Structural Activity Relationship-based Medicinal perspectives of Pyrimidine derivatives as Anti-Alzheimer’s Agent: A Comprehensive Review

2021 ◽  
Vol 20 ◽  
Author(s):  
Subham Das ◽  
Saleem Akbar ◽  
Bahar Ahmed ◽  
Rikeshwar Prasad Dewangan ◽  
Asif Iqubal ◽  
...  
Keyword(s):  
Neurological Disorder ◽  
Membered Ring ◽  
Literature Survey ◽  
Pyrimidine Derivatives ◽  
New Era ◽  
Development Organizations ◽  
Structural Activity Relationship ◽  
Alternative Position ◽  
Sar Study ◽  
Pyrimidine Moiety

: Pyrimidine is an aromatic and heterocyclic organic compound containing a 6-membered ring consisting of four carbon and two nitrogen atoms on an alternative position. Pyrimidine scaffolds described its existence between the medicinal chemist’s cause of its synthesizing practicability and nonpoisonous nature. However, the reason behind the neurological disorder is still an open challenge in scientific research and development organizations. Despite high throughput research in the field of anti-Alzheimer’s drugs, the efficacy void is quite common before the researchers. Researchers have constantly investigated all the probabilities to restraint the unwanted adverse effects of the anti-Alzheimer’s agents or focusing on a more considerable perspective to decline or rehabilitate neurological disorder. The drug development has revealed aspiration to medicinal chemists and researchers to felicitate research by look over through a considerable literature survey. Therefore, the SAR study-based approach has been emphasized that pharmacological advancements of Pyrimidine moiety in the new era as therapeutics anti-Alzheimer’s agents.

scholarly journals Faxian’s Biography and His Contributions to Asian Buddhist Culture: Latest Textual Analysis

2015 ◽  
Vol 8 (1) ◽  
pp. 38 ◽  
Author(s):  
Xican Li
Keyword(s):  
Textual Analysis ◽  
Literature Survey ◽  
Shanxi Province ◽  
Accurate Information ◽  
Asian Countries ◽  
New Era ◽  
Ancient India ◽  
Jin Dynasty ◽  
The Poor ◽  
Buddhist Culture

<p class="1Body">To provide more updated and accurate information on Faxian, an eminent monk of ancient China’s Jin Dynasty (266–421 CE), the present study conducts a literature survey to analyze his native region. It is found that Faxian was actually born in modern Linfen City in Shanxi Province, not Xiangyuan County as previously described. In his childhood, he became a novice monk and was compassionate toward the poor. To search out and collect Buddhist scriptures, Faxian undertook a westward pilgrimage to India from 399 to 412 CE. During this hard and dangerous pilgrimage, Faxian burst into tears three times. Finally, he succeeded in bringing a trove of Buddhist scriptures back to China from India. For the rest of his life, along with Buddhabhadra, he was engaged in translating Buddhist scriptures into Chinese. These translated scriptures were highly beneficial for Chinese Buddhism, especially the precepts (sila-vinaya) and Mahāyāna works. Faxian himself is demonstrated to have been a Mahāyāna Buddhist follower. His pilgrimage experience was recorded in his work “Record of Buddhist Kingdoms”, which provides important information about ancient Asian kingdoms. Faxian’s story promoted Asian tourism relevant to Buddhist culture. As a pioneer in the 4<sup>th</sup> century, Faxian started a new era of westbound pilgrimage to ancient India, including the similar pilgrimages of Xuanzang and Yijing in the 7<sup>th</sup> century. Even today, Faxian continues to strengthen friendship among Asian countries.</p>

scholarly journals The Flögel-three-component reaction with dicarboxylic acids – an approach to bis(β-alkoxy-β-ketoenamides) for the synthesis of complex pyridine and pyrimidine derivatives

2014 ◽  
Vol 10 ◽  
pp. 394-404 ◽  
Author(s):  
Mrinal K Bera ◽  
Moisés Domínguez ◽  
Paul Hommes ◽  
Hans-Ulrich Reissig
Keyword(s):  
Dft Calculations ◽  
Carboxylic Acids ◽  
Aromatic Compounds ◽  
Dicarboxylic Acids ◽  
Membered Ring ◽  
Simple Synthesis ◽  
Pyrimidine Derivatives ◽  
Three Component Reaction ◽  
Palladium Catalyzed ◽  
Pyridine And Pyrimidine Derivatives

An extension of the substrate scope of the Flögel-three-component reaction of lithiated alkoxyallenes, nitriles and carboxylic acids is presented. The use of dicarboxylic acids allowed the preparation of symmetrical bis(β-ketoenamides) from simple starting materials in moderate yields. Cyclocondensations of these enamides to 4-hydroxypyridine derivatives or to functionalized pyrimidines efficiently provided symmetrically and unsymmetrically substituted fairly complex (hetero)aromatic compounds containing up to six conjugated aryl and hetaryl groups. In addition, subsequent functionalizations of the obtained heterocycles by palladium-catalyzed couplings or by oxidations are reported. We also describe the simple synthesis of a structurally interesting macrocyclic bispyrimidine derivative incorporating a 17-membered ring, whose configuration was elucidated by DFT calculations and by subsequent reactions.

scholarly journals Crystal structure of (E)-13-(pyrimidin-5-yl)parthenolide

2015 ◽  
Vol 71 (12) ◽  
pp. 1536-1538 ◽  
Author(s):  
Shobanbabu Bommagani ◽  
Narsimha R. Penthala ◽  
Sean Parkin ◽  
Peter A. Crooks
Keyword(s):  
Crystal Structure ◽  
Title Compound ◽  
Heck Reaction ◽  
Lactone Ring ◽  
Chair Conformation ◽  
Ring System ◽  
Membered Ring ◽  
Reaction Conditions ◽  
Compound C ◽  
Pyrimidine Moiety

The title compound, C19H22N2O3, {systematic name (1aR,4E,7aS,8E,10aS,10bR)-1a,5-dimethyl-8-[(pyrimidin-5-yl)methylidene]-2,3,6,7,7a,8,10a,10b-octahydrooxireno[2′,3′:9,10]cyclodeca[1,2-b]furan-9(1aH)-one} was obtained from the reaction of parthenolide [systematic name (1aR,7aS,10aS,10bR,E)-1a,5-dimethyl-8-methylene-2,3,6,7,7a,8,10a,10b-octahydrooxireno[2′,3′:9,10]cyclodeca[1,2-b]furan-9(1aH)-one] with 5-bromopyrimidine under Heck reaction conditions, and was identified as anEisomer. The molecule possesses ten-, five- (lactone) and three-membered (epoxide) rings with a pyrimidine group as a substituent. The ten-membered ring displays an approximate chair–chair conformation, while the lactone ring shows a flattened envelope-type conformation. The dihedral angle between the pyrimidine moiety and the lactone ring system is 29.43 (7)°.

Design, Synthesis and SAR Study of Novel Spiro [Pyrimido[5,4-b]Quinoline-10,5′-Pyrrolo[2,3-d]Pyrimidine] Derivatives as Promising Anticancer Agents

2018 ◽  
Vol 55 (10) ◽  
pp. 2297-2302 ◽  
Author(s):  
Asha V. Chate ◽  
Sagar P. Kamdi ◽  
Amruta N. Bhagat ◽  
Chetan K. Jadhav ◽  
Amol Nipte ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Sar Study

An unusual tert-butylamine mediated conversion of 6-aryl-7-formyl-2,4,5,8-tetrahydro-1,3-dioxa-5-azocines to 1,2,3,6-tetrahydropyrimidine derivatives

1990 ◽  
Vol 55 (10) ◽  
pp. 2502-2509 ◽  
Author(s):  
Ladislav Štibrányi ◽  
Lubor Fišera ◽  
Rastislav Káčer ◽  
Vladimír Oremus ◽  
Martina Mihulová
Keyword(s):  
Membered Ring ◽  
Dipolar Cycloaddition ◽  
Reaction Sequence ◽  
Pyrimidine Derivatives ◽  
Reaction Conditions ◽  
Photochemical Rearrangement ◽  
Tert Butylamine

An unexpected contraction of the 8-membered ring to a 6-membered one occurring when 6-aryl-7-formyl-2,4,5,8-tetrahydro-1,3-dioxa-5-azocines II were treated with tert-butylamine afforded 4-aryl-5-formyl-1-(1,1-dimethylethyl)-1,2,3,6-tetrahydropyrimidines III. Reaction conditions for the photorearrangement of chlorophenyl-substituted condensed isoxazolines I to II were worked out. The reaction sequence: 1,3-dipolar cycloaddition, photochemical rearrangement, treatment with tert-butylamine constitutes a new route to pyrimidine derivatives from 2H,4H,7H-1,3-dioxepine.

scholarly journals Synthesis of Novel 2-(Pyridin-2-yl) Pyrimidine Derivatives and Study of Their Anti-Fibrosis Activity

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5226
Author(s):  
Yi-Fei Gu ◽  
Yue Zhang ◽  
Feng-li Yue ◽  
Shao-tong Li ◽  
Zhuo-qi Zhang ◽  
...  
Keyword(s):  
Biological Activities ◽  
Collagen Type I ◽  
Type I ◽  
The Novel ◽  
Pyrimidine Derivatives ◽  
Wide Range ◽  
Ic50 Values ◽  
Privileged Structures ◽  
Pyrimidine Moiety

A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare libraries of novel heterocyclic compounds with potential biological activities, a series of novel 2-(pyridin-2-yl) pyrimidine derivatives were designed, synthesized and their biological activities were evaluated against immortalized rat hepatic stellate cells (HSC-T6). Fourteen compounds were found to present better anti-fibrotic activities than Pirfenidone and Bipy55′DC. Among them, compounds ethyl 6-(5-(p-tolylcarbamoyl)pyrimidin-2-yl)nicotinate (12m) and ethyl 6-(5-((3,4-difluorophenyl)carbamoyl)pyrimidin-2-yl)nicotinate (12q) show the best activities with IC50 values of 45.69 μM and 45.81 μM, respectively. Furthermore, the study of anti-fibrosis activity was evaluated by Picro-Sirius red staining, hydroxyproline assay and ELISA detection of Collagen type I alpha 1 (COL1A1) protein expression. Our study showed that compounds 12m and 12q effectively inhibited the expression of collagen, and the content of hydroxyproline in cell culture medium in vitro, indicating that compounds 12m and 12q might be developed the novel anti-fibrotic drugs.

Internet Based Drug Design of New Opioid Analgesics

2018 ◽  
Vol 5 (3) ◽  
Author(s):  
Avnish Kaur ◽  
Meenakshi Mehra ◽  
Mumtaz Ahmed
Keyword(s):  
Drug Design ◽  
Therapeutic Potential ◽  
Opioid Analgesic ◽  
Opioid Analgesics ◽  
Rational Drug Design ◽  
Input Structure ◽  
Rational Drug ◽  
Structural Activity Relationship ◽  
Sar Study ◽  
Use Of Internet

The development of new drug with its therapeutic potential is one of the most vital process in pharmaceutical industry. Now a day, there is development and importance of computational chemistry including molecular docking and a SAR study which deals with pharmacophore based drug design approach. Also, the methodology linked with modification of the target based drug discovery has been performed by using various computational tools. Thus, the present study deals with the Structural Activity Relationship study and pharmacophore based drug design approaches with the use of internet based tools which are free of cost and compatible with any platform. Here, attempts are made to design OPIORPHIN analogue by pharmacophore study to design more potent or equivalent opioid analgesic using free internet based tools by using Java platform to input structure, calculate its drug likeness, molecular properties and toxicity which are important parameters for structure based rational drug design.

scholarly journals Bicyclic Basic Merbarone Analogues as Antiproliferative Agents

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 557
Author(s):  
Andrea Spallarossa ◽  
Matteo Lusardi ◽  
Chiara Caneva ◽  
Aldo Profumo ◽  
Camillo Rosano ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Side Chain ◽  
The Novel ◽  
Bioactive Conformation ◽  
Pyrimidine Derivatives ◽  
Topoisomerase Iiα ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Step Procedure ◽  
Pyrimidine Moiety

Pyrimido-pyrimidine derivatives have been developed as rigid merbarone analogues. In a previous study, these compounds showed potent antiproliferative activity and efficiently inhibited topoisomerase IIα. To further extend the structure–activity relationships on pyrimido-pyrimidines, a novel series of analogues was synthesized by a two-step procedure. Analogues 3–6 bear small alky groups at positions 1 and 3 of the pyrimido-pyrimidine scaffold whereas at position 6a (4-chloro)phenyl substituent was inserted. The basic side chains introduced at position 7 were selected on the basis of the previously developed structure–activity relationships. The antiproliferative activity of the novel compounds proved to be affected by both the nature of the basic side chain and the substituents on the pyrimido-pyrimidine moiety. Derivatives 5d and 5e were identified as the most promising molecules still showing reduced antiproliferative activity in comparison with the previously prepared pyrimido-pyrimidine analogues. In topoisomerase IIα-5d docking complex, the ligand would poorly interact with the enzyme and assume a different orientation in comparison with 1d bioactive conformation.

Fused and Substituted Pyrimidine Derivatives as a Profound Anticancer Agent

2020 ◽  
Vol 20 ◽  
Author(s):  
Nahid Abbas ◽  
Gurubasavaraja S.P. Matada ◽  
Prasad S. Dhiwar ◽  
Shilpa Patel ◽  
Giles Devasahayam
Keyword(s):  
Small Molecules ◽  
Anticancer Agent ◽  
Targeted Agents ◽  
Pyrimidine Derivatives ◽  
Biological Targets ◽  
Routes Of Administration ◽  
Heterocyclic Molecules ◽  
Structural Activity Relationship ◽  
Synthetic Approaches ◽  
Relationship Of

: The rationale behind drug design is strategic utilization of heterocyclic fragments with specific physicochemical properties to form molecular targeted agents. Among the heterocyclic molecules, pyrimidine has proved to be a privileged pharmacophore for various biological cancer targets. The anticancer potential of small molecules with fused and substituted pyrimidine can be enhanced through bioisosteric replacements and altering their ADME parameters. Despite of several small molecules used in cancer chemotherapy, oncology therapeutics has various limitations. Especially in their routes of administration and their concurrent side effects. Such pernicious effects may be overcome, via selective biological targeting. In this review we have discussed the biological targets to inhibit cancer. Structural activity relationship of fused and substituted pyrimidine was studied. Eco friendly synthetic approaches for pyrimidine derivatives have been discussed. This review will give an insight to scientists and researchers of medicinal chemistry discipline to design small molecules having a pyrimidine scaffold with high anticancer potential.

scholarly journals An Insight into the Current Understanding of Status Epilepticus: From Concept to Management

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Khouloud Abdulrhman Al-Sofyani
Keyword(s):  
Status Epilepticus ◽  
Neurological Disorder ◽  
Molecular Mechanisms ◽  
Management Program ◽  
Literature Survey ◽  
Current Understanding ◽  
Extensive Literature ◽  
Mortality And Morbidity ◽  
Diagnosis And Management ◽  
Insight Into

Status epilepticus (SE), a subset of epilepsy, represents a debilitating neurological disorder often associated with alarming mortality and morbidity numbers. Even though SE is one of the extensively researched topics with conspicuous data available in the literature, a scientific gap exists in understanding the heterogeneous facets of the disorder like occurrence, definition, classification, causes, molecular mechanisms, etc., thereby providing a defined management program. Cognizance of this heterogeneity and scientific limitation with its subsequent correlation to the recent advancements in medical and scientific domains would serve not only in bridging the gap but also in developing holistic and prompt management programs. Keeping this as an objective, an extensive literature survey was performed during this study, and key findings have been shared. The present study provides a semantic and perspective synopsis toward acknowledging the diversified nature of SE and its variants with respect to their definition, classification, etiology, diagnosis, and management.

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