Dihydropyrimidinones scaffold as a promising nucleus for synthetic profile and various therapeutic targets: A Review

2020 ◽  
Vol 17 ◽  
Author(s):  
Shaik Khasimbi ◽  
Faraat Ali ◽  
Kiran Manda ◽  
Anjali Sharma ◽  
Garima Chauhan ◽  
...  
Keyword(s):  
Biginelli Reaction ◽  
Critical Role ◽  
Heterocyclic Ring ◽  
Biological Profile ◽  
Design Synthesis ◽  
Wide Range ◽  
Review Reports ◽  
Relationship Of ◽  
Anti Hiv

Background:: This review elaborates the updated synthetic and pharmacological approaches of a known group of dihydropyrimidinones/thiones from the multi-component reaction like Biginelli reaction was named Pietro Biginelli in 1891. This review consists of the reaction of an aromatic aldehyde, urea and ethyl acetoacetate leading to dihydropyrimidinone/thione. Currently, the scientific movement to develop economically viable green methods using compounds that are reusable, non-volatile, easily obtained, etc. Objective:: This review covers the recent synthesis and pharmacological advancement of dihydropyrimidinones/thiones moiety, along with covering the structure-activity relationship of the most potent compounds, which may prove to become better, more efficacious and safer agents. Thus, this review may help the researchers in drug designing and development of new Dihydropyrimidinones entities. Conclusion:: This review focuses on the wide application of dihydropyrimidinone/thione review reports the design, synthesis and pharmacological activities of nitrogen-sulphur containing dihydropyrimidinone moiety by using multi-component reaction. Dihydropyrimidinones (DHPM) pharmacophore is an important heterocyclic ring in medicinal chemistry. It is derived from multi-component reactions, “Biginelli reaction” and plays critical role as anticancer, antioxidant, antimicrobial, antiinflammatory, anti-HIV-1, antimalarial, anti-inflammatory, antihypertensive and anti-tubercular agents. Exhaustive research has led to the determination of its vast biological profile, with a wide range of therapeutic application.

Enhanced myocyte-based biosensing of the blood-borne signals regulating chronotropy

2002 ◽  
Vol 92 (2) ◽  
pp. 581-585 ◽  
Author(s):  
Jay M. Edelberg ◽  
Jason T. Jacobson ◽  
David S. Gidseg ◽  
Lilong Tang ◽  
David J. Christini
Keyword(s):  
Cardiac Myocyte ◽  
Cardiac Tissue ◽  
Critical Role ◽  
Excitable Tissue ◽  
Time Determination ◽  
Molecular Plasticity ◽  
Relationship Of ◽  
High Degree

Biosensors play a critical role in the real-time determination of relevant functional physiological needs. However, typical in vivo biosensors only approximate endogenous function via the measurement of surrogate signals and, therefore, may often lack a high degree of dynamic fidelity with physiological requirements. To overcome this limitation, we have developed an excitable tissue-based implantable biosensor approach, which exploits the inherent electropotential input-output relationship of cardiac myocytes to measure the physiological regulatory inputs of chronotropic demand via the detection of blood-borne signals. In this study, we report the improvement of this application through the modulation of host-biosensor communication via the enhancement of vascularization of chronotropic complexes in mice. Moreover, in an effort to further improve translational applicability as well as molecular plasticity, we have advanced this approach by employing stem cell-derived cardiac myocyte aggregates in place of whole cardiac tissue. Overall, these studies demonstrate the potential of biologically based biosensors to predict endogenous physiological dynamics and may facilitate the translation of this approach for in vivo monitoring.

scholarly journals Magnetic droplet nucleation boundary in orthogonal spin-torque nano-oscillators

2016 ◽  
Vol 7 (1) ◽  
Author(s):  
Sunjae Chung ◽  
Anders Eklund ◽  
Ezio Iacocca ◽  
Seyed Majid Mohseni ◽  
Sohrab R. Sani ◽  
...  
Keyword(s):  
Critical Role ◽  
Perpendicular Magnetic Anisotropy ◽  
Accurate Method ◽  
Spin Transfer Torque ◽  
Spin Transfer ◽  
Spin Torque ◽  
Droplet Nucleation ◽  
Wide Range ◽  
Field Plane

Abstract Static and dynamic magnetic solitons play a critical role in applied nanomagnetism. Magnetic droplets, a type of non-topological dissipative soliton, can be nucleated and sustained in nanocontact spin-torque oscillators with perpendicular magnetic anisotropy free layers. Here, we perform a detailed experimental determination of the full droplet nucleation boundary in the current–field plane for a wide range of nanocontact sizes and demonstrate its excellent agreement with an analytical expression originating from a stability analysis. Our results reconcile recent contradicting reports of the field dependence of the droplet nucleation. Furthermore, our analytical model both highlights the relation between the fixed layer material and the droplet nucleation current magnitude, and provides an accurate method to experimentally determine the spin transfer torque asymmetry of each device.

scholarly journals Design, Synthesis, Molecular Docking and Biological Evaluation of Novel 2-[(2-{[5-(Pyridin-4-yl)-1, 3, 4-Oxadiazol-2-yl]Sulfanyl}Ethyl)Sulfanyl]-1,3-Benzoxazole

2021 ◽  
pp. 472-484
Author(s):  
Anees Fathima ◽  
H. M. Vagdevi ◽  
N. D. Jayanna ◽  
R. Mohammed Shafeeulla ◽  
. Subbaraju
Keyword(s):  
Amino Acids ◽  
Molecular Docking ◽  
Heterocyclic Ring ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Present Communication ◽  
Design Synthesis ◽  
Analysis Technique ◽  
Wide Range ◽  
Structural Activity Relationship

In the present communication, a simple and facile method was adopted to synthesize  a series of novel 2-[(2-{[5-(pyridin-4-yl)-1,3,4-oxadiazol-2-yl]sulfanyl}ethyl)sulfanyl]-1,3-benzoxazole by fusing 5-(pyridin-4-yl)-1,3,4-oxadiazole-2-thiol with substituted 2-[(2-bromoethyl)sulfanyl]-1,3-benzoxazole and 2-[(2-chloroethyl)sulfanyl]-1,3-benzoxazole to obtain heterocyclic ring systems of 1,3,4 oxadiazole linked benzoxazole  moiety. The synthesized compounds were characterized by the aid of LCMS, IR, 1H NMR, 13CNMR, and C, H, N analysis technique. All the newly synthesized compounds were assessed for antimicrobial, antioxidant and antitubercular activities against standard strains. Microbiological results showed that the compounds showcased a wide range of activities and further the results of antimicrobial, antioxidant and molecular docking studies revealed that the compounds 6c, 6d and 6e are more potent and displays excellent docking scores with various amino acids interaction like alkyl-alkyl, pi-alkyl and hydrogen bonding of antitubercular receptor H37R with benzoxazole moieties and displayed encouraging antitubercular results to 6c, 6d and 6e molecules. The structural activity relationship studies illuminated the obtained results.

STEM and ELS Observation of Early Oxide Formation on the Surface of Cr Thin Films

1980 ◽  
Vol 38 ◽  
pp. 412-413
Author(s):  
Fumio Watari ◽  
J. M. Cowley
Keyword(s):  
Thin Films ◽  
Optical System ◽  
Room Temperature ◽  
Oxide Formation ◽  
Initial Nucleation ◽  
Diffraction Patterns ◽  
Relationship Of ◽  
Multiple Twinning ◽  
Moderately High Temperature

STEM coupled with the optical system was used for the investigation of the early oxidation on the surface of Cr. Cr thin films (30 – 1000Å) were prepared by evaporation onto the polished or air-cleaved NaCl substrates at room temperature and 45°C in a vacuum of 10−6 Torr with an evaporation speed 0.3Å/sec. Rather thick specimens (200 – 1000Å) with various preferred orientations were used for the investigation of the oxidation at moderately high temperature (600 − 1100°C). Selected area diffraction patterns in these specimens are usually very much complicated by the existence of the different kinds of oxides and their multiple twinning. The determination of the epitaxial orientation relationship of the oxides formed on the Cr surface was made possible by intensive use of the optical system and microdiffraction techniques. Prior to the formation of the known rhombohedral Cr2O3, a thin spinel oxide, probably analogous to γ -Al203 or γ -Fe203, was formed. Fig. 1a shows the distinct epitaxial growth of the spinel (001) as well as the rhombohedral (125) on the well-oriented Cr(001) surface. In the case of the Cr specimen with the (001) preferred orientation (Fig. 1b), the rings explainable by spinel structure appeared as well as the well defined epitaxial spots of the spinel (001). The microdif fraction from 20A areas (Fig. 2a) clearly shows the same pattern as Fig. Ia with the weaker oxide spots among the more intense Cr spots, indicating that the thickness of the oxide is much less than that of Cr. The rhombohedral Cr2O3 was nucleated preferably at the Cr(011) sites provided by the polycrystalline nature of the present specimens with the relation Cr2O3 (001)//Cr(011), and by further oxidation it grew into full coverage of the rest of the Cr surface with the orientation determined by the initial nucleation.

Calculating the aerodynamics of vertical axis wind turbines

2012 ◽  
Vol 34 (3) ◽  
pp. 169-184 ◽  
Author(s):  
Hoang Thi Bich Ngoc
Keyword(s):  
Wind Turbine ◽  
Incidence Angle ◽  
Vertical Axis ◽  
Rotor Blades ◽  
Vertical Axis Wind Turbine ◽  
Horizontal Axis Wind Turbine ◽  
Velocity Triangle ◽  
Relationship Of ◽  
The Relationship

Vertical axis wind turbine technology has been applied last years, very long after horizontal axis wind turbine technology. Aerodynamic problems of vertical axis wind machines are discussible. An important problem is the determination of the incidence law in the interaction between wind and rotor blades. The focus of the work is to establish equations of the incidence depending on the blade azimuth, and to solve them. From these results, aerodynamic torques and power can be calculated. The incidence angle is a parameter of velocity triangle, and both the factors depend not only on the blade azimuth but also on the ratio of rotational speed and horizontal speed. The built computational program allows theoretically selecting the relationship of geometric parameters of wind turbine in accordance with requirements on power, wind speed and installation conditions.

Tire Treadwear — A Comprehensive Evaluation of the Factors: Generic Type, Aspect Ratio, Tread Pattern, and Tread Composition Part I: Introduction and Details on the Organization of the Program

1986 ◽  
Vol 14 (4) ◽  
pp. 201-218 ◽  
Author(s):  
A. G. Veith
Keyword(s):  
Aspect Ratio ◽  
Comprehensive Evaluation ◽  
Test Method ◽  
Interactive Effects ◽  
Data Analyses ◽  
Main Effect ◽  
Systematic Determination ◽  
Relationship Of ◽  
The Relationship

Abstract This four-part series of papers addresses the problem of systematic determination of the influence of several tire factors on tire treadwear. Both the main effect of each factor and some of their interactive effects are included. The program was also structured to evaluate the influence of some external-to-tire conditions on the relationship of tire factors to treadwear. Part I describes the experimental design used to evaluate the effects on treadwear of generic tire type, aspect ratio, tread pattern (groove or void level), type of pattern (straight rib or block), and tread compound. Construction procedures and precautions used to obtain a valid and functional test method are included. Two guiding principles to be used in the data analyses of Parts II and III are discussed. These are the fractional groove and void concept, to characterize tread pattern geometry, and a demonstration of the equivalence of wear rate for identical compounds on whole tread or multi-section tread tires.

Discovery of Antibacterial Agents Inhibiting the Energy-Coupling Factor (ECF) Transporters by Structure-Based Virtual Screening

2020 ◽  
Author(s):  
Eleonora Diamanti ◽  
Inda Setyawati ◽  
Spyridon Bousis ◽  
leticia mojas ◽  
lotteke Swier ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Energy Coupling ◽  
Coupling Factor ◽  
Design Synthesis ◽  
Screening Design ◽  
Starting Point ◽  
Wide Range ◽  
Vitamin Uptake

Here, we report on the virtual screening, design, synthesis and structure–activity relationships (SARs) of the first class of selective, antibacterial agents against the energy-coupling factor (ECF) transporters. The ECF transporters are a family of transmembrane proteins involved in the uptake of vitamins in a wide range of bacteria. Inhibition of the activity of these proteins could reduce the viability of pathogens that depend on vitamin uptake. Because of their central role in the metabolism of bacteria and their absence in humans, ECF transporters are novel potential antimicrobial targets to tackle infection. The hit compound’s metabolic and plasma stability, the potency (20, MIC Streptococcus pneumoniae = 2 µg/mL), the absence of cytotoxicity and a lack of resistance development under the conditions tested here suggest that this scaffold may represent a promising starting point for the development of novel antimicrobial agents with an unprecedented mechanism of action.<br>

DINAMIKA POLITIK PERSETUJUAN BERSAMA TENTANG PENETAPAN DESA ADAT DI KABUPATEN ROKAN HULU TAHUN 2014

2017 ◽  
Vol 15 (1) ◽  
pp. 21
Author(s):  
Haryo Suganda ◽  
Raja Muhammad Amin
Keyword(s):  
Regulatory Region ◽  
Field Research ◽  
Analysis Techniques ◽  
Political Dynamics ◽  
Political Interests ◽  
Wide Range ◽  
Information Method ◽  
Qualitative Descriptive ◽  
The Village

This study is motivated the identification of policies issued by the regional Governmentof Rokan Hulu in the form of Regulatory region number 1 by 2015 on the determination of thevillage and Indigenous Village. Political dynamics based on various interests against themanufacture of, and decision-making in the process of formation of the corresponding localregulations determination of Indigenous Villages in the Rokan Hulu is impacted to a verysignificantamount of changes from the initial draft of the number i.e. 21 (twenty one) the villagebecame Customary 89 (eighty-nine) the Indigenous Villages who have passed. Type of thisresearch is a qualitative descriptive data analysis techniques. The research aims to describe theState of the real situation in a systematic and accurate fact analysis unit or related research, aswell as observations of the field based on the data (information). Method of data collectionwas done with interviews, documentation, and observations through fieldwork (field research).The results of the research on the process of discussion of the draft local regulations andmutual agreement about Designation of Indigenous Villages in the Rokan Hulu is, showed thatthe political dynamics that occur due to the presence of various political interests, rejectionorally by Villagers who were judged to have met the requirements of Draft Regulations to beformulated and the area for the set to be Indigenous Villages, and also there is a desire fromsome villages in the yet to Draft local regulations in order to set the Indigenous village , there isa wide range of interests of these aspects influenced the agreement to assign the entire localVillage which is in the Rokan Hulu become Indigenous village, and the village of Transmigrationinto administrative Villages where the initiator of the changes in the number of IndigenousVillages in the Rokan Hulu it is the desire of the local Government of its own.

Synthesis and Biological Activity of Quaternary Quinolinium Salts: A Review

2020 ◽  
Vol 23 (21) ◽  
pp. 2271-2294 ◽  
Author(s):  
Divya Utreja ◽  
Shivali Sharma ◽  
Akhil Goyal ◽  
Komalpreet Kaur ◽  
Sonia Kaushal
Keyword(s):  
Tyrosine Kinases ◽  
Biological Activities ◽  
Polymeric Materials ◽  
Tubulin Polymerization ◽  
Quinoline Derivatives ◽  
Heterocyclic Chemistry ◽  
Biological Profile ◽  
Drug Candidates ◽  
Anti Hiv ◽  
Quinolinium Salts

Heterocyclic chemistry is the only branch of chemistry that has applications in varied areas such as dyes, photosensitizers, coordination compounds, polymeric materials, biological, and many other fields. Quinoline and its derivatives have always engrossed both synthetic chemists and biologists because of their diverse chemical and pharmacological properties as these ring systems can be easily found in various natural products, especially in alkaloids. Among alkaloids, quinoline derivatives i.e. quinolinium salts have attracted much attention nowadays owing to their diverse biological profile such as antimicrobial, antitumor, antifungal, hypotensive, anti-HIV, analgesics and anti-inflammatory, etc. Quinoline and its analogs have recently been examined for their modes of function in the inhibition of tyrosine kinases, proteasome, tubulin polymerization, topoisomerase, and DNA repair. These observations have been guiding scientists for the expansion of new quinoline derivatives with improved and varied biological activities. Quinolinium salts have immense possibilities and scope to investigate these compounds as potential drug candidates. Therefore, we shall present a concise compilation of this work to aid in present knowledge and to help researchers explore an interesting quinoline class having medicinal potential.

Antineoplastic Activity, Structural Modification, Synthesis and Structure-activity Relationship of Dammarane-type Ginsenosides: An Overview

2019 ◽  
Vol 23 (5) ◽  
pp. 503-516 ◽  
Author(s):  
Qiang Zhang ◽  
Xude Wang ◽  
Liyan Lv ◽  
Guangyue Su ◽  
Yuqing Zhao
Keyword(s):  
Structural Modification ◽  
Gastrointestinal Disease ◽  
Structure Activity Relationship ◽  
Cerebrovascular Diseases ◽  
Activity Relationship ◽  
Cycle Arrest ◽  
Structure Activity ◽  
Wide Range ◽  
Structural Association ◽  
Relationship Of

Dammarane-type ginsenosides are a class of tetracyclic triterpenoids with the same dammarane skeleton. These compounds have a wide range of pharmaceutical applications for neoplasms, diabetes mellitus and other metabolic syndromes, hyperlipidemia, cardiovascular and cerebrovascular diseases, aging, neurodegenerative disease, bone disease, liver disease, kidney disease, gastrointestinal disease and other conditions. In order to develop new antineoplastic drugs, it is necessary to improve the bioactivity, solubility and bioavailability, and illuminate the mechanism of action of these compounds. A large number of ginsenosides and their derivatives have been separated from certain herbs or synthesized, and tested in various experiments, such as anti-proliferation, induction of apoptosis, cell cycle arrest and cancer-involved signaling pathways. In this review, we have summarized the progress in structural modification, shed light on the structure-activity relationship (SAR), and offered insights into biosynthesis-structural association. This review is expected to provide a preliminary guide for the modification and synthesis of ginsenosides.

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