138 research outputs found

    Design and synthesis of novel thiophenecarbohydrazide, thienopyrazole and thienopyrimidine derivatives as antioxidant and antitumor agents

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    Etilni ester 2-amino-5-acetil-4-metil-tiofen-3-karboksilne kiseline (1) i 5-acetil-2-amino-4-metiltiofen-3-karbohidrazid (2) sintetizirani su i upotrebljeni kao reaktanti u sintezi novih spojeva 1-(5-amino-4-(3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3a), 1-(5-amino-4-(4-klor-3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3b), 1-(4-metil-2-amino-5-acetiltiofen-3-karbonil) pirazolidin-3,5-diona (4), (Z)-N'-(4-metil-2-amino-5-acetiltiofen-3-karbonil) formohidrazonske kiseline (5a), (Z)-etil-N'-(4-metil-2-amino-5-acetiltiofen-3-karbonilformo hidrazonata (5b), 6-acetil-3-amino-2,5-dimetiltieno2,3-dpirimidin-4(3H)-one (8), 5-metil-3-amino-2-merkapto-6-acetiltieno2,3-dpirimidin-4(3H)-ona (10) i 5-metil-6-acetil-2-tiokso-2,3-dihidrotieno2,3-dpirimidin-4(1H)-ona (12) kao potencijalnih antioksidansa i citostatika. Farmakološka ispitivanja ukazuju na to da spojevi 6a, 6b, 8, 10 i 12 imaju značajno antitumorsko i antioksidativno djelovanje.2-Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene-3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5-amino-4-(3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3a), 1-(5-amino-4-(4-chloro-3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3b), 1-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) pyrazolidine-3,5-dione (4), (Z)-N'-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) formohydrazonic acid (5a), (Z)-ethyl-N'-(4-methyl-2-amino-5-acetylthiophene-3-carbonylformo hydrazonate (5b), 6-acetyl-3-amino-2,5-dimethylthieno2,3-dpyrimidin-4(3H)-one (8), 5-methyl-3-amino-2-mercapto-6-acetylthieno2,3-dpyrimidin-4(3H)-one (10) and 5-methyl-6-acetyl-2-thioxo-2,3-dihydrothieno2,3-dpyrimidin-4(1H)-one (12) as potential antioxidant and antitumor agents. Pharmacological results showed that compounds 6a, 6b, 8, 10 and 12 exhibited promising antitumor and antioxidant activity

    Pharmacotherapy

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    The intent of this book is to provide an overview of current conceptualizations of Pharmacotherapy. The book focuses on three major areas; diagnosis, treatment, and prevention for a wide array of diseases; Cognitive and Psychological disorders (Schizophrenia and Nicotine addiction), Inflammatory disorders (New Chemical anti-inflammatory and Immunotherapy), updated antihypertensive therapy and healing of ulcers with venous origin. A separate chapter is dedicated to the rationality of drug use in earthquake injuries. The last chapter deals with Imaging of potential therapeutic or diagnostic agents in animal models in the early stage of research. We hope this book is useful to a wide range of people, from students first learning about Pharmacotherapy, to advanced clinicians and researchers

    Resveratrol

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    This book intends to strike a balance between developments in research and the fact that researchers must absorb and link to scientific advances with clinical practice so that the management of diseases can be based on sound physiological concepts. This book addresses several controversial issues regarding a natural molecule with fascinating pharmacological and therapeutic effects. The book contains three sections: Section 1: Pharmacology and Therapeutic Applications of Resveratrol; Section 2: Bioavailability, Metabolism, and Mode of Action of Resveratrol; Section 3: Resveratrol and Its Role in Chronic and Degenerative Diseases. Does it Add Life to Years or Years to Life? It is our hope that this book will motivate readers to approach the evidence on the use resveratrol and thereby spark an interest in making further contributions to the current scientific debate and treatment development efforts

    Antiviral Drugs

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    With the increasing emergence of viral infections worldwide, researchers are working to develop new and non-conventional treatments for infectious diseases. This is particularly true for SARS-CoV-2, which initiated a pandemic in 2019. With a focus on coronavirus, this book provides an overview of antiviral agents and new approaches to drug design. It includes five chapters that address new avenues for drug discovery, reprofiling of current drugs, computer-aided drug design, and more

    Drug Repurposing

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    Drug repurposing or drug repositioning is a new approach to presenting new indications for common commercial and clinically approved existing drugs. For example, chloroquine, an old antimalarial drug, showed promising results for treating COVID-19, interfering with MDR in several types of cancer, and chemosensitizing human leukemic cells.This book focuses on the hypothesis, risk/benefits, and economic impacts of drug repurposing on drug discovery in dermatology, infectious diseases, neurological disorders, cancer, and orphan diseases. It brings together up-to-date research to provide readers with an informative, illustrative, and easy-to-read book useful for students, clinicians, and the pharmaceutical industry

    Pharmacovigilance

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    Pharmacovigilance or drug safety may be defined as a science that relates to the "collection, detection, assessment, monitoring, and prevention" of side/adverse effects of drugs. It is also essential to monitor for adverse effects even after a drug or therapy has been on the market for some time, as new ones may emerge. This book addresses several fundamental issues in three major sections well-presented in easy-to-understand formats. The authors of this book contributed the latest research, and each chapter has been reviewed and updated to enhance the book's educational value, clarity, and readability

    Phenolic Compounds

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    Phenolics are commonly available compounds in foods, beverages, and spices. They have great importance in all aspects of daily life including industry, health, and research. As such, this book presents a comprehensive overview of phenolic compounds and their potential applications in industry, environment, and public health. Chapters cover such topics as the production of these compounds and their uses in environmental sustainability, climate change, green industry, and treatment of human disease

    Metformin

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    Currently, there are many complicated health disorders with different etiologies and pathogeneses, including cancers, obesity, periodontitis, cardiovascular disease, liver, skin and renal disorders. It is now known that the causes and pathogenesis of many complex chronic diseases are usually polyfactorial: genetic, environmental, constitutive factors, or a combination of these. Recently, poly-target molecules containing enzymes capable of catalyzing several reactions have been efficiently used in the treatment of several metabolic disorders, and infectious and inflammatory diseases. This book describes the history of the discovery of metformin and its chemistry. Topics presented include new approaches to the role of metformin in the treatment of diabetic patients and its ability to target multiple signaling pathways

    Evidence-based Strategies in Herbal Medicine, Psychiatric Disorders and Emergency Medicine

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    This book intends to strike a balance between developments in pharmacotherapy research and the facts that researchers must absorb, as well as link scientific advances with clinical practice so that the management of diseases can be based on sound physiological concepts. Each chapter has been reviewed and new authors have brought up-to-date research to make the book more informative, illustrative, and easy to read. The book focuses on three major areas: Experimental, preclinical, and clinical applications of herbal medicine; Evidence-based strategies in emergency medicine and New approach in management of psychiatric disorders. The first three chapters describe new and modern applications of common herbs for treatment of several inflammatory and skin disorders, e.g. ulcerative colitis, bronchial asthma, osteoarthritis, multiple sclerosis, and melasma. Chapter four deals with the most severe hypertensive states that pose an immediate threat to life, and how to manage these situations. The fifth chapter is dedicated to tackling polypharmacy psychiatric disorders. We hope this book is useful to a wide range of readers, from students first learning about pharmacotherapy, through advanced clinicians and researchers who are looking for a review of current treatments and conceptualizations of the condition. It is our hope that this book may motivate readers to approach the evidence on pharmacotherapy with an open mind, and thereby spark an interest in initiating further contributions to the current scientific debate and treatment development efforts

    Natural Products and Cancer Drug Discovery

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    This book, Natural Products and Cancer Drug Discovery, is written by leading experts in natural products in cancer therapy. The first two sections describe new applications of common herbs and foods for treatment of cancer. Section 3 deals with the development of new chemotherapeutics from Cannabis and endophytic fungi. Section 4 presented formulations of natural products for treatment of malignant melanoma. Made-to-order anticancer therapy from natural products using computational and tissue engineering approaches is addressed in the fifth section. It is our hope that this book may motivate readers to approach the evidence of anticancer natural products with an open mind and thereby spark an interest in making further contributions to the cancer treatment efforts
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