Synthesis and Antimicrobial Activity of (Z)-2-(4-((5-((1-Benzylpiperidin-4-yl)methylene)-
2,4-dioxothiazolidin-3-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamides

In current times, researchers adopted the click chemistry approach for the synthesis of various druglike molecules by using a few reliable, feasible, practical and selective chemical transformations via click formation. In present work, we focussed on the most triazole clubbed thiazolidine-2,4-dione derivatives as the most promising motifs for broad biological application. A total of fifteen (CF-4a-o) derivatives were synthesized and well characterized with various analytical techniques.

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Enamine/Transition Metal Combined Catalysis: Catalytic Transformations Involving Organometallic Electrophilic Intermediates

Topics in Current Chemistry ◽

10.1007/s41061-019-0267-y ◽

2019 ◽

Vol 377 (6) ◽

Cited By ~ 2

Author(s):

Samson Afewerki ◽

Armando Córdova

Keyword(s):

Transition Metal ◽

Metal Complex ◽

Carbonyl Compounds ◽

Transition Metal Catalysis ◽

Chemical Transformations ◽

Considerable Effort ◽

Metal Catalysis ◽

First Report ◽

Wide Range ◽

Selective Chemical

AbstractThe concept of merging enamine activation catalysis with transition metal catalysis is an important strategy, which allows for selective chemical transformations not accessible without this combination. The amine catalyst activates the carbonyl compounds through the formation of a reactive nucleophilic enamine intermediate and, in parallel, the transition metal activates a wide range of functionalities such as allylic substrates through the formation of reactive electrophilic π-allyl-metal complex. Since the first report of this strategy in 2006, considerable effort has been devoted to the successful advancement of this technology. In this chapter, these findings are highlighted and discussed.

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Physicochemical Properties and Antimicrobial Activity of Evaporated Extract of Cow Dung Against Some Pathogens

Journal of Scientific Research ◽

10.3329/jsr.v5i1.11962 ◽

2012 ◽

Vol 5 (1) ◽

pp. 135-141

Author(s):

M. Waziri ◽

J. S. Suleiman

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Inhibitory Concentration ◽

Analytical Techniques ◽

Food Additive ◽

Cow Dung ◽

Northern Nigeria ◽

Elemental Contents ◽

Mic Value

The evaporated extract of cow dung is traditionally used in Northern Nigeria and Cameroun as food additive and in treatment of infectious diseases. In this study, the cow dung ash extract was prepared and tested for some elemental contents as well as the antimicrobial activity against Cyanobacteria (C.bacteria), Staphylococcus aureus (S.aureus), Bacillus subtilis (B.subtilis) and Escherichia coli (E.coli) using different analytical techniques. The extract was highly basic with pH of 11.7 and the elements vary in the following decreasing order of concentration; K>Na>Mg>Ca>Fe>Al>Zn. S. aureus was the most sensitive bacteria with minimum inhibitory concentration (MIC) value of 0.082 mg/mL while B. subtilis was the least sensitive with MIC value of 4.3 mg/mL. The result of this study indicate that the extract can supplement the dietary Na and K requirements for the users and supports the folkloric use of the extract in treatment of infections.© 2013 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: http://dx.doi.org/10.3329/jsr.v5i1.11962 J. Sci. Res. 5 (1), 135-141 (2013)

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Synthesis and Antimicrobial Activity of 1,2,3-Triazole Linked Benzo[d]oxazole-2-thiol/ oxazolo[4,5-b]pyridine-2-thiol Derivatives

Asian Journal of Organic & Medicinal Chemistry ◽

10.14233/ajomc.2021.ajomc-p293 ◽

2021 ◽

Vol 6 (1) ◽

pp. 7-12

Author(s):

Pankaj Gour ◽

Lata Deshmukh ◽

Tulshiram Dadmal ◽

Archana Ramteke

Keyword(s):

Antimicrobial Activity ◽

Click Chemistry ◽

Pathogenic Fungi ◽

E Coli

A new series of 1,2,3-triazole linked mercaptobenzoxazole/oxazolo- [4,5-b] pyridine-2-thiol derivatives (6a-j) were synthesized starting from 2-aminophenol/2-aminopyridin-3-ol in three steps via cyclization, alkylation followed by reaction with various aromatic azides using click chemistry approach. All the synthesized compounds were evaluated for their antimicrobial activity viz. E. coli, P. aeruginosa, S. aureus and S. pyogenus and three pathogenic fungi viz. C. albicans, A. niger and A. clavatus and promising compounds were identified.

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Synthesis, Characterization, and Antimicrobial Activity of a Series of 2-(5-Phenyl-1,3,4-oxadiazol-2-yl)-N-[(1-aryl-1H-1,2,3-triazol-4-yl)methyl]anilines Using Click Chemistry

Russian Journal of General Chemistry ◽

10.1134/s1070363218070228 ◽

2018 ◽

Vol 88 (7) ◽

pp. 1488-1494 ◽

Cited By ~ 2

Author(s):

N. Venkatagiri ◽

T. Krishna ◽

P. Thirupathi ◽

K. Bhavani ◽

C. K. Reddy

Keyword(s):

Antimicrobial Activity ◽

Click Chemistry

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Ethenesulfonyl Fluoride (ESF) and Its Derivatives in SuFEx Click Chemistry and More

Synthesis ◽

10.1055/s-0039-1690038 ◽

2019 ◽

Vol 52 (05) ◽

pp. 673-687 ◽

Cited By ~ 3

Author(s):

Yan-Ping Meng ◽

Shi-Meng Wang ◽

Wan-Yin Fang ◽

Zhi-Zhong Xie ◽

Jing Leng ◽

...

Keyword(s):

Organic Chemistry ◽

Click Chemistry ◽

Exchange Reaction ◽

Organic Synthesis ◽

Medicinal Chemistry ◽

Materials Science ◽

Click Reaction ◽

Chemical Properties ◽

Chemical Transformations ◽

Absolute Reliability

The sulfur(VI) fluoride exchange reaction (SuFEx), developed by Sharpless and co-workers in 2014, is a new category of click reaction that creates molecular connections with absolute reliability and unprecedented efficiency through a sulfur(VI) hub. Ethenesulfonyl fluoride (ESF), as one of the most important sulfur(VI) hubs, exhibits extraordinary reactivity in SuFEx click chemistry and organic synthesis. This review summarizes the chemical properties and applications of ESF in click chemistry, organic chemistry, materials science, medicinal chemistry and in many other fields related to organic synthesis.1 Introduction2 Chemical Transformations of ESF3 Chemical Transformations of 2-Arylethenesulfonyl Fluorides4 Novel SuFEx Reagents Derived from ESF5 Applications of ESF Derivatives in Medicinal Chemistry6 Applications of ESF Derivatives in Materials Science7 Conclusion

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Stereochemistry of Dehydrogenation by D-Galactose Oxidase

Canadian Journal of Chemistry ◽

10.1139/v71-575 ◽

1971 ◽

Vol 49 (21) ◽

pp. 3429-3437 ◽

Cited By ~ 52

Author(s):

A. Maradufu ◽

G. M. Cree ◽

A. S. Perlin

Keyword(s):

Hydrogen Atom ◽

Isotope Effect ◽

Galactose Oxidase ◽

Relative Impact ◽

Chemical Transformations ◽

Product Analysis ◽

Deuterium Isotope Effect ◽

Oxidation Rates ◽

Selective Chemical ◽

Sugar Derivatives

The stereochemistry of dehydrogenation of the primary carbinol group of D-galactose by D-galactose oxidase has been determined. Using D-galactose-6-d and methyl β-D-galactopyranoside-6-d, it has been established that the reaction involves removal of the pro-S 6-hydrogen atom. This conclusion is based on product analysis, and on the relative impact of the deuterium isotope effect on oxidation rates of substrates having different R:S deuteration patterns. The absolute configurations at C-6 of these substrates have been determined by selective chemical transformations to products of known configuration. The rotational conformation of the 6-carbinol group of D-galactose and its possible relationship to the specificity of the enzyme are discussed, as well as the stereochemistry of reductive deuteration of aldehydo sugar derivatives.

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Biosynthetically-inspired oxidations of capillobenzopyranol

Organic & Biomolecular Chemistry ◽

10.1039/c7ob00868f ◽

2017 ◽

Vol 15 (22) ◽

pp. 4811-4815 ◽

Cited By ~ 2

Author(s):

Henry P. Pepper ◽

Hiu C. Lam ◽

Jonathan H. George

Keyword(s):

Marine Sponge ◽

Chemical Transformations ◽

Selective Chemical

The marine sponge meroterpenoid capillobenzopyranol has been converted into the co-isolated verrubenzospirolactone using simple and selective chemical transformations.

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Synthesis, Characterization and Pharmacological Screening of Some Novel 2- substituted and 1(H)-substituted Benzimidazole Derivatives as potent Anti-cancer agents

Journal of University of Shanghai for Science and Technology ◽

10.51201/jusst/21/121067 ◽

2022 ◽

Vol 24 (1) ◽

pp. 34-47

Author(s):

Pankaj S. Kore ◽

◽

Santosh K. Singh ◽

Shrinivas K. Mohite ◽

◽

...

Keyword(s):

Microwave Irradiation ◽

Organic Synthesis ◽

Structural Motif ◽

Benzimidazole Derivatives ◽

Chemical Transformations ◽

Benzimidazole Ring ◽

Biological Application ◽

Irradiation Energy ◽

Anti Cancer ◽

Pharmacological Screening

The most of drugs containing Benzimidazole ring is a prominent structural motif found in numerous therapeutically active compounds. Benzimidazole and its synthetic analogues have been found to exhibit industrial, agricultural and biological application such as antitubercular, anti-inflammatory, analgesic, anticancer, anticoagulant, as well as good antifungal and anti microbial activity. Recent advances in technology considers microwave irradiation energy as the most efficient means of heating reactions for chemical transformations that can be accomplished in a minutes. Microwave irradiation assists organic synthesis (MAOS) not only helps in implementing green chemistry but also led to progress in organic synthesis. We report pharmacological screening of some novel 2 substituted and 1(h)-substituted Benzimidazole derivatives.

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Conjugation of Synthetic Polyproline Moietes to Lipid II Binding Fragments of Nisin Yields Active and Stable Antimicrobials

Frontiers in Microbiology ◽

10.3389/fmicb.2020.575334 ◽

2020 ◽

Vol 11 ◽

Author(s):

Jingjing Deng ◽

Jakob H. Viel ◽

Vladimir Kubyshkin ◽

Nediljko Budisa ◽

Oscar P. Kuipers

Keyword(s):

Antimicrobial Activity ◽

Click Chemistry ◽

Enterococcus Faecium ◽

Proteolytic Enzymes ◽

Active Peptide ◽

Lipid Ii ◽

Promising Strategy ◽

C Terminus ◽

Insight Into ◽

Better Than

Coupling functional moieties to lantibiotics offers exciting opportunities to produce novel derivatives with desirable properties enabling new functions and applications. Here, five different synthetic hydrophobic polyproline peptides were conjugated to either nisin AB (the first two rings of nisin) or nisin ABC (the first three rings of nisin) by using click chemistry. The antimicrobial activity of nisin ABC + O6K3 against Enterococcus faecium decreased 8-fold compared to full-length nisin, but its activity was 16-fold better than nisin ABC, suggesting that modifying nisin ABC is a promising strategy to generate semi-synthetic nisin hybrids. In addition, the resulting nisin hybrids are not prone to degradation at the C-terminus, which has been observed for nisin as it can be degraded by nisinase or other proteolytic enzymes. This methodology allows for getting more insight into the possibility of creating semi-synthetic nisin hybrids that maintain antimicrobial activity, in particular when synthetic and non-proteinaceous moieties are used. The success of this approach in creating viable nisin hybrids encourages further exploring the use of different modules, e.g., glycans, lipids, active peptide moieties, and other antimicrobial moieties.

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