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2021

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Full-Text Articles in Pharmacy and Pharmaceutical Sciences

A Community Health Initiative: Health To The Power Of You, Stephanie Hendricks Oct 2021

A Community Health Initiative: Health To The Power Of You, Stephanie Hendricks

Purdue Journal of Service-Learning and International Engagement

In April 2020, the COVID-19 pandemic impacted the number of visits to ambulatory care practices and was reported to have declined by nearly 60%. The extent of this decline is alarming as outpatient visits help manage chronic diseases in patients, such as diabetes, high blood pressure, and high cholesterol. This trend sparked an interest in pharmacist and student pharmacist, Dr. Cynthia Koh-Knox Sharp and Stephanie Hendricks, respectively, as it offered an opportunity to help serve the Greater Lafayette community. We created Health to the Power of You (HealthYou), which targets two of Lafayette’s neglected populations: community members experiencing …


Cd44-Targeted, Indocyanine Green-Paclitaxel-Loaded Human Serum Albumin Nanoparticles For Potential Image-Guided Drug Delivery., Karthik Thangavel, Asha Lakshmikuttyamma, Chellappagounder Thangavel, Sunday A. Shoyele Oct 2021

Cd44-Targeted, Indocyanine Green-Paclitaxel-Loaded Human Serum Albumin Nanoparticles For Potential Image-Guided Drug Delivery., Karthik Thangavel, Asha Lakshmikuttyamma, Chellappagounder Thangavel, Sunday A. Shoyele

College of Pharmacy Faculty Papers

The use of multifunctional nanomedicines for image-guided drug delivery is currently being universally evaluated as a means of efficiently managing cancers and other diseases. In this study we evaluated the potential of an indocyanine green (ICG) and paclitaxel (PTX) loaded human serum albumin (HSA) nanoparticles that was conjugated with hyaluronic acid for use in image-guided drug delivery targeted to CD44-positive non-small cell lung cancer (NSCLC). Series of NSCLC cell lines were evaluated for the expression of CD44 using both western blot analysis and qRT-PCR and compared to a normal lung fibroblast cell line (MRC-5). Using Fluorescence microscopy and photoacoustic imaging …


Crime Scene Investigation: Simulated Post-Mortem Lc-Ms/Ms Analysis Of Cocaine And Cocaine Metabolites In Synthetic Human Serum, Matt J. Vergne Oct 2021

Crime Scene Investigation: Simulated Post-Mortem Lc-Ms/Ms Analysis Of Cocaine And Cocaine Metabolites In Synthetic Human Serum, Matt J. Vergne

Faculty Works

This laboratory experiment introduces upper-division undergraduate analytical chemistry students to liquid chromatography-tandem mass spectrometry (LC-MS/MS) in a forensic application: the analysis of cocaine and metabolites of cocaine in simulated serum ostensibly from drug overdose victims. For this investigation, students developed the analytical methods. First, the students determined the multiple reaction monitoring (MRM) transitions and optimized collision energy. The MS methods developed were then added to an LC method for LC-MS/MS quantitation with a 2.5 min run time. Students successfully quantified the drugs and metabolites, and they were able to identify which samples indicated cocaine use and overdose


Graduation Of Antidepressant Assortment By The Method Of Expert Evaluations On The Pharmaceutical Market Of The Republic Of Uzbekistan, Abror Rahimov Oct 2021

Graduation Of Antidepressant Assortment By The Method Of Expert Evaluations On The Pharmaceutical Market Of The Republic Of Uzbekistan, Abror Rahimov

Problems and Perspectives in Pharmaceutics and Drug Discovery

In the condition of the pharmaceutical market of Uzbekistan, for the first time, we carried an expert evaluation of the nomenclature of antidepressant drugs, considering the competence of experts and the representativeness of respondents of the studied group of drugs. Marketing research was carried out to study the opinions of psychiatrists from Tashkent city for two months: September – October 2020. As a tool for measuring the opinions of experts, an expert survey questionnaire was developed in advance with specified criteria. The study of antidepressants used in domestic conditions was carried out under the international non-proprietary name (INN). Also, based …


Cyclic Peptide-Gadolinium Nanocomplexes As Sirna Delivery Tools, Amir Nasrolahi Shirazi, Muhammad Imran Sajid, Dindyal Mandal, David Stickley, Stephanie Nagasawa, Joshua Long, Sandeep Lohan, Keykavous Parang, Rakesh Kumar Tiwari Oct 2021

Cyclic Peptide-Gadolinium Nanocomplexes As Sirna Delivery Tools, Amir Nasrolahi Shirazi, Muhammad Imran Sajid, Dindyal Mandal, David Stickley, Stephanie Nagasawa, Joshua Long, Sandeep Lohan, Keykavous Parang, Rakesh Kumar Tiwari

Pharmacy Faculty Articles and Research

We have recently reported that a cyclic peptide containing five tryptophan, five arginine, and one cysteine amino acids [(WR)5C], was able to produce peptide-capped gadolinium nanoparticles, [(WR)5C]-GdNPs, in the range of 240 to 260 nm upon mixing with an aqueous solution of GdCl3. Herein, we report [(WR)5C]-GdNPs as an efficient siRNA delivery system. The peptide-based gadolinium nanoparticles (50 µM) did not exhibit significant cytotoxicity (~93% cell viability at 50 µM) in human leukemia T lymphoblast cells (CCRF-CEM) and triple-negative breast cancer cells (MDA-MB-231) after 48 h. Fluorescence-activated cell sorting (FACS) analysis indicated …


Impact Of Covid 19 On Library Services In Us Pharmacy Programs, Sherrill Brown, Julie Kalabalik Hoganson, Ivan Portillo Oct 2021

Impact Of Covid 19 On Library Services In Us Pharmacy Programs, Sherrill Brown, Julie Kalabalik Hoganson, Ivan Portillo

Library Presentations, Posters, and Audiovisual Materials

"The COVID 19 pandemic resulted in many academic libraries closing physical spaces and the reduction of personnel due to quarantine measures. The potential reduction in library services could have a negative impact on research by pharmacy faculty"


Glycoscience Center Of Research Excellence (Glycore), Karin King Ballering Oct 2021

Glycoscience Center Of Research Excellence (Glycore), Karin King Ballering

Annual Poster Session 2021

Presenter: Karin King Ballering


Coupling Fdm 3d Printing With Hot-Melt Extrusion To Produce Hypertensive Dual Therapy Fixed Dose Combination Tablet, Abdullah Alzahrani, Sagar Narala, Dinesh Nyavanandi, Mashan Almutairi, Ahmed Almotairy, Suresh Bandari, Michael Repka Oct 2021

Coupling Fdm 3d Printing With Hot-Melt Extrusion To Produce Hypertensive Dual Therapy Fixed Dose Combination Tablet, Abdullah Alzahrani, Sagar Narala, Dinesh Nyavanandi, Mashan Almutairi, Ahmed Almotairy, Suresh Bandari, Michael Repka

Annual Poster Session 2021

Presenter: Abdullah Alzahrani


Schottiin, A New Prenylated Isoflavone From Psorothamnus Schottii And Antibacterial Synergism Studies Between Methicillin And Fremontone Against Mrsa, Mallika Kumarihamy, Siddharth K. Tripathi, Shabana Khan, Ilias Muhammad Oct 2021

Schottiin, A New Prenylated Isoflavone From Psorothamnus Schottii And Antibacterial Synergism Studies Between Methicillin And Fremontone Against Mrsa, Mallika Kumarihamy, Siddharth K. Tripathi, Shabana Khan, Ilias Muhammad

Annual Poster Session 2021

Presenter: Mallika Kumarihamy


New Hydroxy-1,4-Naphthoquinone And Phenoxy-Phenyl-Naphthoquinone Compounds As Drug-Resistant Antimalarials, Seong Jong Kim, Md Imdadul H. Khan, Yuexin Li, Benjamin Sawyer, Michael K. Riscoe, Shabana I. Khan, Babu L. Tekwani, Hoang V. Le Oct 2021

New Hydroxy-1,4-Naphthoquinone And Phenoxy-Phenyl-Naphthoquinone Compounds As Drug-Resistant Antimalarials, Seong Jong Kim, Md Imdadul H. Khan, Yuexin Li, Benjamin Sawyer, Michael K. Riscoe, Shabana I. Khan, Babu L. Tekwani, Hoang V. Le

Annual Poster Session 2021

Presenter: Benjamin Sawyer


Negative Impacts Of Flood-Associated Water Quality Stressors On Early Oyster Life Stages, Jessica Pruett, Ann Fairly Pandelides, Kristine Willett, Stephanie Showalter Otts, Deborah Gochfeld Oct 2021

Negative Impacts Of Flood-Associated Water Quality Stressors On Early Oyster Life Stages, Jessica Pruett, Ann Fairly Pandelides, Kristine Willett, Stephanie Showalter Otts, Deborah Gochfeld

Annual Poster Session 2021

Presenter: Jessica Pruett


Discovery Of 5Α-Pregnan-2Β,3Α-Diol-20-One As A Neurohiv Protective Agent, Md Imdadul H. Khan, Mohammed F. Salahuddin, Nicholas S. Akins, Fakhri Mahdi, Seong Jong Kim, Jing Li, Jason J. Paris, Hoang V. Le Oct 2021

Discovery Of 5Α-Pregnan-2Β,3Α-Diol-20-One As A Neurohiv Protective Agent, Md Imdadul H. Khan, Mohammed F. Salahuddin, Nicholas S. Akins, Fakhri Mahdi, Seong Jong Kim, Jing Li, Jason J. Paris, Hoang V. Le

Annual Poster Session 2021

Presenter: Md Imdadul Khan


Liquid Chromatography- Tandem Mass Spectrometry (Lc-Ms-Ms) As A Detection Method For Cocaine As A Perfomance Enhancing Drug, Isha Kalaria, Shrishti Dubey Oct 2021

Liquid Chromatography- Tandem Mass Spectrometry (Lc-Ms-Ms) As A Detection Method For Cocaine As A Perfomance Enhancing Drug, Isha Kalaria, Shrishti Dubey

Annual Poster Session 2021

Presenters: Isha Kalaria, Shrishti Dubey


Scanning Electron Microscopy Core, Vijayasankar Raman, Soumyajit Majumdar Oct 2021

Scanning Electron Microscopy Core, Vijayasankar Raman, Soumyajit Majumdar

Annual Poster Session 2021

Presenter: Vijayasankar Raman


Biomolecular Sciences, University Of Mississippi. Department Of Biomolecular Sciences Oct 2021

Biomolecular Sciences, University Of Mississippi. Department Of Biomolecular Sciences

Annual Poster Session 2021

Presenter: Department of BioMolecular Sciences


Hiv-1 Tat Protein Promotes Neuroendocrine Dysfunction Concurrent With The Potentiation Of Oxycodone’S Psychomotor Behavioral Effects In Female Transgenic Mice, Salahuddin Mohammed, Fakhri Mahdi, Jason J. Paris Oct 2021

Hiv-1 Tat Protein Promotes Neuroendocrine Dysfunction Concurrent With The Potentiation Of Oxycodone’S Psychomotor Behavioral Effects In Female Transgenic Mice, Salahuddin Mohammed, Fakhri Mahdi, Jason J. Paris

Annual Poster Session 2021

Presenter: Salahuddin Mohammed


Environmental Enrichment Provided To Adult Zebra Finches (Taeniopygia Guttata) Differentially Influences Sexes On A Spatial Learning Task, Arma'rosa Wilks-Mohead, Laura West, Lainy B. Day Oct 2021

Environmental Enrichment Provided To Adult Zebra Finches (Taeniopygia Guttata) Differentially Influences Sexes On A Spatial Learning Task, Arma'rosa Wilks-Mohead, Laura West, Lainy B. Day

Annual Poster Session 2021

Presenter: Arma'Rosa Wilks-Mohead


Age-Related Neuroendocrine, Cognitive, And Behavioral Co-Morbidities Are Promoted By Hiv-1 Tat Expression In Male Mice, Alaa Qraeya, Fakhri Mahdi, Marc Kaufman, Nicole M. Ashpole, Jason J. Paris Oct 2021

Age-Related Neuroendocrine, Cognitive, And Behavioral Co-Morbidities Are Promoted By Hiv-1 Tat Expression In Male Mice, Alaa Qraeya, Fakhri Mahdi, Marc Kaufman, Nicole M. Ashpole, Jason J. Paris

Annual Poster Session 2021

Presenter: Alaa Qraeya


Regulation Of Brain Primary Cilia Length By Mch Signaling: Evidence From Pharmacological, Genetic, Optogenetic, And Chemogenic Manipulations, Wedad Alhassen, Yuki Kobayashi, Jessica Su, Brianna Robbins, Henry Nguyen, Thant Myint, Micah Yu, Surya M. Nauli, Yumiko Saito, Amal Alachkar Oct 2021

Regulation Of Brain Primary Cilia Length By Mch Signaling: Evidence From Pharmacological, Genetic, Optogenetic, And Chemogenic Manipulations, Wedad Alhassen, Yuki Kobayashi, Jessica Su, Brianna Robbins, Henry Nguyen, Thant Myint, Micah Yu, Surya M. Nauli, Yumiko Saito, Amal Alachkar

Pharmacy Faculty Articles and Research

The melanin-concentrating hormone (MCH) system is involved in numerous functions, including energy homeostasis, food intake, sleep, stress, mood, aggression, reward, maternal behavior, social behavior, and cognition. In rodents, MCH acts on MCHR1, a G protein-coupled receptor, which is widely expressed in the brain and abundantly localized to neuronal primary cilia. Cilia act as cells’ antennas and play crucial roles in cell signaling to detect and transduce external stimuli to regulate cell differentiation and migration. Cilia are highly dynamic in terms of their length and morphology; however, it is not known if cilia length is causally regulated by MCH system activation …


Conference Proceedings: Select Abstracts Presented At 2021 Advocate Aurora Health Scientific Day Oct 2021

Conference Proceedings: Select Abstracts Presented At 2021 Advocate Aurora Health Scientific Day

Journal of Patient-Centered Research and Reviews

Abstracts published within this supplement were presented at the 47th annual Advocate Aurora Health Scientific Day, held virtually on May 26, 2021. This research symposium provides a forum for disseminating results from studies conducted by faculty, fellows, residents, and other allied health professionals associated with Midwest-based health system Advocate Aurora Health, which publishes the Journal of Patient-Centered Research and Reviews.


Cyclic Dipeptides: The Biological And Structural Landscape With Special Focus On The Anti-Cancer Proline-Based Scaffold, Joanna Bojarska, Adam Mieczkowski, Zyta M. Ziora, Mariusz Skwarczynski, Istvan Toth, Ahmed O. Shalash, Keykavous Parang, Shaima Ahmed El-Mowafi, Eman H. M. Mohammed, Sherif Elnagdy, Maha Alkhazindar, Wojciech M. Wolf Oct 2021

Cyclic Dipeptides: The Biological And Structural Landscape With Special Focus On The Anti-Cancer Proline-Based Scaffold, Joanna Bojarska, Adam Mieczkowski, Zyta M. Ziora, Mariusz Skwarczynski, Istvan Toth, Ahmed O. Shalash, Keykavous Parang, Shaima Ahmed El-Mowafi, Eman H. M. Mohammed, Sherif Elnagdy, Maha Alkhazindar, Wojciech M. Wolf

Pharmacy Faculty Articles and Research

Cyclic dipeptides, also know as diketopiperazines (DKP), the simplest cyclic forms of peptides widespread in nature, are unsurpassed in their structural and bio-functional diversity. DKPs, especially those containing proline, due to their unique features such as, inter alia, extra-rigid conformation, high resistance to enzyme degradation, increased cell permeability, and expandable ability to bind a diverse of targets with better affinity, have emerged in the last years as biologically pre-validated platforms for the drug discovery. Recent advances have revealed their enormous potential in the development of next-generation theranostics, smart delivery systems, and biomaterials. Here, we present an updated review on the …


Obsolete Or Essential? Gastrointestinal Decontamination In Severe Bupropion Ingestions: A Case Series, Alexandra Amaducci Do, Andrew F. Miller Do, Derek J. Fikse Do, Gillian A. Beauchamp Md Oct 2021

Obsolete Or Essential? Gastrointestinal Decontamination In Severe Bupropion Ingestions: A Case Series, Alexandra Amaducci Do, Andrew F. Miller Do, Derek J. Fikse Do, Gillian A. Beauchamp Md

Department of Emergency Medicine

No abstract provided.


Oral Budesonide Is An Effective Alternative To Prednisone For Treatment Of Autoimmune Hepatitis, Natanie J. Anilovich Oct 2021

Oral Budesonide Is An Effective Alternative To Prednisone For Treatment Of Autoimmune Hepatitis, Natanie J. Anilovich

Clinical Research in Practice: The Journal of Team Hippocrates

A clinical decision report using:

Manns MP, Woynarowski M, Kreisel W, et al. Budesonide induces remission more effectively than prednisone in a controlled trial of patients with autoimmune hepatitis. Gastroenterology. 2010;139(4):1198-1206. https://doi.org/10.1053/j.gastro.2010.06.046

for a patient with autoimmune hepatitis developing septic arthritis secondary to prednisone therapy.


Long-Term Survival Of Older Patients Hospitalized For Covid-19. Do Clinical Characteristics Upon Admission Matter?, Michał Chojnicki, Agnieszka Neumann-Podczaska, Mikołaj Seostianin, Zofia Tomczak, Hamza Tariq, Jerzy Chudek, Sławomir Tobis, Iwona Mozer-Lisewska, Aleksandra Suwalska, Andrzej Tykarski, Piotr Merks, Sylwia Kropińska, Małgorzata Sobieszczańska, Frank Romanelli, Katarzyna Wieczorowska-Tobis Oct 2021

Long-Term Survival Of Older Patients Hospitalized For Covid-19. Do Clinical Characteristics Upon Admission Matter?, Michał Chojnicki, Agnieszka Neumann-Podczaska, Mikołaj Seostianin, Zofia Tomczak, Hamza Tariq, Jerzy Chudek, Sławomir Tobis, Iwona Mozer-Lisewska, Aleksandra Suwalska, Andrzej Tykarski, Piotr Merks, Sylwia Kropińska, Małgorzata Sobieszczańska, Frank Romanelli, Katarzyna Wieczorowska-Tobis

Pharmacy Practice and Science Faculty Publications

Older adults are particularly susceptible to COVID-19 in terms of both disease severity and risk of death. To compare clinical differences between older COVID-19 hospitalized survivors and non-survivors, we investigated variables influencing mortality in all older adults with COVID-19 hospitalized in Poznań, Poland, through the end of June 2020 (n = 322). In-hospital, post-discharge, and overall 180-day mortality were analyzed. Functional capacity prior to COVID-19 diagnosis was also documented. The mean age of subjects was 77.5 ± 10.0 years; among them, 191 were females. Ninety-five (29.5%) died during their hospitalization and an additional 30 (9.3%) during the post-discharge period …


Collagen-Based Biomaterials With Possible Therapeutic Effects, Ramona Mihaela Nedelcuţă, Gigi Călin, Mihai Cristian Nedelcuţă, Vlad Dumitru Baleanu, Dragos Virgil Davitoiu, Bogdan Socea, Bogdan-Petre Stănoiu Oct 2021

Collagen-Based Biomaterials With Possible Therapeutic Effects, Ramona Mihaela Nedelcuţă, Gigi Călin, Mihai Cristian Nedelcuţă, Vlad Dumitru Baleanu, Dragos Virgil Davitoiu, Bogdan Socea, Bogdan-Petre Stănoiu

Journal of Mind and Medical Sciences

Epidermolysis bullosa (EB) is a rare, serious genetic disease, incurable through the current means. Apart from this initial definition, there was later some ease in the definition of the disease, including the manifestations of toxic epidermal necrolysis and Stevens Johnson syndrome in this entity. In medical practice, there are cases that do not overlap with the description in the literature, thus the treatment must be adapted and personalized to the particularities. We present the case of a female new-born, with "de novo" mutation for the early-onset antenatal epidermolysis and our personalized therapeutic management, based on collagen from bovine corneas by …


Tracking Development Assistance For Health And For Covid-19: A Review Of Development Assistance, Government, Out-Of-Pocket, And Other Private Spending On Health For 204 Countries And Territories, 1990–2050, Angela E. Micah, Ian E. Cogswell, Brandon Cunningham, Satoshi Ezoe, Anton C. Harle, Ismaeel Yunusa Ph. D. Oct 2021

Tracking Development Assistance For Health And For Covid-19: A Review Of Development Assistance, Government, Out-Of-Pocket, And Other Private Spending On Health For 204 Countries And Territories, 1990–2050, Angela E. Micah, Ian E. Cogswell, Brandon Cunningham, Satoshi Ezoe, Anton C. Harle, Ismaeel Yunusa Ph. D.

Faculty Publications

Background

The rapid spread of COVID-19 renewed the focus on how health systems across the globe are financed, especially during public health emergencies. Development assistance is an important source of health financing in many low-income countries, yet little is known about how much of this funding was disbursed for COVID-19. We aimed to put development assistance for health for COVID-19 in the context of broader trends in global health financing, and to estimate total health spending from 1995 to 2050 and development assistance for COVID-19 in 2020.

Methods

We estimated domestic health spending and development assistance for health to generate …


Assessment Of Antimicrobial Pharmacokinetics Curricula Across Schools And Colleges Of Pharmacy In The United States, Gary Fong, Elias B. Chahine, Julie Ann Justo, Navaneeth Narayanan, Emily L. Heil, Kayla R. Stover, Jonathan C. Cho, Zachary N. Jenkins, Conan Macdougall Oct 2021

Assessment Of Antimicrobial Pharmacokinetics Curricula Across Schools And Colleges Of Pharmacy In The United States, Gary Fong, Elias B. Chahine, Julie Ann Justo, Navaneeth Narayanan, Emily L. Heil, Kayla R. Stover, Jonathan C. Cho, Zachary N. Jenkins, Conan Macdougall

Pharmacy Faculty Articles and Research

Introduction

Advances in technology and understanding of pharmacokinetic/pharmacodynamic relationships have prompted guideline updates and advances in precision dosing, but the role of clinical pharmacokinetics (PK) in pharmacy education remains inconsistent. Previous surveys of pharmacy school PK curricula revealed large variations in content, integration, and teaching tools but did not focus on antimicrobials or details of andragogy used.

Objective

Identify how antimicrobial PK is taught in pharmacy curricula across the United States, as well as instructor perceptions of current practices.

Methods

An online survey was distributed to 118 pharmacy programs across the United States in 2018. This 30-minute questionnaire covered curriculum …


Fatal Police Violence By Race And State In The Usa, 1980–2019: A Network Meta-Regression, Fablina Sharara, Eve E. Wool, Gregory J. Bertolacci, Nicole Davis Weaver, Shelley Balassyano, Ismaeel Yunusa Ph. D., Et Al. Oct 2021

Fatal Police Violence By Race And State In The Usa, 1980–2019: A Network Meta-Regression, Fablina Sharara, Eve E. Wool, Gregory J. Bertolacci, Nicole Davis Weaver, Shelley Balassyano, Ismaeel Yunusa Ph. D., Et Al.

Faculty Publications

Background

The burden of fatal police violence is an urgent public health crisis in the USA. Mounting evidence shows that deaths at the hands of the police disproportionately impact people of certain races and ethnicities, pointing to systemic racism in policing. Recent high-profile killings by police in the USA have prompted calls for more extensive and public data reporting on police violence. This study examines the presence and extent of under-reporting of police violence in US Government-run vital registration data, offers a method for correcting under-reporting in these datasets, and presents revised estimates of deaths due to police violence in …


Incident Light And Morphology Determine Coral Productivity Along A Shallow To Mesophotic Depth Gradient, Michael P. Lesser, Marc Slattery, Curtis D. Mobley Oct 2021

Incident Light And Morphology Determine Coral Productivity Along A Shallow To Mesophotic Depth Gradient, Michael P. Lesser, Marc Slattery, Curtis D. Mobley

Faculty and Student Publications

While the effects of irradiance on coral productivity are well known, corals along a shallow to mesophotic depth gradient (10–100 m) experience incident irradiances determined by the optical properties of the water column, coral morphology, and reef topography. Modeling of productivity (i.e., carbon fixation) using empirical data shows that hemispherical colonies photosynthetically fix significantly greater amounts of carbon across all depths, and throughout the day, compared with plating and branching morphologies. In addition, topography (i.e., substrate angle) further influences the rate of productivity of corals but does not change the hierarchy of coral morphologies relative to productivity. The differences in …


Computationally Assisted Lead Optimization Of Novel Potent And Selective Mao-B Inhibitors, Vedanjali Gogineni, Manal A. Nael, Narayan D. Chaurasiya, Khaled M. Elokely Oct 2021

Computationally Assisted Lead Optimization Of Novel Potent And Selective Mao-B Inhibitors, Vedanjali Gogineni, Manal A. Nael, Narayan D. Chaurasiya, Khaled M. Elokely

Faculty and Student Publications

A series of dietary flavonoid acacetin 7-O-methyl ether derivatives were computationally designed aiming to improve the selectivity and potency profiles against monoamine oxidase (MAO) B. The designed compounds were evaluated for their potential to inhibit human MAO-A and-B. Compounds 1c, 2c, 3c, and 4c were the most potent with a Ki of 37 to 68 nM against MAO-B. Compounds 1c–4c displayed more than a thousand-fold selectivity index towards MAO-B compared with MAO-A. Moreover, compounds 1c and 2c showed reversible inhibition of MAO-B. These results provide a basis for further studies on the potential application of these modified flavonoids for the …