Molecular design of multitarget neuroprotective agents 5. Modification with pharmacologically active fragments of 4,4- and 1,4-dipropargyl-5-methyl-2-phenylpyrazol-3-one

2021 ◽  
Vol 70 (10) ◽  
pp. 2019-2022
Author(s):  
A. Yu. Aksinenko ◽  
T. V. Goreva ◽  
T. A. Epishina
Keyword(s):  
Molecular Design ◽  
Neuroprotective Agents ◽  
Active Fragments ◽  
Pharmacologically Active

scholarly journals A fast and efficient ‘on-solvent’ cascade assembling of salicylaldehydes and dimethylbarbituric acid into 5-(1,3-dimethyl-2,4-dioxo-1,3,4,5-tetrahydro-2H-chromeno[2,3-d]pyrimidin-5-yl)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-triones

2018 ◽  
Vol 24 (2) ◽  
pp. 79-83
Author(s):  
Michail N. Elinson ◽  
Anatoly N. Vereshchagin ◽  
Alexander D. Korshunov ◽  
Mikhail P. Egorov
Keyword(s):  
Cascade Reaction ◽  
Active Fragments ◽  
Pharmacologically Active

AbstractA fast (15 min) and efficient cascade reaction of salicylaldehydes and 1,3-dimethylbarbituric acid in the presence ofp-TsOH as a catalyst furnishes substituted 5-(1,3-dimethyl-2,4-dioxo-1,3,4,5-tetrahydro-2H-chromeno[2,3-d]pyrimidin-5-yl)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-triones1a–h, containing both chromeno[2,3-d]pyrimidine and hexahydropyrimidine-2,4,6-trione pharmacologically active fragments, in 95–99% yields. This new procedure is characterized by the use of inexpensive reagents and a simple workup.

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

Permeability Enhancing and Chemotactic Activities of Lower Molecular Weight Degradation Products of Human Fibrinogen

1981 ◽  
Vol 45 (01) ◽  
pp. 090-094 ◽  
Author(s):  
Katsuo Sueishi ◽  
Shigeru Nanno ◽  
Kenzo Tanaka
Keyword(s):  
Molecular Weight ◽  
Degradation Products ◽  
Electron Microscopic Observation ◽  
Chemotactic Activity ◽  
Lower Molecular Weight ◽  
Electron Microscopic ◽  
Human Fibrinogen ◽  
Rabbit Skin ◽  
Molecular Weights ◽  
Active Fragments

SummaryFibrinogen degradation products were investigated for leukocyte chemotactic activity and for enhancement of vascular permeability. Both activities increased progressively with plasmin digestion of fibrinogen. Active fragments were partially purified from 24 hr-plasmin digests. Molecular weights of the permeability increasing and chemotactic activity fractions were 25,000-15,000 and 25,000 respectively. Both fractions had much higher activities than the fragment X, Y, D or E. Electron microscopic observation of the small blood vessels in rabbit skin correlated increased permeability with the formation of characteristic gaps between adjoining endothelial cells and their contraction.These findings suggest that lower molecular weight degradation products of fibrinogen may be influential in contributing to granulocytic infiltration and enhanced permeability in lesions characterized by deposits of fibrin and/or fibrinogen.

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.

Thermodynamics of the interaction between the spike protein of severe acute respiratory syndrome- coronavirus-2 and the receptor of human angiotensin converting enzyme 2. Effects of possible ligands

2020 ◽  
Author(s):  
Cristina Garcia-Iriepa ◽  
Cecilia Hognon ◽  
Antonio Francés-Monerris ◽  
Isabel Iriepa ◽  
Tom Miclot ◽  
...  
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Molecular Mechanisms ◽  
Molecular Design ◽  
Binding Free Energy ◽  
Transmembrane Protein ◽  
Spike Protein ◽  
Converting Enzyme ◽  
Angiotensin Converting Enzyme 2 ◽  
Rational Molecular Design ◽  
Rational Evaluation

<div><p>Since the end of 2019, the coronavirus SARS-CoV-2 has caused more than 180,000 deaths all over the world, still lacking a medical treatment despite the concerns of the whole scientific community. Human Angiotensin-Converting Enzyme 2 (ACE2) was recently recognized as the transmembrane protein serving as SARS-CoV-2 entry point into cells, thus constituting the first biomolecular event leading to COVID-19 disease. Here, by means of a state-of-the-art computational approach, we propose a rational evaluation of the molecular mechanisms behind the formation of the complex and of the effects of possible ligands. Moreover, binding free energy between ACE2 and the active Receptor Binding Domain (RBD) of the SARS-CoV-2 spike protein is evaluated quantitatively, assessing the molecular mechanisms at the basis of the recognition and the ligand-induced decreased affinity. These results boost the knowledge on the molecular grounds of the SARS-CoV-2 infection and allow to suggest rationales useful for the subsequent rational molecular design to treat severe COVID-19 cases.</p></div>

Restriction of Access to Dark State: A New Mechanistic Model for Heteroatom-Containing AIE Systems

2019 ◽  
Author(s):  
Yujie Tu ◽  
Junkai Liu ◽  
Haoke Zhang ◽  
Qian Peng ◽  
Jacky W. Y. Lam ◽  
...  
Keyword(s):  
Excited States ◽  
Radiative Decay ◽  
Molecular Design ◽  
Mechanistic Model ◽  
Zinc Ion ◽  
Easy Access ◽  
Triplet States ◽  
Dark State ◽  
Ion Probe ◽  
Π State

Aggregation-induced emission (AIE) is an unusual photophysical phenomenon and provides an effective and advantageous strategy for the design of highly emissive materials in versatile applications such as sensing, imaging, and theragnosis. "Restriction of intramolecular motion" is the well-recognized working mechanism of AIE and have guided the molecular design of most AIE materials. However, it sometimes fails to be workable to some heteroatom-containing systems. Herein, in this work, we take more than one excited state into account and specify a mechanism –"restriction of access to dark state (RADS)" – to explain the AIE effect of heteroatom-containing molecules. An anthracene-based zinc ion probe named APA is chosen as the model compound, whose weak fluorescence in solution is ascribed to the easy access from the bright (π,π*) state to the closelying dark (n,π*) state caused by the strong vibronic coupling of the two excited states. By either metal complexation or aggregation, the dark state is less accessible due to the restriction of the molecular motion leading to the dark state and elevation of the dark state energy, thus the emission of the bright state is restored. RADS is found to be powerful in elucidating the photophysics of AIE materials with excited states which favor non-radiative decay, including overlap-forbidden states such as (n,π*) and CT states, spin-forbidden triplet states, which commonly exist in heteroatom-containing molecules.

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.

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