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Design and Implementation of a Laboratory-Based Drug Design and Synthesis Advanced Pharmacy Practice Experience
APPE research drug design synthesis medicinal chemistry
2018/8/17
Objective. To provide students with an opportunity to participate in medicinal chemistry research within the doctor of pharmacy (PharmD) curriculum.
Design. We designed and implemented a 3-course seq...
Total Synthesis of (±)-Decursivine and (±)-Serotobenine: A Witkop Photocyclization/Elimination/O-Michael Addition Cascade Approach
Total Synthesis of (±) Decursivine and (±)-Serotobenine A Witkop Photocyclization/Elimination/O-Michael Addition Cascade Approach
2012/7/3
Decursivine和Serotobenine是一类具有苯并二氢呋喃，吲哚并八元内酰胺多环体系的吲哚生物碱，分别具有抗疟疾及广泛的抗菌活性，其良好的生物活性和独特新颖的结构，引起了合成化学家的关注。其中Michael A. Kerr小组以18步3%的总收率首次完成了(±)-Decursivine的全合成，Tohru Fukuyama小组以24步8%的总收率首次完成了(-)-Serotobenin...
Synthesis of metronidazole derivatives as antigiardiasis agents
Metronidazole Giardiasis Imidazole Epoxide
2010/4/6
Metronidazole (MTZ) and its derivatives have been extensively used to treat infections caused by protozoa and anaerobic bacteria. In this investigation several novel imidazole and nitroimidazol deriva...
Synthesis and smooth muscle Calcium channel antagonist effects of new derivatives of 1,4-Dihydropyridine containing Nitroimidazol substituent
Dihydropyridine Calcium channels antagonist GPILSM
2009/12/29
A group of racemic 3-[(2-hydroxyethyl), (2-Methoxyethyl), (2-acetylethyl) or (2-cyanoethyl)], 5- methyl, ethyl or isopropyl-1, 4-dihydro-2, 6-dimethyl-4-(1-methyl-5-nitro-2-imidazolyl)-3, 5-pyridinedi...
Synthesis and in vitro dual calcium channel antagonist-agonist activity of some 1, 4-Dihydo-2,6-dimethyl-3-nitro and cyano-4-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-pyridinecarboxylates
Calcium channel antagonist-agonist activity Dihydropyridines QSAR
2009/12/14
Background and purpose of the study: The vasorelaxant action of the dihydropyridines (DHPs) provides many useful clinical indications. However, their negative effects on cardiac contractility is still...
SYNTHESIS AND ANTICONVULSANT ACTIVITY OF NOVEL 2-AMINO-5-[4-CHLORO-2-(2-CHLOROPHENOXY) PHENYL]-1,3,4-THIADIAZOLE DERIVATIVES
1,3,4-thiadiazole Anticonvulsant activity Maximal electroshock
2010/4/9
Several novel 2-amino-5-[4-chloro-2-(2-chlorophenoxy)phenyl]-1,3,4-thiadiazole derivatives 4a-d were synthesized and their anticonvulsant activity was determined by evaluation of the ability of theses...
Mechanism-Based Inhibitors of Deoxythymidine Synthesis as Neoplastic Agents
Mechanism-Based Inhibitors Deoxythymidine Synthesis Neoplastic Agents
2016/3/10
5-Fluorouracil and methotrexate are antimetabolites widely used in the treatment of neoplastic disease. They act by inactivating the two enzymes involved in the biosynthesis of the pyrimidine nucleoti...