scholarly journals Applications substituted 2-aminothiophenes in drug design

2021 ◽  
Vol 9 (2) ◽  
Author(s):  
Zita Puterová ◽  
Alžbeta Krutošíková ◽  
Daniel Végh
Keyword(s):  
Antimicrobial Activity ◽  
Drug Design ◽  
Adenosine Receptor ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
A1 Adenosine Receptor ◽  
Active Compounds ◽  
Thiophene Derivatives ◽  
Anti Inflammatory ◽  
Bacteria And Fungi

Highly substituted thiophene derivatives are important heterocycles found in numerous biologically active compounds. Title compounds are attractive derivatives because their applications in pharmaceuticals, agriculture and pesticides. They exhibit antimicrobial activity against various Gram(+) and Gram(-) bacteria and fungi. Many of these molecules act as allosteric enhancers of A1-adenosine receptor, glucagon antagonists as well as antioxidant and anti-inflammatory agents.

scholarly journals Monoterpenes as a renewable source of biologically active compounds

2017 ◽  
Vol 89 (8) ◽  
pp. 1105-1117 ◽  
Author(s):  
Nariman F. Salakhutdinov ◽  
Konstantin P. Volcho ◽  
Olga I. Yarovaya
Keyword(s):  
Biological Activity ◽  
Absolute Configuration ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Great Promise ◽  
Active Compounds ◽  
Renewable Source ◽  
The Creation ◽  
Anti Inflammatory

AbstractMonoterpenes and their derivatives play an important role in the creation of new biologically active compounds including drugs. The review focuses on the data on various types of biological activity exhibited by monoterpenes and their derivatives, including analgesic, anti-inflammatory, anticonvulsant, antidepressant, anti-Alzheimer, anti-Parkinsonian, antiviral, and antibacterial (anti-tuberculosis) effects. Searching for novel potential drugs among monoterpene derivatives shows great promise for treating various pathologies. Special attention is paid to the effect of absolute configuration of monoterpenes and monoterpenoids on their activity.

scholarly journals The Study of Pyridazine Compounds on Prostanoids: Inhibitors of COX, cAMP Phosphodiesterase, and TXA2Synthase

2014 ◽  
Vol 2014 ◽  
pp. 1-16 ◽  
Author(s):  
Mohammad Asif
Keyword(s):  
Structural Feature ◽  
Thromboxane A2 ◽  
Antiplatelet Agents ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Camp Phosphodiesterase ◽  
Active Compounds ◽  
Cox Inhibitors ◽  
Antipyretic Activity ◽  
Anti Inflammatory

The pyridazine moiety is an important structural feature of various pharmacological active compounds. Synthetic pyridazine compounds have been reported as effective antiprostaglandins (PGs), 5-lipoxygenase (5-LOX), and antiplatelet agents, that is, inhibitors of prostaglandin or cyclooxygenase (COX-I & COX-II) enzyme, platelet cAMP phosphodiesterase, and thromboxane A2 (TXA2) synthase. These compounds are selective and nonselective COX inhibitors and showed analgesic, anti-inflammatory, and antipyretic activity. Pyridazine compounds with antiplatelet agents inhibited TXA2enzyme. Pyridazines also exhibited antirheumatoid activity. These pyridazine compounds hold considerable interest relative to the preparation of organic intermediates and other anticipated biologically active compounds.

scholarly journals The investigation of the cranberry (Vaccinium oxycoccos L.) concentrated juice antimicrobial activity

2018 ◽  
pp. 84-92
Author(s):  
K. M. Yatsiuk ◽  
M. I. Feodorovska ◽  
R. V. Kutsyk
Keyword(s):  
Antimicrobial Activity ◽  
Biofilm Formation ◽  
Antimicrobial Properties ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Urinary System ◽  
Cranberry Juice ◽  
Active Compounds ◽  
Gram Negative ◽  
Uropathogenic Bacteria

The urinary system infections is one of the most common diseases of the genitourinary system in women. Of particular interest in the prevention and treatment of chronic cystitis is the consumption of the cranberry (Vaccinium oxycoccos L.) fruits. This plant has long been used in urological practice due to the content of proantocianidins, flavonoids, organic acids (benzoic, citric, quinic, ursolic), pectin substances, vitamins, microelements etc. Numerous clinical studies (including randomized, double-blind, placebo-controlled) reveal statistically reliable efficiency of cranberry juice in the forms of concentrates, cocktails and capsules to urinary system infections prevention in women. Since the main pathogens of urinary system infections are Escherichia coli, Enterococcus faecalis, Pseudomonas aeruginosa, Staphylococcus aureus, the aim of our work was to study the antimicrobial properties of the cranberry concentrated juice. Comparative testing of antimicrobial activity was performed using micromethod of diffusion in agar. The carried out study indicates that the concentrated juice maintains antimicrobial properties to the most common uropathogenic microorganisms. Effective antimicrobial concentration was found according with analysis of microbial cultures growth curves in a nutrient medium with various juice dilutions. Gram-positive bacteria (S. aureus, E. faecalis) are more sensitive to the cranberry concentrated juice than gram-negative (E. coli and P. aeruginosa). The adhere ability to a solid surface with the subsequent formation of biofilm is an important factor in the uropathogenic bacteria virulence. Therefore, the next step was to study the effect of cranberry juice biologically active compounds on the biofilms formation in the uropathogenic bacteria broth cultures. It was determined that cranberry juice suppresses the biofilm formation of S. aureus with the greatest intensity. It was observed the 45,3–55,8% reduction of the biofilm creating intensity in the presence of the condensed juice subbacteriostatic dilutions. When the condensed juice was diluted as 1:160, inhibition of E. faecalis biofilm formation ability on 44,90% was detected. The effect of cranberry biologically active compounds on the biofilms formation by gram-negative bacteria was observed in the range of 20%. Thus, the obtained cranberry concentrated juice can be recommended as the remedy for application in prevention of recurrent urinary system infections.

scholarly journals 2,3-Dihydroquinazolin-4(1H)-one as a privileged scaffold in drug design

RSC Advances ◽  
2018 ◽  
Vol 8 (37) ◽  
pp. 20894-20921 ◽  
Author(s):  
Mariateresa Badolato ◽  
Francesca Aiello ◽  
Nouri Neamati
Keyword(s):  
Drug Design ◽  
Structural Component ◽  
Heterocyclic Compounds ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Privileged Scaffold

2,3-Dihydroquinazolin-4-one (DHQ) belongs to the class of nitrogen-containing heterocyclic compounds representing a core structural component in various biologically active compounds.

Nickel(0)-Catalyzed Linear-Selective Hydroarylation of Unactivated Alkenes and Styrenes with Arylboron Acids

2018 ◽  
Author(s):  
Honggui Lv ◽  
Li-Jun Xiao ◽  
Dongbing Zhao ◽  
Qi-Lin Zhou
Keyword(s):  
Butyric Acid ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Highly Efficient ◽  
Organoboronic Acids

Herein, we realized the first linear-selective hydroarylation of unactivated alkenes and styrenes with organoboronic acids by introducing directing groupon alkenes. Our method is highly efficient and scalable, and provides a modular route to assemble structurally diverse alkylarenes, especially for γ-aryl butyric acid derivatives, which have been widely utilized as chemical feedstocks to access multiple marketed drugs, and biologically active compounds.<br>

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