Design, Synthesis and Biological Evaluation of Non-Peptidic Bivalent ligands (Record no. 21605)
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| 000 -LEADER | |
|---|---|
| fixed length control field | 02136nam a22001577a 4500 |
| 005 - DATE AND TIME OF LATEST TRANSACTION | |
| control field | 20220923145345.0 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 220719b ||||| |||| 00| 0 eng d |
| 082 ## - DEWEY DECIMAL CLASSIFICATION NUMBER | |
| Classification number | 547.2 |
| Item number | D4601 |
| 100 ## - MAIN ENTRY--PERSONAL NAME | |
| Student name | Tanveer Ahmed, |
| Class | MPhil(chemistry) |
| Session | 2015-2017 |
| Supervisor | Supervised by Dr.Mehr-un-Nisa |
| 245 ## - TITLE STATEMENT | |
| Title | Design, Synthesis and Biological Evaluation of Non-Peptidic Bivalent ligands |
| Statement of responsibility, etc | /Tanveer Ahmed |
| 260 ## - PUBLICATION, DISTRIBUTION, ETC. (IMPRINT) | |
| Place of publication, distribution, etc | Lahore : |
| Name of publisher, distributor, etc | Department of Chemistry, Div. S&T, University of Education, |
| Date of publication, distribution, etc | 2017 |
| 300 ## - PHYSICAL DESCRIPTION | |
| Extent | 110 p. |
| Other physical details | xxi |
| Accompanying material | CD |
| 520 ## - SUMMARY, ETC. | |
| Summary, etc | Selective serotonin re-uptake inhibitors (SSRIs) is a novel class of antidepressants and opioids is a class of analgesics. Opioid and SSRIs Bivalent ligands (53-60) have been designed, synthesized by direct linkage (59, 60) of two pharmacophores i.e., opioid and SSRIs and by the introduction of some spacers/linkers (53-58) between them to minimize the adverse side effect profile and checked for their opioid and SSRIs<br/>activities for the treatment of pain and depression in a single molecule concurrently. For the design of opioids and SSRIs bivalent ligands (53-60) in Silicoand rational approaches have been applied. The synthesized bivalent ligands (53-60) have been characterized by spectroscopic analyses i.e1H NMR, 13C NMR, LRMS, HRMS. Multitarget screening of bivalent ligands (53-60) was carried out against all the brain receptors. Primary binding assay of opioid and SSRIs bivalent ligands (53-60) have<br/>been investigated for their μ, δ and κ-opioid and SSRIs receptors. Most of the bivalent ligands 54Ki μ =o.3nM, δ =o.7nM, κ = 6nM;56Ki μ =0.6nM, δ =0.54nM, κ=0.53nM;and 58Ki μ =0.4nM, δ =0.6nM, κ =2.6nMshowed high affinities and<br/>afficacies for μ δ and κ-opioid receptors and low affinities for SSRIs receptors. Later, functional assays of most effective ligands (53-60) have been carried out. Additional outcomes proved that these ligands (53-60) are excellent analgesics than bivalent ligands and hence could be designed in future as triple re-uptake inhibitors (TRIs) i.e., another class of antidepressants. |
| 650 ## - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name as entry element | Biological Evaluation - Bivalent ligands - Chemistry |
| 942 ## - ADDED ENTRY ELEMENTS (KOHA) | |
| Koha item type | Theses |
| Withdrawn status | Damaged status | Home library | Current library | Date acquired | Full call number | Barcode | Date last seen | Price effective from | Koha item type |
|---|---|---|---|---|---|---|---|---|---|
| UE-Central Library | UE-Central Library | 19.07.2022 | 547.2 D4601 | TTH38 | 19.07.2022 | 19.07.2022 | Theses |
