Biological Activity of Novel N-Substituted Amides of endo-3- (3-Methylthio-1,2,4-triazol-5-yl)bicyclo[2.2.1]hept-5-ene-2- carboxylic Acid and N-Substituted Amides of 1-(5-Methylthio- 1,2,4-triazol-3-yl)cyclohexane-2-carboxylic Acids

2012 ◽  
Vol 67 (3-4) ◽  
pp. 123-128
Author(s):  
Anna Pachuta-Stec ◽  
Urszula Kosikowska ◽  
Anna Chodkowska ◽  
Monika Pitucha ◽  
Anna Malm ◽  
...  
Keyword(s):  
Biological Activity ◽  
Carboxylic Acid ◽  
Carboxylic Acids ◽  
Condensation Reaction ◽  
Primary Amines ◽  
Pharmacological Activities

N-Substituted amides of endo-3-(3-methylthio-1,2,4-triazol-5-yl)bicyclo[2.2.1]hept-5-ene- 2-carboxylic acid and 1-(5-methylthio-1,2,4-triazol-3-yl)cyclohexane-2-carboxylic acid were prepared by the condensation reaction of endo-S-methyl-N1-(bicyclo[2.2.1]hept-5-ene-2,3- dicarbonyl)isothiosemicarbazide and S-methyl-N1-(cyclohexane-2,3-dicarbonyl)isothiosemicarbazide with primary amines. The synthesized compounds were screened for their microbiological and pharmacological activities

Synthesis of 3-(Cyclohexylamino)-2-arylimidazo[1,2-a]pyridine-8- carboxylic Acids Via an Efficient Three-component Condensation Reaction between Cyclohexylisocyanide and 2-Aminopyridine-3-carboxylic Acid in the Presence of Aromatic Aldehyde

2018 ◽  
Vol 21 (4) ◽  
pp. 298-301 ◽  
Author(s):  
Ghasem Marandi
Keyword(s):  
Biological Sciences ◽  
Carboxylic Acid ◽  
Carboxylic Acids ◽  
High Performance ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
New Materials ◽  
One Pot ◽  
High Yields ◽  
Benzaldehyde Derivatives

Aim and Objective: The reaction of cyclohexylisocyanide and 2-aminopyridine-3- carboxylic acid in the presence of benzaldehyde derivatives in ethanol led to 3-(cyclohexylamino)-2- arylimidazo[1,2-a]pyridine-8-carboxylic acids in high yields. In a three component condensation reaction, isocyanide reacts with 2-aminopyridine-3-carboxylic acid and aromatic aldehydes without any prior activation. Material and Methods: The synthesized products have stable structures which have been characterized by IR, 1H, 13C and Mass spectroscopy as well as CHN-O analysis. Results: In continuation of our attempts to develop simple one-pot routes for the synthesis of 3- (cyclohexylamino)-2-arylimidazo[1,2-a]pyridine-8-carboxylic acids, aromatic aldehydes with divers substituted show a high performance. Conclusion: In conclusion, this study introduces the art of combinatorial chemistry using a simple one-pot procedure for the synthesis of new materials which are interesting compounds in medicinal and biological sciences.

Tetrazoloquinolines: Synthesis, Reactions, and Applications

2020 ◽  
Vol 24 (4) ◽  
pp. 439-464 ◽  
Author(s):  
Rizk E. Khidre ◽  
Tahah A. Ameen ◽  
Mounir A. I. Salem
Keyword(s):  
Carboxylic Acid ◽  
Chemical Reactions ◽  
Sodium Azide ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Pharmacological Activities ◽  
Synthesis Reactions ◽  
Intramolecular Cyclocondensation

This review summarizes the synthesis, reactions, and biological activities of tetrazolo[1,5-a]quinoline derivatives. These derivatives were synthesized by several methods such as i) from the reaction of 2-chloroquinoline with sodium azide ii) from diazotization 2-hydrazinylquinoline derivatives, and iii) from intramolecular cyclocondensation of 2-azidoarylidenes. Also, the chemical reactions and pharmacological activities of some tetrazoloquinolines such as tetrazolo[1,5-a]quinoline-4-carbaldehyde, 5-chlorotetrazolo[ 1,5-a]quinoline, 4-(chloromethyl)tetrazolo[1,5-a]quinoline, tetrazolo[1,5- a]quinoline-4-carboxylic acid, and 5-azidotetrazolo[1,5-a]quinoline were discussed.

Flavones and Their Analogues as Bioactive Compounds – An Overview

2019 ◽  
Vol 16 (4) ◽  
pp. 377-391 ◽  
Author(s):  
B.S. Jayashree ◽  
H. Venkatachalam ◽  
Sanchari Basu Mallik
Keyword(s):  
Biological Activity ◽  
Free Radical ◽  
Bioactive Compounds ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Cost Effective ◽  
Free Radical Scavenging ◽  
Polyphenolic Compounds ◽  
Pharmacological Activities ◽  
Poor Solubility

Flavonoids constitute a large group of polyphenolic compounds that are known to have antioxidant properties, through their free radical scavenging abilities. They possess a chromone (γ- benzopyrone) moiety, responsible for eliciting many pharmacological activities. Even though, natural flavonoids are highly potent, owing to their poor solubility, they are less used. Therefore, attempts have been made to improve their stability, solubility, efficacy and kinetics by introducing various substituents on the flavone ring. For nearly the last two decades, flavones were synthesized in our laboratory by simple, convenient and cost-effective methods, with the knowledge of both synthetic and semi-synthetic chemistry. In this direction, it was considered worthwhile to present an overview on the synthesized flavonoids. This review creates a platform for highlighting various modifications done on the flavone system along with their biological activity.

scholarly journals Propylphosphonic acid anhydride–mediated amidation of Morita–Baylis–Hillman–derived indolizine-2-carboxylic acids

2021 ◽  
pp. 174751982098715
Author(s):  
Khethobole C Sekgota ◽  
Michelle Isaacs ◽  
Heinrich C Hoppe ◽  
Ronnett Seldon ◽  
Digby F Warner ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Carboxylic Acids ◽  
Coupling Agent ◽  
Methyl Esters ◽  
Acid Anhydride

Propylphosphonic acid anhydride has been successfully used as a coupling agent in the synthesis of a series of indolizine-2-carboxamido derivatives from indolizine-2-carboxylic acid and its 3-acetylated analogue. The acid substrates were obtained by saponification of the corresponding methyl esters produced, in turn, selectively and efficiently, by time-controlled cyclisation of a single Morita–Baylis–Hillman adduct. Various amino and hydrazino compounds with medicinal potential have been used to prepare indolizine-2-carboxamido and hydrazido derivatives.

scholarly journals Chemical Diversity and Biological Activity of Secondary Metabolites from Soft Coral Genus Sinularia since 2013

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 335
Author(s):  
Xia Yan ◽  
Jing Liu ◽  
Xue Leng ◽  
Han Ouyang
Keyword(s):  
Biological Activity ◽  
Secondary Metabolites ◽  
Coral Species ◽  
Soft Coral ◽  
Biological Activities ◽  
Vital Role ◽  
Chemical Diversity ◽  
Pharmacological Activities ◽  
Lead Compounds ◽  
Coral Genus

Sinularia is one of the conspicuous soft coral species widely distributed in the world’s oceans at a depth of about 12 m. Secondary metabolites from the genus Sinularia show great chemical diversity. More than 700 secondary metabolites have been reported to date, including terpenoids, norterpenoids, steroids/steroidal glycosides, and other types. They showed a broad range of potent biological activities. There were detailed reviews on the terpenoids from Sinularia in 2013, and now, it still plays a vital role in the innovation of lead compounds for drug development. The structures, names, and pharmacological activities of compounds isolated from the genus Sinularia from 2013 to March 2021 are summarized in this review.

scholarly journals Curcumin and Its Potential Impact on Microbiota

Nutrients ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 2004
Author(s):  
Marzena Jabczyk ◽  
Justyna Nowak ◽  
Bartosz Hudzik ◽  
Barbara Zubelewicz-Szkodzińska
Keyword(s):  
Biological Activity ◽  
Gut Microbiota ◽  
Health Effects ◽  
Pharmacokinetic Profile ◽  
Health Impact ◽  
Pharmacological Activities ◽  
Poor Solubility ◽  
Potential Impact ◽  
Bidirectional Interactions

Curcumin is one of the most frequently researched herbal substances; however, it has been reported to have a poor bioavailability and fast metabolism, which has led to doubts about its effectiveness. Curcumin has antioxidant and anti-inflammatory effects, and has demonstrated favorable health effects. Nevertheless, well-reported in vivo pharmacological activities of curcumin are limited by its poor solubility, bioavailability, and pharmacokinetic profile. The bidirectional interactions between curcumin and gut microbiota play key roles in understanding the ambiguity between the bioavailability and biological activity of curcumin, including its wider health impact.

scholarly journals Isolation, Structure Elucidation, and Biological Activity of a New Alkaloid from Zanthoxylum rhetsa

2011 ◽  
Vol 6 (11) ◽  
pp. 1934578X1100601
Author(s):  
Karsten Krohn ◽  
Stephan Cludius-Brandt ◽  
Barbara Schulz ◽  
Mambatta Sreelekha ◽  
Pottachola Mohamed Shafi
Keyword(s):  
Biological Activity ◽  
Carboxylic Acid ◽  
Medicinal Plant ◽  
Plant Extract ◽  
Structure Elucidation ◽  
Biologically Active ◽  
Reduction Product ◽  
Pharmacological Properties ◽  
Evergreen Tree

Several biologically active alkaloids (1-4, 6), including a new quinazoline-6-carboxylic acid (1), were isolated from the medicinal plant Zanthoxylum rhetsa, an evergreen tree, native to subtropical areas. Whereas the pharmacological properties of the plant extract and single constituents have been widely tested, we now show that all of the metabolites have antialgal activities, all but 6 are antibacterial, and 6 and the reduction product 5 (derived from 4) are also antifungal.

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