scholarly journals Design, step-economical diversity-oriented synthesis of an N-heterocyclic library containing a pyrimidine moiety: discovery of novel potential herbicidal agents

RSC Advances ◽  
2021 ◽  
Vol 11 (25) ◽  
pp. 15380-15386
Author(s):  
Dong Ma ◽  
Yang Yin ◽  
Ying-Lu Chen ◽  
Yi-Tao Yan ◽  
Jun Wu
Keyword(s):  
Herbicidal Activity ◽  
Biological Screening ◽  
Diversity Oriented Synthesis ◽  
Significant Potential ◽  
Synthesis Strategy ◽  
Pyrimidine Moiety

A diverse library of pyrimidine–N-heterocycle hybrids was developed through a step-economical diversity-oriented synthesis strategy. In vivo biological screening showed some derivatives exhibited significant potential herbicidal activity.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

scholarly journals Treatment of murine Candida krusei or Candida glabrata infection with L-743,872.

1997 ◽  
Vol 41 (9) ◽  
pp. 1937-1939 ◽  
Author(s):  
J R Graybill ◽  
R Bocanegra ◽  
M Luther ◽  
A Fothergill ◽  
M J Rinaldi
Keyword(s):  
Body Weight ◽  
Broad Spectrum ◽  
Candida Glabrata ◽  
Clinical Development ◽  
Candida Krusei ◽  
Murine Models ◽  
Fungal Cell ◽  
Significant Potential ◽  
Cell Counts

L-743,872 is a broad-spectrum pneumocandin antifungal drug developed by Merck Research Co., and in the present work it was evaluated in vivo in murine models of Candida krusei and Candida glabrata infection. Mice were infected intravenously with two isolates of C. krusei and treated with fluconazole or L-743,872. Fluconazole was beneficial only in immune-competent mice infected with isolate 94-2696. At > 0.5 mg/kg of body weight/day, L-743,872 was effective against both infecting isolates in immune-competent and immune-suppressed mice. Against C. glabrata, L-743,872 was effective, at doses > or = 0.5 mg/kg, in reducing fungal cell counts in the kidneys but not in the spleen. L-743,872 has significant potential for clinical development.

Antibacterial properties and in vivo studies of tannic acid-stabilized silver–halloysite nanomaterials

Clay Minerals ◽  
2020 ◽  
Vol 55 (2) ◽  
pp. 112-119
Author(s):  
Anna Stavitskaya ◽  
Christina Shakhbazova ◽  
Yulia Cherednichenko ◽  
Läysän Nigamatzyanova ◽  
Gölnur Fakhrullina ◽  
...  
Keyword(s):  
Tannic Acid ◽  
Antibacterial Properties ◽  
Halloysite Nanotubes ◽  
In Vivo Studies ◽  
Negative Effects ◽  
Antibacterial Performance ◽  
Synthesis Strategy ◽  
Clay Nanotubes

AbstractTannic acid-stabilized silver nanoparticles were synthesized in situ on halloysite clay nanotubes. The synthesis strategy included simple steps of tannic acid adsorption on clay nanotubes and further particle formation from silver salt solution. Pristine halloysite nanotubes as well as amino-modified clays were used for silver stabilization in water or ethanol. The materials were tested for antibacterial performance using three different methods. All of the materials produced showed antimicrobial activity. The pristine halloysite-based material with ~5 nm particles produced using ethanol as the solvent and tannic acid as the reducing agent showed the greatest antibacterial activity against Serratia marcescens. The materials were tested in vivo on Caenorhabditis elegans nematodes to ensure their safety, and they showed no negative effects on nematode growth and life expectancy.

Design and Preparation of an Electrospun Biomaterial Surgical Patch

2009 ◽  
Vol 24 (1_suppl) ◽  
pp. 158-168 ◽  
Author(s):  
Hai Lu ◽  
Wei-Jun Chen ◽  
Yan Xing ◽  
Da-Jun Ying ◽  
Bo Jiang
Keyword(s):  
Tensile Strength ◽  
Elastic Modulus ◽  
Yield Strength ◽  
Collagen Type ◽  
Sem Images ◽  
Significant Potential ◽  
Clinical Transplantation ◽  
Porcine Pericardium ◽  
Porous Morphology

A biomaterial patch of electrospun collagen type fibers was designed and produced by electrospinning seven different concentrations (8%-20% w/v) of collagen solutions. The tensile strength, yield strength, and elastic modulus of the electrospun collagen fibrous patches were found to be suitable for clinical transplantation. No significant differences versus fresh porcine pericardium as controls were observed. The SEM images of the groups showed that the patches were smooth with uniform interwoven and porous morphology. The fibrous patches were biocompatible and did not elicit local or systemic toxic effects when implanted in vivo. These electrospun collagen fibrous patches have significant potential as surgical biomaterial patches.

scholarly journals A Multidimensional Diversity-Oriented Synthesis Strategy for Structurally Diverse and Complex Macrocycles

2016 ◽  
Vol 128 (37) ◽  
pp. 11305-11309 ◽  
Author(s):  
Feilin Nie ◽  
Dominique L. Kunciw ◽  
David Wilcke ◽  
Jamie E. Stokes ◽  
Warren R. J. D. Galloway ◽  
...  
Keyword(s):  
Diversity Oriented Synthesis ◽  
Synthesis Strategy

scholarly journals Seedless gold nanostars with seed-like advantages for biosensing applications

2019 ◽  
Vol 6 (2) ◽  
pp. 181971 ◽  
Author(s):  
Masauso Moses Phiri ◽  
Danielle Wingrove Mulder ◽  
Barend Christiaan Vorster
Keyword(s):  
Growth Control ◽  
Building Blocks ◽  
Anisotropic Growth ◽  
Visible Spectroscopy ◽  
Naked Eye ◽  
Gold Nanostars ◽  
Plasmonic Sensing ◽  
Synthesis Strategy ◽  
Biomedical Diagnosis

Gold nanostars (AuNSs) are seen as promising building blocks for biosensors with potential for easy readouts based on naked-eye and ultraviolet–visible spectroscopy detection. We present a seedless synthesis strategy for AuNSs that has the advantages of the seeded methods. The method used ascorbic acid as a reducing agent and silver nitrate as an anisotropic growth control assisting agent. AuNSs with multiple branches and a diameter of 59 nm were produced. They showed good stability when capped with PVP and modified with an enzyme in relatively strong ionic conditions. We investigated their application in plasmonic sensing by modifying them with glucose oxidase and detection of glucose. The AuNSs were found to be a good scaffold for the enzyme, proved to be stable and sensitive as transducers. Thus, the AuNSs showed good promise for further applications in plasmonic biosensing for in vivo biomedical diagnosis.

Fast & easy preparation of 3D scaffolds from methyl benzoate by a diversity oriented synthesis strategy based on Diels–Alder and ene-reactions

2017 ◽  
Vol 15 (26) ◽  
pp. 5585-5592
Author(s):  
Dominique Brossard ◽  
Pascal Retailleau ◽  
Vincent Dumontet ◽  
Philippe Breton ◽  
Sandy Desrat ◽  
...  
Keyword(s):  
Diels Alder ◽  
Methyl Benzoate ◽  
3D Scaffolds ◽  
Ene Reactions ◽  
Diversity Oriented Synthesis ◽  
Ene Reaction ◽  
3D Shape ◽  
Synthesis Strategy

Thermic dimerization of methyl 1,3-cyclohexadiene 2-carboxylate gave original 3D-shape compounds by Diels–Alder cycloaddition and original [6 + 4]-ene reaction.

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