Pharmacy and Pharmaceutical Sciences Commons^™

Hydrodynamic Characterization Of Laboratory And Production Equipment For Pharmaceutical Testing And Manufacturing Using Experimental And Computational Approaches, Chadakarn Sirasitthichoke

Dissertations

The hydrodynamics of process units used in pharmaceutical industry, i.e., the distribution of velocity profiles and shear stresses within the vessel, often controls the process performance, significantly affecting product quality. The hydrodynamics is strongly influenced by several factors such as the vessel shape, stirrer type, presence of internals and baffles, agitation intensity, and liquid properties. Most of these parameters can be varied by the process designers and the operators to achieve the desired process outcomes. The impact of the hydrodynamics on the process outcome can be profound in both large vessels (e.g., reactors) and smaller vessels (e.g., dissolution vessels), involving …

Biologic Tnf-Α Inhibitors Reduce Microgliosis, Neuronal Loss, And Tau Phosphorylation In A Transgenic Mouse Model Of Tauopathy, Weijun Ou, Joshua Yang, Juste Simanauskaite, Matthew Choi, Demi M. Castellanos, Rudy Chang, Jiahong Sun, Nataraj Jagadeesan, Karen D. Parfitt, David H. Cribbs, Rachita K. Sumbria

Pharmacy Faculty Articles and Research

Background

Tumor necrosis factor-α (TNF-α) plays a central role in Alzheimer’s disease (AD) pathology, making biologic TNF-α inhibitors (TNFIs), including etanercept, viable therapeutics for AD. The protective effects of biologic TNFIs on AD hallmark pathology (Aβ deposition and tau pathology) have been demonstrated. However, the effects of biologic TNFIs on Aβ-independent tau pathology have not been reported. Existing biologic TNFIs do not cross the blood–brain barrier (BBB), therefore we engineered a BBB-penetrating biologic TNFI by fusing the extracellular domain of the type-II human TNF-α receptor (TNFR) to a transferrin receptor antibody (TfRMAb) that ferries the TNFR into the brain via …

The Benefits Of Astaxanthin To Improve Pain Relief In Patients With Painful Diabetic Neuropathy: An Open-Label, Randomized Controlled Trial, Rizaldy Taslim Pinzon, Mary Rose Angelina Budi Harsana

Pharmaceutical Sciences and Research

Treatment of diabetic neuropathy is still carried out by providing symptomatic therapy, which only improves ± 50% of the total symptoms felt by patients, but does not tackle the underlying causes of the disease. Astaxanthin is a potent antioxidant, anti-inflammatory, and anti-diabetic carotenoid that could be an additional treatment option. We aimed to measure the effectiveness of administering astaxanthin as an additional therapy to improve the impact of pain and discomfort experienced daily by diabetes mellitus patients with painful diabetic neuropathy. We conducted a randomized experimental study with an open label design of 36 patients who had been diagnosed with …

Ameliorating Role Of Ulva Lactuca Extract On Neurobehavioral And Neurochemical Abnormalities Caused By Lithium In Rats, Samira Bouhalit, Noura Brahmi

Journal of Bioresource Management

Lithium is a relevant mood-stabilizing agent that is used in the management of depressive and manic episodes in bipolar, disorder; however, its application may cause diverse side effects including oxidative stress. This work investigated the neuroprotective and anti-stress activity of Ulva lactuca extract (MEUL) against lithium induced neuronal toxicity in rats. Lithium (2 g/kg) was administered in diets with or without MEUL (250 mg/kg BW by gavage) for 90 days. Lithium induced oxidative stress lead to an elevation in lipid peroxidation and oxidation protein product levels, a reduced superoxide dismutase, glutathione peroxidase activities, glutathione, and ascorbic acid concentrations in brain. …

The Effect Of Heparinoid As Systemic Prophylactic Anticoagulants On Covid-19 Patient Mortality And Its Safety Profiles: A Systematic Review And Meta-Analysis, Ariska Deffy Anggarany, Rani Sauriasari, Muhammad Alkaff, Famila Takhwifa, Hayatun Nufus, Diana Paramita

Pharmaceutical Sciences and Research

Coagulopathy is one of the complications of COVID-19 and is associated with a higher risk of mortality. However, evidence regarding the effectiveness and safety of anticoagulant therapy in various doses among COVID-19 patients is limited. This systematic review and meta-analysis aims to review and explore the effect of using heparinoids as a systemic anticoagulant at prophylactic doses on mortality in COVID-19 patients. Systematic searches were conducted of various databases (Pubmed, ScienceDirect, SpringerLink, Scopus, and ProQuest) covering the period 2019-2021. We assessed the quality of the articles using the STROBE checklist. Studies with a high risk of bias were excluded before …

Effect Of Propolis On Bone Quality And Cortical Bone Thickness Of Ovariectomized Female Wistar White Rats As A Model For Osteoporosis, Dian Ayu Juwita, Almahdy Ahmadin, Fitri Rachmaini, Rahmad Abdillah, Rosalia Medisa Fatma

Pharmaceutical Sciences and Research

Estrogen deficiency increases the rate of osteoporosis, especially in menopausal women, by altering the bone tissue microarchitecture. Propolis has compounds that could be used as an alternative therapy to treat estrogen deficiency and to protect against bone damage. This study aims to determine the effect of propolis on bone quality and cortical bone thickness of femoral metaphysis in ovariectomized female Wistar white rats as a model for menopausal osteoporosis. The rats were divided into five groups: negative control group (not subjected to ovariectomy), sham group (subjected to ovariectomy), and treatment groups that were subjected to ovariectomy and given propolis orally …

The Effect Of Pre-Extraction Preparation On Antioxidant Compounds Of Sauropus Androgynus (L.) Merr. Leaves Extracts, Ni Putu Ermi Hikmawanti, Sofia Fatmawati, Zainal Arifin, Niken Cahyaningrum, Muhammad Arif Fauzan

Pharmaceutical Sciences and Research

Sauropus androgynus (L.) Merr. (Phyllanthaceae) is a green vegetable. It is rich in natural antioxidant compounds such as phenolics and flavonoids. The pre-extraction preparation can affect the results of extracting compounds from natural materials. This study aims to determine the effect of pre-extraction procedures, including sample form (fresh/dried), drying process (oven-drying/indirect sunlight-drying/air-drying), and particle size (ground/powdered) on total phenolic and flavonoid levels of ethanolic extracts of S. androgynus leaves and their antioxidant activity against DPPH radicals. S. androgynus leaves were extracted using the cold maceration method. The total phenolic and flavonoid contents of the extract were determined by the colorimetric …

Comparative Analytical Study Of Phytochemicals In Selected Antidiabetic Medicinal Plant Seeds In Sri Lanka, Gowri Rajkumar, Mihiri Rangika Jayasinghe, Vinotha Sanmugarajah

Pharmaceutical Sciences and Research

Medicinal plants are universally used in the management of various diseases in different medical practices. A varied diversity of compounds extracted from plants may show anticancer, antibacterial, and antidiabetic activities. Comparative laboratory studies and scientific approach of efficacy related to phytochemicals found in medicinal plants in Sri Lanka have not been reported yet. This study aims to evaluate the phytochemicals in selected four different plant seeds such as Syzygium cumini (L.) Skeels, Brassica alba (L.) Rabenh, Trigonella foenum-graecum L. and Nigella sativa L., which are used in the management of diabetes mellitus in Sri Lanka. The ethanol extracts of …

The Efficacy Of Oral Ivabradine In Acute Phase In Non St-Segment Elevation Myocardial Infarction (Nstemi) Post Pci: A Pilot Study, Manar M. Ahmed, Maggie M. Abbassi, Gamal Shaaban, Samar F. Farid

Bulletin of Faculty of Pharmacy Cairo University

Background: An elevated heart rate is a major risk factor for cardiovascular mortality and morbidity. This study aims to evaluate the beneficial effect of heart rate reduction of oral ivabradine in patients presenting with non ST-segment elevation myocardial infarction (NSTEMI) during acute stage post percutaneous coronary intervention. Results: A total of 100 patients admitted to the emergency department, National Heart Institute, Cairo, Egypt, were randomized into two groups as follows: Group A: 50 patients with NSTEMI treated with ivabradine (5 mg twice daily) in addition to the conventional treatment; Group B: 50 patients with NSTEMI treated with the conventional treatment …

Knowledge, Attitude, Practices, And Barriers Of Pharmacovigilance Among Healthcare Workers: A Cross-Sectional Survey From Lahore, Pakistan, Zia U. Mustafa, Muhammad Salman, Noman Asif, Alina Z. Rao, Qurat U.A. Khan, Asma S. Nawaz, Muhammad W. Mumtaz, Athar Masood, Muhammad F.A. Khan, Naureen Shehzadi, Khalid Hussain

Bulletin of Faculty of Pharmacy Cairo University

Background: Adverse drug reactions (ADRs) are associated with increased length of hospital stay, permanent disability and even death. Objectives: The purpose of this study was to assess knowledge, attitude, practice (KAP), and barriers related to Pharmacovigilance (PV) among Pakistani healthcare workers (HCWs). Methods: A cross-sectional study was conducted in the second largest metropolitan city (Lahore) of Pakistan during a period of 4 months (JuneeSeptember 2018). A self-administered questionnaire was used to collect data from the doctors, pharmacists, and nurses from 8 tertiary care hospitals, recruited via convenient sampling. All data were analyzed in SPSS version 21. Results: A total of …

Study The Effects Of Taurine Oral Supplement Used For Type 2 Diabetic Patients On Body Weight; Glycemic Control And Some Bone Mineralization Biochemical Markers, Falah Hassan Sheri, Hiba Dawood, Jubran K. Hassan, Qais A. Aljazaeari

Bulletin of Faculty of Pharmacy Cairo University

Background: Taurine is sulfur containing semi-essential amino acid that has important roles in many biological processes, but; its effects on glucose homeostasis, weight; growth and bone mineralization were not well defined in human. Objectives: evaluation the effects of oral taurine used for 3 months on bone mineralization biomarker; glycemic control and body weight in type II diabetic patients. Methods: interventional double-blind placebo-controlled study in which 80 patients with type2 diabetes mellitus (age range 45e55) assigned in either control (n ¼ 40) or study (n ¼ 40) group. The last group received 1000 mg capsule of taurine once a -d for …

The Use Of Natural Polymers In Formation Of Polyelectrolyte Complexation, Niharika Lal, Athira Nair, Navneet Verma

Bulletin of Faculty of Pharmacy Cairo University

In recent years, great advances have been made towards the development of various techniques for novel drug delivery systems. These techniques focus on the rate of drug delivery, duration of action and site of action. One of such technique in fabricating novel drug delivery system is the use of polymers in development of in-situ drug delivery systems. Polymers used as carriers have revolutionized over the years. The formation of a polymer complex with other oppositely charged polymers resulted in the formation of polyelectrolyte complexes, which possess unique physicochemical properties with high biocompatibility. The polyelectrolyte's themselves are characterized as cationic, anionic …

Pharmacy-Led Medication Reconciliation Program Reduces Adverse Drug Events And Improves Satisfaction In A Community Hospital, L. Hayley Burgess, Joan Kramer, Carley Castelein, Joseph M. Parra, Victoria Timmons, Samantha Pickens, Sarah Fraker, Christopher Cameron Skinner

HCA Healthcare Journal of Medicine

Background

Pharmacy-led medication reconciliation identifies and corrects medication errors that can potentially cause moderate to severe harm. This research sought to identify the impact of pharmacy-led medication reconciliation on patient outcomes and describe the changes in healthcare workers’ perceptions of the program.

Methods

A pharmacy-led admission medication reconciliation program pilot started in July 2019, and a discharge medication reconciliation proof of concept was tested in September 2020 at a 432-bed hospital. The following periods were compared: August 2018 to February 2019 (pre-program implementation) and August 2019 to February 2020 (post-program implementation). Endpoints included patient outcomes, workforce productivity and interdisciplinary healthcare …

A Snapshot Investigation Into The Availability And Access To Codeine-Containing Medications Amongst The Irish Population., Katie O'Brien, Pádraig Mckeown, Joseph Phelan

International Undergraduate Journal of Health Sciences

Codeine phosphate is a mild to moderate analgesic and has a weak cough suppressant activity that is available to purchase as an over the counter (OTC) painkiller in Ireland as a compound product. In recent years, countries such as Australia have introduced laws that prohibit the sale of the drug without a valid prescription. This move by Australia begs the question as to why this legislation was introduced and should Ireland follow suit.

The primary aims of the study were to determine knowledge among the general public of codeine-containing medications and their usage levels. The survey also investigated whether current …

Development Of A Bamlanivimab Infusion Process In The Emergency Department For Outpatient Covid-19 Patients, Danny Pham, Sandy Wong, Christina T. Nguyen, Stephen C. Lee, Kimberly J. Won

Pharmacy Faculty Articles and Research

The coronavirus disease 2019 (COVID-19) pandemic has prompted the creation of new therapies to help fight against the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Bamlanivimab is a SARS-CoV-2 monoclonal antibody that is administered as an intravenous infusion to ambulatory patients with mild or moderate COVID-19, but a concern that arose was deciding the optimal location for patients to receive the medication. This report describes the development and implementation of a bamlanivimab infusion center in the emergency department of three hospitals in Orange County, California, shortly after bamlanivimab received emergency use authorization. As a result, a total of 601 …

Direct Nose To The Brain Nanomedicine Delivery Presents A Formidable Challenge, Robert A. Yokel

Pharmaceutical Sciences Faculty Publications

This advanced review describes the anatomical and physiological barriers and mechanisms impacting nanomedicine translocation from the nasal cavity directly to the brain. There are significant physiological and anatomical differences in the nasal cavity, olfactory area, and airflow reaching the olfactory epithelium between humans and experimentally studied species that should be considered when extrapolating experimental results to humans. Mucus, transporters, and tight junction proteins present barriers to material translocation across the olfactory epithelium. Uptake of nanoparticles through the olfactory mucosa and translocation to the brain can be intracellular via cranial nerves (intraneuronal) or other cells of the olfactory epithelium, or extracellular …

Novel Biomarkers Of Ciliary Extracellular Vesicles Interact With Ciliopathy And Alzheimer’S Associated Proteins, Ashraf M. Mohieldin, Amal Alachkar, John R. Yates Iii, Surya M. Nauli

Pharmacy Faculty Articles and Research

Ciliary extracellular vesicles (ciEVs), released from primary cilia, contain functional proteins that play an important role in cilia structure and functions. We have recently shown that ciEVs and cytosolic extracellular vesicles (cyEVs) have unique and distinct biomarkers. While ciEV biomarkers have shown some interactions with known ciliary proteins, little is known about the interaction of ciEV proteins with proteins involved in ciliopathy and neurodegenerative disorders. Here, we reveal for the first time the protein-protein interaction (PPI) between the top five ciEVs biomarkers with ciliopathy and Alzheimer disease (AD) proteins. These results support the growing evidence of the critical physiological roles …

Clinical Utility And Cost Effectiveness Of Long-Acting Lipoglycopeptides Used In Deep-Seated Infections Among Patients With Social And Economic Barriers To Care, Kayla Antosz, Majdi N. Al-Hasan, Z. Kevin Lu, Benjamin Tabor, Julie Ann Justo, Alexander Milgrom, Joseph Kohn, P. Brandon Bookstaver

Faculty Publications

The use of long-acting lipoglycopeptides (LaLGPs) in serious, deep-seated infections is of increasing interest. The purpose of this study is to evaluate the economic and clinical utility of LaLGPs in patients requiring protracted antibiotic courses who are not ideal candidates for oral transition or outpatient parenteral antibiotic therapy (OPAT). This is a retrospective, observational, matched cohort study of adult patients who received a LaLGP. Patients were matched 1:1 to those who received standard of care (SOC). Cost effectiveness was evaluated as total healthcare-related costs between groups. Clinical failure was a composite endpoint of mortality, recurrence, or need for extended antibiotics …

Evaluating The 0–10 Point Pain Scale On Adolescent Opioid Use In Us Emergency Departments, Michael T. Phan, Daniel M. Tomaszewski, Cody Arbuckle, Sun Yang, Brooke Jenkins, Michelle A. Fortier, Theodore Heyming, Erik Linstead, Candice Donaldson, Zeev N. Kain

Pharmacy Faculty Articles and Research

Objective: To evaluate trends in national emergency department (ED) adolescent opioid use in relation to reported pain scores. Methods: A retrospective, cross-sectional analysis on National Hospital Ambulatory Medical Care Survey (NHAMCS) data was conducted on ED visits involving patients aged 11–21 from 2008–2017. Crude observational counts were extrapolated to weighted estimates matching total population counts. Multivariate models were used to evaluate the role of a pain score in the reported use of opioids. Anchors for pain scores were 0 (no pain) and 10 (worst pain imaginable). Results: 31,355 observations were captured, which were extrapolated by the NHAMCS to represent 162,515,943 …

Recombinant Human Proteoglycan 4 Regulates Phagocytic Activation Of Monocytes And Reduces Il-1Β Secretion By Urate Crystal Stimulated Gout Pbmcs, Sandy Elsayed, Gregory D. Jay, Ralph Cabezas, Marwa Qadri, Tannin A. Schmidt, Khaled A. Elsaid

Pharmacy Faculty Articles and Research

Objectives

To compare phagocytic activities of monocytes in peripheral blood mononuclear cells (PBMCs) from acute gout patients and normal subjects, examine monosodium urate monohydrate (MSU) crystal-induced IL-1β secretion ± recombinant human proteoglycan 4 (rhPRG4) or interleukin-1 receptor antagonist (IL-1RA), and study the anti-inflammatory mechanism of rhPRG4 in MSU stimulated monocytes.

Methods

Acute gout PBMCs were collected from patients in the Emergency Department and normal PBMCs were obtained from a commercial source. Monocytes in PBMCs were identified by flow cytometry. PBMCs were primed with Pam3CSK4 (1μg/mL) for 24h and phagocytic activation of monocytes was determined using fluorescently labeled latex beads. MSU …

Symmetrical Drug-Related Intertriginous And Flexural Exanthema Induced By Cellulitis Prophylaxis, Tiffany Truong, Jonathan H. Ryder, Erica Lee, Clayton Mowrer, Ashley Wysong, Jasmine R. Marcelin

Graduate Medical Education Research Journal

Penicillin VK and hydroxyzine are typically well-tolerated antipruritic agents that are indicated in the prophylaxis of cellulitis. We herein report a case of a unique rash occurring during penicillin VK and hydroxyzine treatment in combination with the ingestion of cashews.

A 77-year-old male presented with new onset rash. Eleven days after the administration of penicillin VK and hydroxyzine for cellulitis prophylaxis, he developed a symmetric, erythematous, scaling rash on his buttocks and perineal region with associated pruritus and bleeding without fevers, chills, adenopathy, night sweats, or any other symptoms. He was diagnosed with symmetrical drug-related intertriginous and flexural exanthema (SDRIFE) …

Mansouramycins E–G, Cytotoxic Isoquinolinequinones From Marine Streptomycetes, Mohamed Shaaban, Khaled A. Shaaban, Gerhard Kelter, Heinz Herbert Fiebig, Hartmut Laatsch

Center for Pharmaceutical Research and Innovation Faculty Publications

Chemical investigation of the ethyl acetate extract from the marine-derived Streptomyces sp. isolate B1848 resulted in three new isoquinolinequinone derivatives, the mansouramycins E–G (1a–3a), in addition to the previously reported mansouramycins A (5) and D (6). Their structures were elucidated by computer-assisted interpretation of 1D and 2D NMR spectra, high-resolution mass spectrometry, and by comparison with related compounds. Cytotoxicity profiling of the mansouramycins in a panel of up to 36 tumor cell lines indicated a significant cytotoxicity and good tumor selectivity for mansouramycin F (2a), while the activity profile of E ( …

Design And Synthesis Of Fused Pyrimidines As Single Agents With Combination Chemotherapy Potential, As Tubulin Polymerization And One-Carbon Metabolism Inhibitors For Cancer, Tasdique Quadery

Electronic Theses and Dissertations

This dissertation describes the design, synthesis, and biological evaluation of bicyclic fused pyrimidines as single agents with combination chemotherapy potential with both antiangiogenic and cytotoxic effects. The dissertation also discusses one-carbon metabolism inhibitors and tumor targeting proteolysis targeting chimeras (PROTACs).

In cancer chemotherapy, the two major limitations are the dose-limiting toxicities of clinically used agents and the development of resistance to the treatment. Combination chemotherapy with antiangiogenic agents and microtubule targeting agents has shown an advantage against both these drawbacks. Single agents with both antiangiogenic activity and cytotoxicity would afford a therapy that circumvents pharmacokinetic problems of multiple agents, avoid …

Ketamine As A Treatment Modality For Treatment-Resistant Depression, Tracy Wulff, Shen Cao

Physician Assistant Capstones, 2020-current

Many recent studies have demonstrated the ability of ketamine, an NMDA receptor antagonist, to produce antidepressant effects that may be effective in helping reduce treatment-resistant major depression. In particular, three double-blinded randomized control trials have been conducted to assess the viability and effectiveness of this medication for treatment. This systematic literature review will analyze these studies and determine if the overall research indicates that ketamine is useful in improving depression as measured by the Montgomery–Asberg Depression Rating Scale (MADRS)¹.

Objective: Assess the effectiveness of IV Ketamine in reducing treatment-resistant major depressive disorder as measured by the Montgomery–Asberg …

Delivery Of Sirna With Drugs Targeting Polyamine Metabolism As Combinational Cancer Treatment, Ao Yu

Theses & Dissertations

Cancer has been a major public health issue worldwide for years and is the second leading cause of death in the United States. Important barrier must be broken to extend the life expectancy in every country. The standard care for cancer causes severe side effects which affects patients’ physical health and quality of life. Polyamines are highly related with the cell proliferation and apoptosis. Dysregulated polyamine metabolism in cancer leads to increased polyamine concentration in neoplastic cells. Thus, polyamine metabolism for cancer therapy can be an intriguing target. However, the heterogeneity affecting key cancer pathways poses significant challenges for effective …

Development Of A Muc16-Targeted Near-Infrared Antibody Probe For Fluorescence-Guided Surgery Of Pancreatic Cancer, Madeline T. Olson

Theses & Dissertations

Pancreatic cancer (PDAC) is an extremely lethal disease with an overall survival rate of 10%. Surgery remains the only potentially curative treatment option, but resections are complicated by infiltrative disease, proximity of critical vasculature, peritumoral inflammation, and dense stroma. Surgeons are limited to tactile and visual cues to differentiate cancerous tissue from normal tissue. Furthermore, translating preoperative images to the intraoperative setting poses additional challenges for tumor detection, and can result in undetected and unresected lesions. Thus, PDAC has high rates of incomplete resections, and subsequently, disease recurrence. Fluorescence-guided surgery (FGS) has emerged as a method to improve intraoperative detection …

A New Criterion For Fluoroquinolone-Associated Disability Diagnosis: Functional Gastrointestinal Disorders, Deanna N. Cannizzaro, Lydia F. Naughton, Maya Z. Freeman, Linda Martin, Charles L. Bennett M.D., Ph.D., Cecilia Bove

Faculty Publications

Background and Objectives: Fluoroquinolones (FQs) are a broad-spectrum class of antibiotics routinely prescribed for common bacterial infections despite recent recommendations to use them only for life-threatening cases. In addition to their antimicrobial properties, FQs act in the central nervous system as GABAA receptor inhibitors, which could potentially affect functionality of the vagus nerve at the forefront of gastrointestinal (GI) tract function. Alterations in neural control of digestion have been shown to be linked to Functional Gastrointestinal Disorders (FGIDs), which are usually diagnosed based on self-reported symptoms. The aim of this study was to assess the incidence of FGIDs following FQ …

“Holistic Risk-Based Site Surveillance – A Data-Based Approach To Site Quality Risk Identification And Assessment In The Pharmaceutical Industry”, Matteo Bernasconi, Thomas Friedli, Nuala Calnan (Editor)

Level 3

Effective quality risk management is fundamental in guaranteeing the development and manufacture of high-quality drugs, reducing drug shortages, and avoiding harm to patients’ health. The ability to accurately assess the actual risk environment, predict potential product quality or supply disruption issues and act to eliminate, prevent, reduce or mitigate them is key to improvements in quality management maturity. This paper illustrates a just-launched research project aimed at developing a comprehensive framework for how to assess and predict risks by leveraging a range of diverse factors.

“Gaining Organisational Acceptance Of A Data Analytics Programme In Eli Lilly”, Anthony Maguire, Marcus O'Mahony

Level 3

This paper describes how Eli Lilly overcame barriers to enable new use of data. This was achieved by adopting a deep understanding of end-user needs and the support of site leaders and end-users to standardise process monitoring. A standard approach of ‘Contexting’, ‘Data-Extraction’, ‘Model build’, ‘On-line Config’, ‘Deploy’, was utilised, using a commercial off-the-shelf software. The paper describes proof of concept demonstrations undertaken and discusses the ingredients to make the journey a success.

Total Synthesis Of Decahydroquinoline Poison Frog Alkaloids Ent-Cis-195a And Cis-211a, Takuya Okada, Naizhen Wu, Katsuki Takashima, Jungoh Ishimura, Hiroyuki Morita, Takuya Ito, Takeshi Kodama, Yuhei Yamasaki, Shin-Ichi Akanuma, Yoshiyuki Kubo, Ken-Ichi Hosoya, Hiroshi Tsuneki, Tsutomu Wada, Toshiyasu Sasaoka, Takahiro Shimizu, Hideki Sakai, Linda P. Dwoskin, Syed R. Hussaini, Ralph A. Saporito, Naoki Toyooka

Pharmaceutical Sciences Faculty Publications

The total synthesis of two decahydroquinoline poison frog alkaloids ent-cis-195A and cis-211A were achieved in 16 steps (38% overall yield) and 19 steps (31% overall yield), respectively, starting from known compound 1. Both alkaloids were synthesized from the common key intermediate 11 in a divergent fashion, and the absolute stereochemistry of natural cis-211A was determined to be 2R, 4aR, 5R, 6S, and 8aS. Interestingly, the absolute configuration of the parent decahydroquinoline nuclei of cis-211A was the mirror image of that …