 125-130 ◽  
Author(s):  
Sanja Podunavac-Kuzmanovic ◽  
Dragoljub Cvetkovic ◽  
Dijana Barna
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Theoretical Models ◽  
Qsar Model ◽  
Calibration Model ◽  
Complete Regression ◽  
Statistical Parameters ◽  
High Agreement ◽  
Office Software

2-Amino and 2-methylbenzimidazole derivatives were tested in vitro for their inhibitory activity against the bacteria Bacillus cereus. The minimum inhibitory concentration (MIC) was determined for all compounds. The lipophilicity descriptors were calculated by using CS Chem-Office Software, version 7.0. The stepwise regression method was used to derive the most significant model as a calibration model for predicting the antibacterial activity of this class of compounds. A complete regression analysis resorting to linear and quadratic relationships was made. Theoretical models were validated by leaving one out (LOO) technique, as well as by the calculation of statistical parameters for the established models. The best QSAR model for the prediction of an inhibitory activity of the investigated series of benzimidazoles was developed. A high agreement between the experimental and predicted inhibitory values was obtained. The results indicated that the antibacterial activity could be modeled using the lipophilicity descriptor.

scholarly journals Discovery of novel antituberculosis agents among 3-phenyl-5-(1-phenyl-1H-[1,2,3]triazol-4-yl)-[1,2,4]oxadiazole derivatives targeting aminoacyl-tRNA synthetases

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Mariia Yu. Rybak ◽  
Anatoliy O. Balanda ◽  
Anna P. Yatsyshyna ◽  
Igor. M. Kotey ◽  
Sergiy A. Starosyla ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Molecular Targets ◽  
Trna Synthetase ◽  
Biological Research ◽  
Antibiotic Development ◽  
Antibacterial Screening ◽  
Oxadiazole Derivatives ◽  
Resistant Strains

AbstractAntibiotic resistance is a major problem of tuberculosis treatment. This provides the stimulus for the search of novel molecular targets and approaches to reduce or forestall resistance emergence in Mycobacterium tuberculosis. Earlier, we discovered a novel small-molecular inhibitor among 3-phenyl-5-(1-phenyl-1H-[1,2,3]triazol-4-yl)-[1,2,4]oxadiazoles targeting simultaneously two enzymes—mycobacterial leucyl-tRNA synthetase (LeuRS) and methionyl-tRNA synthetase (MetRS), which are promising molecular targets for antibiotic development. Unfortunately, the identified inhibitor does not reveal antibacterial activity toward M. tuberculosis. This study aims to develop novel aminoacyl-tRNA synthetase inhibitors among this chemical class with antibacterial activity toward resistant strains of M. tuberculosis. We performed molecular docking of the library of 3-phenyl-5-(1-phenyl-1H-[1,2,3]triazol-4-yl)-[1,2,4]oxadiazole derivatives and selected 41 compounds for investigation of their inhibitory activity toward MetRS and LeuRS in aminoacylation assay and antibacterial activity toward M. tuberculosis strains using microdilution assay. In vitro screening resulted in 10 compounds active against MetRS and 3 compounds active against LeuRS. Structure-related relationships (SAR) were established. The antibacterial screening revealed 4 compounds active toward M. tuberculosis mono-resistant strains in the range of concentrations 2–20 mg/L. Among these compounds, only one compound 27 has significant enzyme inhibitory activity toward mycobacterial MetRS (IC50 = 148.5 µM). The MIC for this compound toward M. tuberculosis H37Rv strain is 12.5 µM. This compound is not cytotoxic to human HEK293 and HepG2 cell lines. Therefore, 3-phenyl-5-(1-phenyl-1H-[1,2,3]triazol-4-yl)-[1,2,4]oxadiazole derivatives can be used for further chemical optimization and biological research to find non-toxic antituberculosis agents with a novel mechanism of action.

scholarly journals In vitro Antibacterial Activities of Honey Bee Extracts against Bacterial Isolates of Wound Infections

2021 ◽  
pp. 20-25
Author(s):  
O. A. Ayodele ◽  
J. O. Aribisala ◽  
A. T. Oseni ◽  
M. K. Oladunmoye
Keyword(s):  
Antibacterial Activity ◽  
Honey Bee ◽  
Honey Bees ◽  
Inhibitory Activity ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Diffusion Method ◽  
Wound Infections ◽  
Zones Of Inhibition

Microorganisms most especially bacteria, continue to develop resistance against antimicrobial agents; hence novel sources of antibiotics are urgently needed to reduce this problem. This study was carried out to investigate the antibacterial activities of ethanolic, chloroform and aqueous extracts of Apis mellifera (honey bee) on isolates of wound infections. The isolates used in this study were procured from University of Ilorin Teaching Hospital (UITH) and confirmed using morphological and biochemical tests. The isolates used include; Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pnuemoniae, Proteus mirabilis and Proteus vulgaris. Honey bees were collected from an apitherapist at Sunshine honey and agro foods, Akure, Ondo State Nigeria. The whole insect was used for in vitro antibacterial evaluation of the isolates using agar well diffusion method. Ethanolic extract of A. mellifera had the highest inhibitory activity with mean zones of inhibition ranging from 7.40 mm to 21.67 mm, chloroform extracts had moderate inhibitory activity ranging from 4.63 mm to 10.03 mm while the aqueous extract had the least activity with zones of inhibition ranging from 3.00 mm to 6.30 mm. However, no antibacterial activity was observed against P. aeruginosa for all the extracts. It is concluded that extracts of honey bees most especially the ethanolic extract have antibacterial activity and thus could be a potential antibacterial agent against isolates of wound infections.

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