Unfused heterobicycles as amplifiers of phleomycin. I. Some pyridinyl- and pyrazolyl-pyrimidines, bithiazoles and thiazolylpyridines

1980 ◽  
Vol 33 (10) ◽  
pp. 2291 ◽  
Author(s):  
DJ Brown ◽  
WB Cowden ◽  
GW Grigg ◽  
D Kavulak
Keyword(s):  
Escherichia Coli ◽  
Biological Activities ◽  
In Vitro Cultures ◽  
Derivatives Of

Syntheses are reported for some simple derivatives of 2-(pyridin-2'- yl)pyrimidine; 4-(pyrazol-1'- yl)pyrimidine; 4-(pyrazol-4'- yl)pyrimidine; 4,5'-bithiazole; 2-, 3-, and 4-(thiazol-4'-yl)pyridine and 2-, 3-, and 4-(thiazol-2'-yl)pyridine. Biological activities, as amplifiers of phleomycin against in vitro cultures of Escherichia coli, are tabulated and discussed.

Purine Analogues as Amplifiers of Phleomycin. V. Thioethers of Several Heterocyclic Systems with One or Two Rings

1979 ◽  
Vol 32 (12) ◽  
pp. 2713 ◽  
Author(s):  
DJ Brown ◽  
GW Grigg ◽  
Y Iwai ◽  
KN McAndrew ◽  
T Nagamatsu ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Biological Activities ◽  
In Vitro Cultures ◽  
Purine Analogues

Thioethers, appropriate for testing as amplifiers of phleomycin against in vitro cultures of Escherichia coli, are prepared via corresponding thiones in the purine, imidazo[4,5-b(and 4,5-c)]pyridine, pyrazolo[3,4-d]pyrimidine, quinazoline, benzothiazole, benzoxazole, pyrimidine, imidazole, thiazoline, 1,2,4-triazole, s-triazolo[4,3-c(and 1,5-c)]pyrimidine, oxazolo[4,5-b]pyridine, quinoline and 1,3,5-triazine series. Structures are confirmed by N.M.R. spectra. Biological activities are tabulated and discussed in terms of structure.

Purine analogues as amplifiers of phleomycin. III. Some 2-alkylthio derivatives of imidazole, benzimidazole, benzoxazole and benzothiazole

1978 ◽  
Vol 31 (2) ◽  
pp. 447 ◽  
Author(s):  
DJ Brown ◽  
WC Dunlap ◽  
GW Grigg ◽  
L Danckwerts
Keyword(s):  
Escherichia Coli ◽  
Maximal Activity ◽  
Purine Analogues ◽  
Derivatives Of

Some 2-methylthio and 2-carbamoylalkylthio derivatives of 1-methylimidazole, benzimidazole, benzoxazole, benzothiazole and 6-dimethylaminobenzothiazole have been synthesized by alkylation of the corresponding thiones. Their in vitro activities, as amplifiers of phleomycin against Escherichia coli, varied from slight to high but none was outstanding. 2-(Benzothiazol-2'-ylthio)acetamide (2j)showed maximal activity at c. 0.04 mM with progressive decreases at both higher and lower concentrations.

scholarly journals Biological Characterization of Endotoxins Released from Antibiotic-Treated Pseudomonas aeruginosa and Escherichia coli

1998 ◽  
Vol 42 (5) ◽  
pp. 1015-1021 ◽  
Author(s):  
Teruo Kirikae ◽  
Fumiko Kirikae ◽  
Shinji Saito ◽  
Kaoru Tominaga ◽  
Hirohi Tamura ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Pseudomonas Aeruginosa ◽  
Lipid A ◽  
Biological Activities ◽  
Polymyxin B ◽  
Mitogen Activated Protein Kinase ◽  
No Production ◽  
Endotoxic Activity

ABSTRACT The supernatants taken from Pseudomonas aeruginosa andEscherichia coli cultures in human sera or chemically defined M9 medium in the presence of ceftazidime (CAZ) contained high levels of endotoxin, while those taken from the same cultures in the presence of imipenem (IPM) yielded a very low level of endotoxin. The biological activities of endotoxin in the supernatants were compared with those of phenol water-extracted lipopolysaccharide (LPS). The endotoxin released from the organisms as a result of CAZ treatment (CAZ-released endotoxin) contained a large amount of protein. The protein, however, lacked endotoxic activity, since the endotoxin did not show any in vivo toxic effects in LPS-hyporesponsive C3H/HeJ mice sensitized with d-(+)-galactosamine (GalN) or any activation of C3H/HeJ mouse macrophages in vitro. The activities of CAZ- and IPM-released endotoxin (as assessed by a chromogenicLimulus test) were fundamentally the same as those ofP. aeruginosa LPS, since their regression lines were parallel. The CAZ-released endotoxin was similar to purified LPS with respect to the following biological activities in LPS-responsive C3H/HeN mice and LPS-hyporesponsive C3H/HeJ mice: lethal toxicity in GalN-sensitized mice, in vitro induction of tumor necrosis factor- and NO production by macrophages, and mitogen-activated protein kinase activation in macrophages. The macrophage activation by CAZ-released endotoxin as well as LPS was mainly dependent on the presence of serum factor and CD14 antigen. Polymyxin B blocked the activity. These findings indicate that the endotoxic activity of CAZ-released endotoxin is due primarily to LPS (lipid A).

scholarly journals The Search for New Antibacterial Agents among 1,2,3-Triazole Functionalized Ciprofloxacin and Norfloxacin Hybrids: Synthesis, Docking Studies, and Biological Activity Evaluation

2021 ◽  
Vol 90 (1) ◽  
pp. 2
Author(s):  
Halyna Hryhoriv ◽  
Illia Mariutsa ◽  
Sergiy M. Kovalenko ◽  
Victoriya Georgiyants ◽  
Lina Perekhoda ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Antibacterial Agents ◽  
Docking Studies ◽  
Synthetic Method ◽  
Bacillus Subtilis Atcc ◽  
Resistant Strains ◽  
Derivatives Of

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.

scholarly journals Chemical Composition of Nardostachys grandiflora Rhizome Oil from Nepal – A Contribution to the Chemotaxonomy and Bioactivity of Nardostachys

2015 ◽  
Vol 10 (6) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Prabodh Satyal ◽  
Bhuwan K. Chhetri ◽  
Noura S. Dosoky ◽  
Ambika Poudel ◽  
William N. Setzer
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Cytotoxic Activity ◽  
Biological Activities ◽  
Mcf 7

The essential oil from the dried rhizome of Nardostachys grandiflora, collected from Jaljale, Nepal, was obtained in 1.4% yield, and a total of 72 compounds were identified constituting 93.8% of the essential oil. The rhizome essential oil of N. grandiflora was mostly composed of calarene (9.4%), valerena-4,7(11)-diene (7.1%), nardol A (6.0%), 1(10)-aristolen-9-ol (11.6%), jatamansone (7.9%), valeranal (5.6%), and cis-valerinic acid (5.7%). The chemical composition of N. grandiflora rhizome oil from Nepal is qualitatively very different than those from Indian, Chinese, and Pakistani Nardostachys essential oils. In this study we have evaluated the chemical composition and biological activities of N. grandiflora from Nepal. Additionally, 1(10)-aristolen-9-ol was isolated and the structure determined by NMR, and represents the first report of this compound from N. grandiflora. N. grandiflora rhizome oil showed in-vitro antimicrobial activity against Bacillus cereus, Escherichia coli, and Candida albicans (MIC = 156 μg/mL), as well as in-vitro cytotoxic activity on MCF-7 cells.

scholarly journals Suzuki Reaction for the Synthesis of New Derivatives of 4-Chloro-3,5-Dimethyl Phenol and their in vitro Antibacterial Screening

2019 ◽  
Vol 31 (12) ◽  
pp. 2955-2958
Author(s):  
R.H. Zaooli ◽  
F.A. Hussein ◽  
N.N.A. Jafar ◽  
S.N.K. Al-Thamir
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Elemental Analysis ◽  
Proteus Mirabilis ◽  
Suzuki Reaction ◽  
Antibacterial Properties ◽  
Antibacterial Screening ◽  
Derivatives Of ◽  
Dimethyl Phenol

Many derivatives of 4-chloro-3,5-dimethylphenol have been synthesized using Suzuki reaction and characterized by IR, 1H NMR and micro elemental analysis. These compounds also tested in terms of their antibacterial properties against Staphylococcus aureus, Escherichia coli and Proteus mirabilis.

scholarly journals Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole

2014 ◽  
Vol 79 (3) ◽  
pp. 277-282
Author(s):  
Vesna Vasic ◽  
Jelena Penjisevic ◽  
Irena Novakovic ◽  
Vladimir Sukalovic ◽  
Deana Andric ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Antifungal Activity ◽  
Salmonella Enteritidis ◽  
Biological Evaluation ◽  
Proteus Vulgaris ◽  
Clostridium Sporogenes ◽  
In Vitro Antibacterial Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Series of eight novel 5-substituted derivatives of benzimidazole were synthesized by condensation of corresponding diamine with ethyl-4-[4-(2-chlorophenyl)piperazin-1-yl] butanoate in refluxing 4N hydrochloric acid. In vitro antibacterial activity against ten strains namely, Bacillus subtilis, Clostridium sporogenes, Streptosporangium longisporum, Micrococcus flavus, Sarcina lutea, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis and Proteus vulgaris and antifungal activity against two fungal strains namely, Candida albicans and Saccharomyces cerevisiae, were evaluated. Of all the compounds screened for activity 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-iodo-1H-benzimidazole and 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-methyl-1H-benzimidazole were associated with higher antifungal activity than commercial drugs.

scholarly journals Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4960
Author(s):  
Olalla Barreiro-Costa ◽  
Gabriela Morales-Noboa ◽  
Patricio Rojas-Silva ◽  
Eliana Lara-Barba ◽  
Javier Santamaría-Aguirre ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
In Silico ◽  
Potential Application ◽  
Mammalian Cells ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Therapeutic Use ◽  
Derivatives Of

This work focuses on the search and development of drugs that may become new alternatives to the commercial drugs currently available for treatment of leishmaniasis. We have designed and synthesized 12 derivatives of bis(spiropyrazolone)cyclopropanes. We then characterized their potential application in therapeutic use. For this, the in vitro biological activities against three eukaryotic models—S. cerevisiae, five cancer cell lines, and the parasite L. mexicana—were evaluated. In addition, cytotoxicity against non-cancerous mammalian cells has been evaluated and other properties of interest have been characterized, such as genotoxicity, antioxidant properties and, in silico predictive adsorption, distribution, metabolism, and excretion (ADME). The results that we present here represent a first screening, indicating two derivatives of bis(spiropyrazolone)cyclopropanes as good candidates for the treatment of leishmaniasis. They have good specificity against parasites with respect to mammalian cells.

Sign in / Sign up

Export Citation Format

Share Document