Medicine and Health Sciences Commons^™

Synthesis, Chemistry, Biological Evaluation And Structure-Activity Relationships Of Rac- And Chiral 6-Desmethyl-5Β –Hydroxy-D-Secoartemisinin And Analogs, Mohamed Elsideiq Jihan

Electronic Theses and Dissertations

The prevention and cure of malaria is difficult as it thrives under poor socio- and pharmacoeconomic conditions in third world, tropical and subtropical regions. It is a parasitic disease spread through the bite of an infected Anopheles mosquito. In humans, malaria can be caused by several Plasmodium species that include: Plasmodium falciparum, Plasmodium vivax, Plasmodium ovale, Plasmodium malariae and Plasmodium knowlesi. The natural product artemisinin is a sesquiterpene lactone with an endoperoxide bridge isolated from the Chinese annual herb qinghao (Artemisia annua L or sweet wormwood). The relatively stable endoperoxide bridge is essential for their antimalarial activity. The synthesis of …

Protein-Ligand Interaction Studies And Identification Of New Drug-Like Hits As Cannabinoid Receptor Modulators, Pankaj Pandey

Electronic Theses and Dissertations

The cannabinoid receptors (CB1 and CB2) belong to the family of class A GPCRs. The CB1 receptor is predominately found in the central nervous system and regulates various neuromodulatory and physiological processes while CB2 receptors are found in peripheral tissues, particularly in the immune system tissues. This dissertation reports several projects including: (1) an examination of the putative binding modes of Cannabis-derived ligands with CB1 and CB2 receptors, (2) the identification of novel CB1 inverse agonists, and (3) the identification of allosteric site(s) in the CB2 receptor and screening of new CB2 allosteric modulators (AMs).

Chapter 1 describes background information …

Design, Synthesis, And Biological Evaluation Of Sigma Receptors (Σrs) Ligands As Potential Pharmacotherapy For Cancer And Drug Addiction, Walid Alsharif

Electronic Theses and Dissertations

Sigma receptors are a well-defined unique class of receptors and are highly expressed in the central nervous system and also widely distributed in peripheral organs and tissues. There are two subtypes of sigma receptors: sigma-1 and sigma-2. These receptors are thought to be associated with functions and disorders such as inflammation, depression, anxiety, Alzheimer’s disease, epilepsy and drug abuse. The sigma-1 receptor has been demonstrated to be involved in acute and chronic effects of cocaine and methamphetamine toxicities. However, the role of sigma-2 receptors is less clear due to the lack of availability of detailed protein structural information and truly …