Synthesis, Antimicrobial Assay and SARs of Pyrazole Included Heterocyclic Derivatives

Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neurodegenerative diseases such as depression, Parkinson’s disease and Alzheimer’s disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single heterocyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure- activity relationship to provide better correlation among different structures and their receptor interactions.

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Structure-Bioactivity Relationship Study of Xanthene Derivatives: A Brief Review

Current Organic Synthesis ◽

10.2174/1570179416666191017094908 ◽

2020 ◽

Vol 16 (8) ◽

pp. 1071-1077

Author(s):

Aref G. Ghahsare ◽

Zahra S. Nazifi ◽

Seyed M.R. Nazifi

Keyword(s):

Biological Activities ◽

Cyclic Compound ◽

Research Field ◽

Pharmaceutical Chemistry ◽

Therapeutic Effects ◽

Main Research ◽

Research Fields ◽

Xanthene Derivatives ◽

Anti Cancer ◽

Heterocyclic Derivatives

: Over the last decades, several heterocyclic derivatives compounds have been synthesized or extracted from natural resources and have been tested for their pharmaceutical activities. Xanthene is one of these heterocyclic derivatives. These compounds consist of an oxygen-containing central heterocyclic structure with two more cyclic structures fused to the central cyclic compound. It has been shown that xanthane derivatives are bioactive compounds with diverse activities such as anti-bacterial, anti-fungal, anti-cancer, and anti-inflammatory as well as therapeutic effects on diabetes and Alzheimer. The anti-cancer activity of such compounds has been one of the main research fields in pharmaceutical chemistry. Due to this diverse biological activity, xanthene core derivatives are still an attractive research field for both academia and industry. This review addresses the current finding on the biological activities of xanthene derivatives and discussed in detail some aspects of their structure-activity relationship (SAR).

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A new heterocyclic ring closure in ferricyanide oxidation of 2,4,6-triphenylpyridinium salts

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19833307 ◽

1983 ◽

Vol 48 (11) ◽

pp. 3307-3314 ◽

Cited By ~ 6

Author(s):

Petr Nesvadba ◽

Petr Štrop ◽

Josef Kuthan

Keyword(s):

Alkaline Solution ◽

Heterocyclic Ring ◽

Potassium Ferricyanide ◽

Probable Mechanism ◽

Ring Closure ◽

Pyridinium Salts ◽

Mechanism Of Formation ◽

Pyrrole Derivatives ◽

Quaternary Pyridinium Salts ◽

Heterocyclic Derivatives

The quaternary pyridinium salts Ia-Ic react with alkaline solution of potassium ferricyanide to give the condensed heterocyclic derivatives IIIa, b, IV, whereas the salts Id-If give the pyrrole derivatives IIa-IIc under the same conditions. The diaza heterocycle IIIa reacts with methyl iodide to give methoiodide V, whereas by action of bromine it produces two monobromo derivatives VIa, b. The pyrrole derivatives IIa, b give monobromo derivatives IId, e on bromination. A probable mechanism of formation of the heterocyclic derivatives is discussed.

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Chemical Composition and Antimicrobial Activities of the Essential Oil From the Leaves of Pterocephalus hookeri

Natural Product Communications ◽

10.1177/1934578x20981239 ◽

2020 ◽

Vol 15 (12) ◽

pp. 1934578X2098123

Author(s):

Peng-fei Yang ◽

Hui Lu ◽

Qiong-bo Wang ◽

Zhi-wei Zhao ◽

Qiang Liu ◽

...

Keyword(s):

Gas Chromatography ◽

Chemical Composition ◽

Essential Oil ◽

Chemical Constituents ◽

Antimicrobial Activities ◽

Gas Chromatography Mass Spectrometry ◽

Flame Ionization ◽

And Staphylococcus Aureus ◽

Antimicrobial Assay ◽

Detailed Chemical

Detailed chemical constituents of essential oil from the Pterocephalus hookeri leaves and its antimicrobial activities were investigated in this study. The essential oil, obtained by hydrodistillation, was characterized by gas chromatography-flame ionization detection and gas chromatography-mass spectrometry analyses. Among the 90 identified compounds, hexadecanoic acid (21.27%), phytol (8.03%), furfural (7.08%), oleic acid (5.25%), and phytone (4.56%) were the major components. In the antimicrobial assay, the essential oil showed strong inhibitory activities against Escherichia coli, Candida albicans, and Staphylococcus aureus with minimum inhibitory concentration values of 31.3, 62.5, and 125 µg/mL, respectively. To our knowledge, this is the first report concerning chemical composition and antimicrobial activities of the essential oil from Pterocephalus hookeri.

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Chemical Composition and Antimicrobial Assay of Essential Oil from Whole Aerial Parts of Ainsliaea aptera DC. Collected from two Different Regions of Central Himalaya

Journal of Essential Oil Bearing Plants ◽

10.1080/0972060x.2021.1951361 ◽

2021 ◽

Vol 24 (3) ◽

pp. 510-518

Author(s):

Lalit S. Bisht ◽

Anand B. Melkani ◽

Rajendra Prasad ◽

Lalit Mohan ◽

Manisha Palni ◽

...

Keyword(s):

Chemical Composition ◽

Essential Oil ◽

Central Himalaya ◽

Aerial Parts ◽

Antimicrobial Assay

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Effect of rat polymorphonuclear leukocyte granule components on the growth and survival of Pseudomonas aeruginosa and Salmonella typhimurium

Canadian Journal of Microbiology ◽

10.1139/m83-208 ◽

1983 ◽

Vol 29 (10) ◽

pp. 1339-1343 ◽

Cited By ~ 2

Author(s):

M. C. Modrzakowski ◽

D. Dosch-Meier ◽

R. L. Hodinka

Keyword(s):

Pseudomonas Aeruginosa ◽

Antimicrobial Activity ◽

Salmonella Typhimurium ◽

Polymorphonuclear Neutrophils ◽

Growth Enhancement ◽

Growth And Survival ◽

Whole Cells ◽

Phosphate Buffered Saline ◽

Antimicrobial Assay ◽

Enhancement Property

Granule contents from rat polymorphonuclear neutrophils were prepared by extraction with 0.2 M acetate buffer (pH 4.0), dialyzed against phosphate-buffered saline (pH 7.0), and tested for bactericidal activity against selected target bacteria. Salmonella typhimurium LT-2 and a series of progressively rough lipopolysaccharide outer membrane mutants derived from it were used to monitor antimicrobial activity. Although an antimicrobial potential was present in rat granule contents for S. typhimurium, the growth of Pseudomonas aeruginosa PAO-1 in antimicrobial assay mixtures containing rat granule contents was substantially enhanced over control values. The growth enhancement property of the granule protein was heat resistant and promoted increased oxygen consumption by whole cells.

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