FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2908377580> ?p ?o ?g. }

• W2908377580 abstract "Prion disease is also known as transmissible spongiform encephalopathies (TSEs). They are incurable and fatal neurodegenerative diseases influencing both humans and animals. There is no effective cure for the TSEs currently available and this is of special concern in European countries. TSEs can be potentially represented as inherited, sporadic and iatrogenic. In this project a library of heterocyclic compounds synthesised was screened in scrapie cell line (SMB) hoping to find novel anti-prion lead compounds. The work outlined in this thesis consists of ten chapters:Chapter one contains a general introduction of heterocyclic compounds and their use in drug discovery. It also contains an overview of ketoacids chemistry, isocyanides and multicomponent reactions as efficient ways for synthesising diverse and various heterocyclic compounds. In addition, explains subject aims and objectives. Chapter two describes a method for the synthesis of keto acids, isocyanides and convertible isocyanide from cheap stating materials and the synthesis of cyclic amides (lactams) by multicomponent reactions (3C-4C-Ugi reaction). The methodology which depends on the activation of keto acids (Carboxylic group) using PPTS is an excellent route to accomplish Meyer’s lactamaztion in good yields. The optimisation and diastereoselectivity of all reactions are also discussed. Chapter three describes the synthesis of Ugi-tetrazole derivatives and information about using flow chemistry in this work. The results were investigated of similar reactions achieved using either batch or flow machines. Chapter four describes efforts towards using a microwave technique for synthesis a group of pyrazol-oxopyrrolidine derivatives with satisfactory yields. Chapter five includes an efficient methodology utilized to synthesize isoqunoline and isoindoline libraries from α-ketoacids and β-ketoacids in order to showcase the benefit of α- and β-ketoacids for synthesis of diverse heterocyclic compounds. Chapter six outlines exploiting post-transformations of multicomponent products for synthesis of diverse and various heterocycles with good yields. A central goal of further expansion is to provide collections of stereo chemically and structurally diverse compounds in order to evaluate their biological systems. The reaction of convertible isocyanide for synthesising pyroglutamic acid analogues is described. A developed method includes using bifunctional keto acids or amines via multicomponent reactions and their post-transformations for synthesis of tetrazole-lactams, diones, pyrrole-oxopyrrolidine and a set of medicinally-valuable pyrrolo-pyridine derivatives under mild conditions are also described. Chapter seven describes the main target of all synthesised compounds evaluated as anti-prion diseases. These compounds are designed to bind a putative binding pocket of PrPC and stabilise the normal isoform. This should prevent its conversion into the infectious isoform (PrPS) in brain. Chapter eight, nine and ten contain conclusion and future work, data of all experimental procedures and references respectively." @default.
• W2908377580 created "2019-01-11" @default.
• W2908377580 creator A5077666523 @default.
• W2908377580 date "2018-10-01" @default.
• W2908377580 modified "2023-09-26" @default.
• W2908377580 title "Synthesis of Heterocyclic Compounds Using ketoacids-based Multicomponent Reactions and Evaluation of Their Anti-prion Activities" @default.
• W2908377580 hasPublicationYear "2018" @default.
• W2908377580 type Work @default.
• W2908377580 sameAs 2908377580 @default.
• W2908377580 citedByCount "0" @default.
• W2908377580 crossrefType "dissertation" @default.
• W2908377580 hasAuthorship W2908377580A5077666523 @default.
• W2908377580 hasConcept C178790620 @default.
• W2908377580 hasConcept C185592680 @default.
• W2908377580 hasConcept C21951064 @default.
• W2908377580 hasConcept C2777010268 @default.
• W2908377580 hasConcept C55493867 @default.
• W2908377580 hasConcept C70721500 @default.
• W2908377580 hasConcept C74187038 @default.
• W2908377580 hasConcept C86803240 @default.
• W2908377580 hasConceptScore W2908377580C178790620 @default.
• W2908377580 hasConceptScore W2908377580C185592680 @default.
• W2908377580 hasConceptScore W2908377580C21951064 @default.
• W2908377580 hasConceptScore W2908377580C2777010268 @default.
• W2908377580 hasConceptScore W2908377580C55493867 @default.
• W2908377580 hasConceptScore W2908377580C70721500 @default.
• W2908377580 hasConceptScore W2908377580C74187038 @default.
• W2908377580 hasConceptScore W2908377580C86803240 @default.
• W2908377580 hasLocation W29083775801 @default.
• W2908377580 hasOpenAccess W2908377580 @default.
• W2908377580 hasPrimaryLocation W29083775801 @default.
• W2908377580 hasRelatedWork W164176098 @default.
• W2908377580 hasRelatedWork W2008495872 @default.
• W2908377580 hasRelatedWork W2011628482 @default.
• W2908377580 hasRelatedWork W2107042901 @default.
• W2908377580 hasRelatedWork W2139113438 @default.
• W2908377580 hasRelatedWork W2174378679 @default.
• W2908377580 hasRelatedWork W2335728053 @default.
• W2908377580 hasRelatedWork W2580211573 @default.
• W2908377580 hasRelatedWork W2749843143 @default.
• W2908377580 hasRelatedWork W2751063237 @default.
• W2908377580 hasRelatedWork W2801848810 @default.
• W2908377580 hasRelatedWork W2904670098 @default.
• W2908377580 hasRelatedWork W2909494471 @default.
• W2908377580 hasRelatedWork W2949885218 @default.
• W2908377580 hasRelatedWork W2950452833 @default.
• W2908377580 hasRelatedWork W3203473543 @default.
• W2908377580 hasRelatedWork W3210236610 @default.
• W2908377580 hasRelatedWork W3772171 @default.
• W2908377580 hasRelatedWork W588925716 @default.
• W2908377580 hasRelatedWork W1957331332 @default.
• W2908377580 isParatext "false" @default.
• W2908377580 isRetracted "false" @default.
• W2908377580 magId "2908377580" @default.
• W2908377580 workType "dissertation" @default.