ChemInform Abstract: Iron Catalyzed Cross-Couplings of Azetidines - Application to the Formal Synthesis of a Pharmacologically Active Molecule.

ChemInform ◽  
2015 ◽  
Vol 46 (25) ◽  
pp. no-no
Author(s):  
Dixit Parmar ◽  
Lena Henkel ◽  
Josef Dib ◽  
Magnus Rueping
Keyword(s):  
Active Molecule ◽  
Formal Synthesis ◽  
Pharmacologically Active

Iron catalysed cross-couplings of azetidines – application to the formal synthesis of a pharmacologically active molecule

2015 ◽  
Vol 51 (11) ◽  
pp. 2111-2113 ◽  
Author(s):  
Dixit Parmar ◽  
Lena Henkel ◽  
Josef Dib ◽  
Magnus Rueping
Keyword(s):  
Cross Coupling ◽  
Grignard Reagents ◽  
Active Molecule ◽  
Formal Synthesis ◽  
Iron Catalysis ◽  
The Cross ◽  
Pharmacologically Active

A protocol for the cross-coupling of azetidines with aryl, heteroaryl, vinyl and alkyl Grignard reagents has been developed under iron catalysis. In addition, a short formal synthesis of a pharmacologically active molecule was demonstrated.

Bioavailability of naringenin chalcone in humans after ingestion of cherry tomatoes

2020 ◽  
Vol 90 (5-6) ◽  
pp. 411-416 ◽  
Author(s):  
Carina Kolot ◽  
Ana Rodriguez-Mateos ◽  
Rodrigo Feliciano ◽  
Katharina Bottermann ◽  
Wilhelm Stahl
Keyword(s):  
Plasma Levels ◽  
Average Concentration ◽  
Biologically Active ◽  
Thiol Groups ◽  
Structural Element ◽  
Active Molecule ◽  
Reactive Center ◽  
Average Maximum ◽  
Alpha Beta ◽  
Cherry Tomatoes

Abstract. Chalcones are a type of flavonoids characterized by an α-β unsaturated structural element which may react with thiol groups to activate pathways such as the Nrf2-Keap-1 system. Naringenin chalcone is abundant in the diet but little is known about its bioavailability. In this work, the bioavailability of naringenin chalcone from tomatoes was investigated in a group of healthy men (n=10). After ingestion of 600 grams of tomatoes providing a single dose of 17.3 mg naringenin chalcone, 0.2 mg of naringenin, and 195 mg naringin plasma levels of free and conjugated naringenin and naringenin chalcone (glucuronide and sulfate) were analyzed by UHPLC-QTOF-MS at 0.5, 1, 3, and 6 h post-consumption. Plasma levels of conjugated naringenin increased to about 12 nmol/L with a maximum at about 3 h. Concentrations of free naringenin hardly elevated above baseline. Plasma levels of free and conjugated naringenin chalcone significantly increased. A maximum of the conjugated chalcone was reached at about 3 h after ingestion with an average concentration of about 0.5 nmol/L. No free chalcone was detectable at baseline but low amounts of the unconjugated compound could be detected with an average maximum of 0.8 nmol/L at about 1 h after ingestion. The data demonstrate that naringenin chalcone is bioavailable in humans from cherry tomatoes as a dietary source. However, availability is poor and intramolecular cyclisation as well as extended metabolism likely contribute to the inactivation of the reactive alpha-beta unsaturated reactive center as well as the excretion of the biologically active molecule, respectively.

Laricifomes officinalis – a rich source of pharmacologically active triterpenes

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381 ◽  
Author(s):  
S Sturm ◽  
K Gallmetzer ◽  
A Friedl ◽  
B Waltenberger ◽  
V Temml ◽  
...  
Keyword(s):  
Rich Source ◽  
Pharmacologically Active

Traditional, Pharmacological and Patenting Potential of Neem (Azadirachta indica): A Review

2017 ◽  
Vol 3 (4) ◽  
pp. 383-391
Author(s):  
Mohd Asif Khan ◽  
Shashi Bhooshan Tiwari ◽  
Himanshu Gupta ◽  
Huma Noor
Keyword(s):  
Azadirachta Indica ◽  
Indian Subcontinent ◽  
National Academy Of Sciences ◽  
Neem Tree ◽  
Commercial Plant ◽  
Pharmacological Potential ◽  
Pharmacologically Active ◽  
In The Beginning ◽  
Prevention And Cure ◽  
Academy Of Sciences

Since ancient time, herbal drugs were highly used in the prevention and cure of various human illnesses. In India, Azadirachta indica being commonly known as Neem or Margosa is one of the multi-functional trees; belonging to Meliaceae family. In 1992, the US National Academy of Sciences was published a report entitled ‘Neem- a tree for solving global problems’. It is still considered as ‘village dispensary’ throughout the India. There are two species of Azadirachta which have been investigated; Azadirachta indica that is found in the Indian subcontinent and Azadirachta excelsa Kack that is homegrown to Indonesia and Philippines. A large number of pharmacologically active substances have been identified and isolated from the different parts of neem including azadirachtin, meliacin, gedunin, salanin, nimbin, valassin and various other components which are derived from these main compounds. Many different studies have been evaluated and authenticated for its various traditional and pharmacological activities like itching, leprosy, wound healing, spermicidal, anti-inflammatory, insecticidal, antidiabetic and analgesic etc. In the beginning of 1979, patenting on neem was started by CSIR to separate the active compounds from neem oil. Its great implantation fights with soil erosion, global warming, deforestations and desertification world-wide. In 2002, World Neem Conference raised the neem tree as an industrial or commercial plant. This review is going to explore comprehensively; traditional, pharmacological potential along with patenting, environmental & industrial significant of various parts of neem tree with safety concerns.

Pharmacognostical and pharmacological activity of Justicia gendarussa burm.f.: a comprehensive review

2020 ◽  
Vol 11 (3) ◽  
pp. 3384-3390
Author(s):  
Ashish ◽  
Anjali ◽  
Dixit Praveen K ◽  
Nagarajan K ◽  
Sahoo Jagannath
Keyword(s):  
Pharmacological Activity ◽  
Chemical Constituents ◽  
Biological Action ◽  
Andaman Islands ◽  
Comprehensive Review ◽  
Medicinal Value ◽  
Anti Oxidant ◽  
Phytochemical Constituents ◽  
Pharmacologically Active ◽  
Different Parts

Justicia gendarussa Burm .f. (family Acanthaceae) which is also known as willow-leaves and commonly known as Nili-Nirgundi, it is very commonly found nearby to China and its availability is very common in larger parts of India and Andaman islands. Traditionally it is used to treat various sorts of disorders such as wound healing, anti-inflammatory, anti-oxidant, antiproliferative, anti-arthritic etc. Justicia gendarussa is one of the crucial herbs which has been used in the Ayurveda. Majorly leaves parts of the plant shows the pharmacological activity but the root of the plant Justicia gendarussa is also have the important medicinal values. A large variety of pharmacologically active constituents i.e., alkaloids, flavonoids, saponin, carbohydrates, steroids, triterpenoids, carotenoids, aminoacids, tannins, phenolics, coumarines and anthaquinones are also present in this plant and they makes the plant pharmacologically important. The activity of the plant is also dependent on the solvent which is used for the extraction the various vital chemical constituents. The different- different parts of the plants having the different medicinal values also differ in the chemical values. This review is not only focused on the essential phytochemical constituents which is available in the plant but it also explains their necessary medicinal value to shows the essential biological action and phytopharmacological actions of various parts of the plant.

Development of Solid-Self Micron Emulsifying Drug Delivery Systems

2013 ◽  
Vol 6 (2) ◽  
pp. 2014-2021
Author(s):  
Preethi Sudheer ◽  
Koushik Y ◽  
Satish P ◽  
Uma Shankar M S ◽  
R S Thakur
Keyword(s):  
Drug Delivery ◽  
Systemic Circulation ◽  
Water Soluble ◽  
Future Research ◽  
Steady Increase ◽  
Liquid Form ◽  
Lipophilic Compounds ◽  
Modern Drug ◽  
Pharmaceutical Scientist ◽  
Pharmacologically Active

As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new pharmacologically active lipophilic compounds that are poorly water soluble and solubility is one of the most important parameter to achieve desired concentration of drug in systemic circulation for therapeutic response. It is a great challenge for pharmaceutical scientist to convert those molecules into orally administered formulation with sufficient bioavailability.  Among the several approaches to improve oral bioavailability of these molecules, Self-micron emulsifying drug delivery system (SMEDDS) is one of the approaches usually used to improve the bioavailability of hydrophobic drugs. However, conventional SMEDDS are mostly prepared in a liquid form, which can have several disadvantages. Accordingly, solid SMEDDS (S-SMEDDS) prepared by solidification of liquid/semisolid self-micron emulsifying (SME) ingredients into powders have gained popularity. This article provides an overview of the recent advancements in S-SMEDDS such as methodology, techniques and future research directions.

Biologically Active 2,5-Disubstituted-1,3,4-Oxadiazoles

2009 ◽  
Vol 2 (1) ◽  
pp. 390-406
Author(s):  
Harish Rajak ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
Heterocyclic Compounds ◽  
Medical Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Clinical Use ◽  
Synthetic Drugs ◽  
Physiologic Activity ◽  
Pharmacologically Active

There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.

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