Most Accessed Articles | Design, Synthesis and Characterization of Novel Urolithin Derivatives as Cholinesterase Inhibitor Agents

Author(s): Maryam Norouzbahari, Emine V. Burgaz, Tugba Ercetin, Amirhossein Fallah, Alireza Foroumadi, Loghman Firoozpour, Mustafa F. Sahin, Mustafa Gazi, Hayrettin O. Gulcan*.

Journal Name: Letters in Drug Design & Discovery

Considering the limitations of current cholinesterase inhibitor drugs for the treatment of Alzheimer’s disease, there is ongoing research activities to find out alternative drug candidates. The aryl-spacer-N-benzyl pharmacophore model has been effectively utilized to design various types of cholinesterase inhibitor molecules, including donepezil. Within this research study, we have questioned the significance of the benzyl group within this pharmacophore employing the urolithin derivatives. Urolithins are benzo[c]chromene analogue metabolites of ellagitannins, abundantly found in pomegranate and berry fruits. Read out full article here: http://www.eurekaselect.com/159057

 

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HIGHLIGHTED ARTICLE – TRYPANOTHIONE REDUCTASE: A TARGET FOR THE DEVELOPMENT OF ANTI-TRYPANOSOMA CRUZI DRUGS – MINI-REVIEWS IN MEDICINAL CHEMISTRY

MRMC-Articles-17 -18-2017-Gildardo Rivera

To access the article, please visit: http://www.eurekaselect.com/150897

Press Release for EurekAlert! New hopes in cancer battle — a review of new molecules and treatment strategies

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Cancer treatment is still one of the most intractable challenge for medicine. There are several approaches to fight cancer, which include: surgery, radiation therapy, chemotherapy, immunotherapy, targeted therapy and hormone therapy. From all these treatment methods, chemotherapy seems to be the most widely used. Therefore, it is understandable that scientists are trying to discover new molecules which may be applied as effective chemotherapeutics.

The researchers from Jan Dugosz University in Czstochowa and Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences reviewed the most significant achievements in the area of cancer treatment, published in 2014/2015. This review describes newly discovered anticancer molecules interacting with DNA or affecting cancer cell cycles. New cancer treatment strategies, which increase efficiency of chemotherapy or radiotherapy and new chemotherapeutic delivery systems have also been mentioned in the review. Multiplicity of the described compounds proves that cancer battle is still in progress. We constantly learn something new about cancer cells and hopefully we are getting closer to find effective cancer treatment. We know that molecules can interact with cancer DNA by inhibiting its synthesis, transcription or duplication.

Chemotherapeutics are also able to affect tumor cell cycle by suppressing itsproliferation and angiogenesis, and also promoting its apoptosis.

However, developing effective cancer treatment is, still, a demanding task because the number of cancer cell-types known to researchers constantly increases. In spite of all these odds, we hope that along with the development of science, people will win the race with still incurable cancers.

Reference: Turek, M.; (2016). New Hopes in Cancer Battle – A Review of New Molecules and Treatment Strategies Med. Chem., DOI: 10.2174/1573406412666160502153700

 

For more information about the article, please visit: http://benthamscience.com/journals/medicinal-chemistry/article/141662/

 

Press Release for EurekAlert! Non-ambient conditions in the investigation and manufacturing of drug forms

Before it reaches the store shelf, a drug molecule must be prepared in a very specific way. The nature of this prepared form is of the utmost importance, as it must be robust through manufacture, packaging, transport and storage. Ultimately, this prepared drug form must have the necessary physical properties to ensure that the correct amount of drug is available to the consumer. For the successful preparation of this drug form, one often needs to produce solid samples with a controlled crystal structure and specific particle size and shape. To complicate matters, these drug crystals are often required as a part of multi-component composites. The present review summarizes how extreme pressure and temperature conditions help to achieve this goal.

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To become a drug, a pharmacologically active compound must be prepared in a specific form. This form must be robust during manufacturing, packaging, storage and transport, and must administer the correct dose to the patient. To successfully prepare a drug form, one often needs to produce solid samples with controlled crystal structure and a specific particle size and shape. To further complicate matters, these compounds, these drug particles must often end up as a part of a multi-component composite. The present review summarizes how extreme pressure and temperature conditions help achieve this highly tuned material.

In modern culture, it is very rare to find an individual who has never taken any form of medication. It must follow that the pharmaceutical industry is required to produce an enormous quantity of drug products, which can take  a variety of different forms: solutions for injections, inhalation powders, sprays, tablets, ointments, patches, amongst others. In many cases, although adopting different administration routes, different trade names are used to market the very same active pharmaceutical ingredient (API). This begs the question: if these products are the same API, is there any difference in which form is taken?

Quite simply put, yes.

Drug molecules move around the body and, by necessity, act at the molecular level. However, many of these compounds are manufactured as solids, which must either be dissolved prior to injection, or are expected to dissolve on digestion in biological fluids. In either case, dissolution is required to release individual molecules into the body.

Solid pharmaceuticals containing the same API (either pure or with additives) can have different crystal structures (polymorphism) or be amorphous. Additionally, solid particles can differ in size, shape, meso-structure, and surface charge. Within the bulk material, the spatial distribution of an API and the additives can vary. Control of these, and many other, characteristics is within the scope of materials sciences and solid-state chemistry. The chemical and material properties of their physical form therefore needs to be identified and optimized for in vivo performance, reliable manufacture and the protection of intellectual property. 

Drugs are materials, not simply molecules [1-12], By viewing drugs in this way, one can apply the knowledge of solid-state chemistry, materials science and non-ambient conditions to obtain solid forms with optimized properties. These conditions include, among others, different types of mechanical and ultrasonic treatment, hydrostatic compression, high-temperature or cryogenic spray-drying, and crystallization from supercritical solvents. Solid-state reactions (e.g. dehydration or clathrate decomposition) can be efficient in accessing metastable polymorphs or in uniformly micronizing the sample. To achieve control over drug forms and the processes used for their robust manufacturing, one needs to account for both the thermodynamic and kinetic aspects of their transformations.

The review contains over 400 references and provides a comprehensive guide through the vast ocean of publications in this field. This work is based on the personal experience of the author over several decades of active research. ###

For more information visit: http://benthamscience.com/journals/current-pharmaceutical-design/volume/22/issue/32/page/4981/

Elena V Boldyreva

Institute of Solid State Chemistry and Mechanochemistry, Siberian Branch of Russian Academy of Sciences, ul. Kutateladze, 18, Novosibirsk 630128 Russia

 

Highlighted Article Of the Journal; Recent Patents on Drug Delivery & Formulation

DDF-Articles (3)

For details, visit: http://benthamscience.com/journal/index.php?journalID=rpddf

Recent Issue of Journal Drug Delivery Letters Have been published

Drug Delivery Letters, 4 Issue 3

Aims & Scope

Drug Delivery Letters publishes short papers in all important aspects of drug delivery, gene delivery, and drug targeting. Short papers report seminal results and research approaching conclusion of importance in the field.

The journal scope covers all basic and applied research in drug delivery and targeting at molecular and cellular levels and novel delivery systems. The manuscript submission process is fully electronic , to ensure the rapid publication of research results.

http://www.eurekaselect.com/125804/issue/3

Abstracted & Indexed In

PubsHub., J-Gate, and Chemical Abstracts.

For details about the latest issue, visit:

http://benthamscience.com/journal/index.php?journalID=ddl

Indian Authors have made substantial contributions to Bentham Science Journal, Current Drug Targets:

Journal Name: Current Drug Targets

Article Title: Sirtuins Family- Recent Development as a Drug Target for Aging, Metabolism, and Age Related Diseases

Author(s): Chiranjib Chakraborty and George Priya Doss. C

Abstract:Silent information regulator 2 (Sir2) proteins, or sirtuins, are a family of proteins which influence several physiological responses and have implications for treating diseases of ageing. In this context, we have presented a summarized view on the discovery of Sir2 family proteins, the enzymatic activities, the role of sirtuins in aging, lifespan and onset of age-related symptoms. In addition, we have described the roles of mammalian sirtuins-with particular emphasis on their associations to aging, metabolism, and age related diseases with recent references. Current findings provide an understanding about mammalian sirtuins and their target diseases, small molecules discovery or drug discovery targeting sirtuin to tackle the serious diseases of aging.

For details, visit: http://benthamscience.com/journal/abstracts.php?journalID=cdt&articleID=109718

 

Article Title: Crucial Protein Based Drug Targets and Potential Inhibitors for Osteoporosis: New Hope and Possibilities

Author(s): Chiranjib Chakraborty and C George Priya Doss

Abstract:Osteoporosis, a multifaceted bone disorder, is considered as a serious health problem throughout the world and the magnitude of diseased patients is increasing day by day. A number of successful therapeutics is available in the market for treatment. However, upon long-term administration, most of these drugs cause side-effects with some limitations. Henceforth, development of new therapeutic strategies can be a way to solve this problem as well as to develop cost effective and better tolerated therapies. Detailed understanding about the mechanistic action of the drug targets can be a great aid in the drug development process. Here in this review, we discussed the existing potential protein target class and their inhibitors related to osteoporosis. We have highlighted the existing potential protein drug targets, oestrogen receptor, calcium sensing receptor, P2Y receptor, activin receptor, calcitonin receptor, therapeutic manipulation of protease class such as cathepsin K, targeting WNT/ β-catenin signaling and targeting RANK-RANKL signaling pathway, TNF inhibition through TNF receptor. We hope this detailed report will provide a better way of understanding towards the discovery and also for development of novel therapeutics.

For details, visit: http://benthamscience.com/journal/abstracts.php?journalID=cdt&articleID=116634

 

Article Title: The First Approved Agent in the Glitazar’s Class: Saroglitazar

Author(s): Ritesh Agrawal

Abstract: The new chemical entity (NCE) has been knocked as novel antidiabetic agent, e.g. Saroglitazar. Saroglitazar is a drug for the treatment of Type II diabetes. Saroglitazar is marketed under the trade name Lipaglyn, developed by the Zydus Cadila. Lipaglyn is the first indigenously developed NCE by any Indian pharmaceutical company, ever. Lipaglyn has been approved for the treatment of Type II diabetes by the Drug Controller General of India in June 2013. Lipaglyn is indicated for the patients suffering from diabetes dyslipidemia. It also provides the option of a once-daily oral therapy. Saroglitazar regulates the lipid parameters as well as glycemic control. The present article describes Saroglitazar with its chemical synthesis and patent status with its summary of clinical studies.

For more details, visit: http://benthamscience.com/journal/abstracts.php?journalID=cdt&articleID=113860

 

Article Title: Identification of Novel Drug Targets in HpB38, HpP12, HpG27, Hpshi470, HpSJM180 Strains of Helicobacter pylori : An In Silico Approach for Therapeutic Intervention

Author(s): Nageswara Rao Reddy Neelapu and T. Pavani

Abstract: Helicobacter species colonizes the stomach and are associated with the development of gastritis disease. Drugs for treatment of Helicobacter infection relieve pain or gastritis symptoms but they are not targeted specifically to Helicobacter pylori. Therefore, there is dire need for discovery of new drug targets and drugs for the treatment of H. pylori. The main objective of this study is to screen the potential drug targets by in silico analysis for the potent strains of H. pylori which include HpB38, HpP12, HpG27, Hpshi470 and HpSJM180. Genome and metabolic pathways of pathogen H. pylori and the host Homosapien sapiens are compared and genes which were unique to H. pylori were filtered and catalogued. These unique genes were subjected to gene property analysis to identify the potentiality of the drug targets. Among the total number of genes analysed in different strains of H. pylori nearly 558, 569, 539, 569, 567 number of genes in HpB38, HpP12, HpG27, Hpshi470 and HpSJM180 found qualified as unique molecules and among them 17 qualified as potential drug targets. Membrane fusion protein of hefABC efflux system, 50 S ribosomal protein L33, Hydrogenase expression protein/formation of HypD, Cag pathogenecity island protein X, Apolipoprotein N acyl transferase, DNA methyalse, Histone like binding protein, Peptidoglycan-associated lipoprotein OprL were found to be critical drug targets to H. pylori. Three (hefABC efflux system, Hydrogenase expression protein/formation of HypD, Cag pathogenecity island protein X) of the 17 predicted drug targets are already experimentally validated either genetically or biochemically lending credence to our unique approach.

For more details, visit: http://benthamscience.com/journal/abstracts.php?journalID=cdt&articleID=109207

NEWS!!

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Chemical Abstracts Service (CAS) indexes Current Chromatography and Clinical Cancer Drugs:

Chemical Abstracts Service, a division of the American Chemical Society accepts to index two new journals Current Chromatography and Clinical Cancer Drugs published by Bentham Science Publishers.

Chemical Abstracts Service (CAS) aims to deliver comprehensive and useful digital information environment for scientific research and discovery. 

Current Chromatography is an international peer-reviewed journal, which publishes expert reviews, original research articles and thematic issues in all core areas of separation science. For details, please visit the journal website at:http://benthamscience.com/journal/index.php?journalID=cchg.

Clinical Cancer Drugs publishes original research, expert reviews, and thematic issues in all core areas of translational and clinical cancer drug research. For details, please visit the journal website at: http://benthamscience.com/journal/index.php?journalID=ccand.

For more details, visit: http://benthamscience.com/press-release-main.php

A Basic Introduction to Drugs, Drug Targets and Molecular Interaction

Watch this simple yet engaging video on the basics of drugs, drug targets and molecular interaction on our Youtube Channel:

https://www.youtube.com/watch?v=nF2sKS1F-O8

It is illustrative and informative, and you will definitely enjoy watching it. To learn more about drugs and drug targets, Bentham Science Publishers offer a number of journals, such as Current Drug Targets, Current Drug Therapy, Current Drug Metabolism, Current Drug Safety etc. Kindly check http://benthamscience.com/a-z.htm#C for more details.

Drugs, Drug Targets and Molecular Interaction
Drugs, Drug Targets and Molecular Interaction
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