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Mini Reviews in Medicinal Chemistry

Amit K Keshari, Ashok K Singh, Sudipta Saha
Thiazolopyrimidine derivatives containing bridgehead nitrogen atom are now-a-days attracting the attention of many medicinal chemists throughout the world to explore this framework for its potential. This biologically important scaffold is formed by the fusion of two aromatic rings, thiazole and pyrimidine, in such a way that one carbon atom at the ring junction is replaced by a nitrogen atom and is, therefore, being common for both the heterocyclic rings. One of the most common example of this type of fusion is thiazolo[3,2-a]pyrimidine which is being used perpetually with tremendous success in various field of therapeutic applications...
February 16, 2017: Mini Reviews in Medicinal Chemistry
Marcela Krečmerová
The review covers basic principles of the prodrug strategy applied to antiviral nucleoside drugs or drug candidates. Specific role of amino acids as promoieties is explained with respect to transport mechanisms, pharmacokinetics and a low toxicity of compounds. Synthetic approaches to the most important representatives (compounds under clinical investigations or available on the market) are described, including valacyclovir, valganciclovir, valomaciclovir stearate, valcyclopropavir, valtorcitabine, valopicitabine and several attempts to amino acid modifications of antiretroviral nucleosides...
February 16, 2017: Mini Reviews in Medicinal Chemistry
Mayank Kinger, Sushil Kumar, Vinod Kumar
Inflammation plays an important role in maintaining the body's homeostasis. It repairs the damaged tissues of the body resulting from injury or infection. In addition, a diverse array of diseases like hepatitis, arthritis and colitis has been reported and described to be associated with inflammatory processes. Some autoimmune diseases like inflammatory bowel disease (IBD) emerge by the influence of numerous genes in complex environmental situations belongs to inflammation. The currently available processes for curing inflammation and related disorders facilitate the use of non steroidal anti-inflammatory drugs (NSAIDs)...
February 8, 2017: Mini Reviews in Medicinal Chemistry
Pedro Aguilar-Zárate, Jorge E Wong-Paz, Juan J Buenrostro-Figueroa, Juan A Ascacio, Juan C Contreras-Esquivel, Cristóbal N Aguilar
The ellagitannins are a group of phenolic compounds with biological activities. The ellagic acid is the product obtained from hydrolysis of ellagitannins. Information related to the biosynthesis of ellagitannins still been scarce and confused. The ellagitannins are obtained from plants and their purification process implies mainly the use of chromatographic techniques. The ellagitannin acyl hydrolase (EAH) also known as ellagitannase is an enzyme capable to hydrolyze the ester bonds of ellagitannins and the consequent releasing of ellagic acid...
February 8, 2017: Mini Reviews in Medicinal Chemistry
Mehdi El Arbi, Emna Ketata, Aref Neifar, Wafa Mihoubi, Girish K Gupta, Pascal Pigeon, Siden Top, Ali Gargouri, Gérard Jaouen
The inhibitory effects of four series of aryl butene derivatives, active against breast cancer, on the monophenolase activity of tyrosinase, in melanin-free ink from Sepia officinalis, have been studied. Hydroxytamoxifen 1, ferrociphenol 17 and several aryl butene analogs have shown strong antiproliferative activity on hormone-dependent and hormone-independent breast cancer cells and were evaluated in leukemia K562 cell proliferation. Their potential to induce skin depigmentation by evaluating their anti-tyrosinase activity was also estimated...
February 8, 2017: Mini Reviews in Medicinal Chemistry
Zhi Li, Wen-Hua Chen
Synthetic anionophores are created to mediate the transmembrane transport of anions across phospholipid bilayer membranes. By replacing the defective natural anion channels, they are thought to have high potentials as chemotherapeutic agents for the treatment of channelopathies. In addition, there is a hope that synthetic anionophores may serve as therapeutic agents for cancers and bacterial infections. Because of the amphiphilicity of phospholipid bilayer membranes, lipophilicity has been well studied as one of the most important structural factors that affect the activity of synthetic anionophores...
February 6, 2017: Mini Reviews in Medicinal Chemistry
Daniel Tarade, Siyaram Pandey, James McNulty
One of the most studied anti-cancer compounds of the last several decades is the microtubule targeting agent and cis-stilbene, combretastatin A4 (CA4). Despite promising results at the pre-clinical level, future clinical use of CA4 as a monotherapy is in question due metabolic vulnerability and conformational instability. Thus, medicinal chemists have focused on synthesizing derivatives with improved pharmokinetic profile. One common strategy has been the incorporation of the ethylene linker into a ring system, thus preventing the isomerization of CA4 into the virtually inactive trans-isomer...
January 27, 2017: Mini Reviews in Medicinal Chemistry
G Chawla, B Naaz, A A Siddiqui
Inflammation is the condition associated with many life-threatening diseases like cancer, cardiovascular diseases, Alzheimer's disease etc. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to reduce inflammation. One common problem associated with them is the gastric side effects which restrict their frequent use. The researchers have been involved in developing newer NSAIDs with the effort to reduce their adverse effects. Among the various heterocyclic moieties, the 1,3,4-oxadiazole moiety is found to have a wide range of pharmacological activities and attracting the researchers to work on this nucleus...
January 27, 2017: Mini Reviews in Medicinal Chemistry
Nutan Sharma, Sunita Bhagat, Tejpal Singh Chundawat
GPR40, an orphan G-protein coupled receptor that is activated by medium and long-chain fatty acids and is highly expressed in pancreatic islets, adipose depots and the gastrointestinal tract are involved in energy source recognition, absorption, storage and/or metabolism. Since its deorphanization in 2003, G-protein-coupled receptor GPR40 have emerged as potential target for type II diabetes because they have been hypothesized to participate in the adverse effects of chronic fatty acid exposure on function of β-cell...
January 20, 2017: Mini Reviews in Medicinal Chemistry
Solomon Habtemariam, Abebech Belai
Inflammatory bowel disease (IBD), commonly represented by ulcerative colitis and Crohn's disease, is a form of chronic inflammatory disorders of the gastrointestinal system. Its current drug treatment include the use of antibiotics, 5-aminosalicylates, corticosteroids, immune-modifying agents and biologics such as anti-TNF agents and adhesion molecules blockers. These drugs have inherent problems of efficacy as many IBD sufferers need surgical intervention at some stage, high cost especially for the protein-based drugs, loss of efficacy and unwanted side effects...
January 20, 2017: Mini Reviews in Medicinal Chemistry
Anna Lucia Tornesello, Maria Lina Tornesello, Franco M Buonaguro
Radiolabeled peptides, designed to bind with high affinity receptors selectively expressed on cell membranes of different human tissues, represent valuable tools for in vivo imaging of several human diseases. Solid-phase peptide synthesis as well as availability of bifunctional chelating agents and prosthetic groups allows the production and radiolabeling of several peptide-based molecules which are useful to target specific receptors on different cancer types. Among them, octreotide and other analogues of somatostatin, vasoactive intestinal peptide, CCK analogues, bombesin, α-MSH analogues, neurotensin, exendin, RGD substance P, conjugated to appropriate chelators, such as DTPA, NOTA, DOTA or TETA, and radiolabeled with specific radionuclides, have already been translated into the clinical practice with remarkable sensitivity and diagnostic accurateness...
January 20, 2017: Mini Reviews in Medicinal Chemistry
Sunita Thapa, Min Lv, Hui Xu
Acetylcholinesterase is a serine hydrolase that terminates the action of the neurotransmitter acetylcholine by hydrolyzing it into acetic acid and choline. The molecule, having an ellipsoidal structure, possesses three binding sites; active site (with catalytic anionic and esteratic subsites), aromatic gorge and peripheral anionic site, where the inhibiting compounds interact. The acetylcholinesterase inhibitors bind to the molecule and interfere with the breakdown of acetylcholine leading to the deposition of acetylcholine in the nerve synapses and causing disrupted neurotransmission...
January 20, 2017: Mini Reviews in Medicinal Chemistry
Miroslav Pohanka
Quantum dots are an emerging nanomaterial with broad use in technical disciplines. However, their application in field of biomedicine becomes also relevant and significant possibilities have appeared since the discovery in 1980s. The current review is focused on therapeutic applications of quantum dots. They are introduced as potent carriers of drugs and as a material well suited for diagnosis of disparate pathologies like visualization of cancer cells or pathogenic microorganisms. Quantum dots toxicity and modifications for the toxicity reduction are discussed here as well...
January 20, 2017: Mini Reviews in Medicinal Chemistry
Gangliang Huang, Fengying Zhao, Lu Zhou, Shiqi Huang, Hui Li
In recent years, the antioxidant effects of polysaccharides have become a hot spot in the field of polysaccharide research. Herein, the action mechanisms of polysaccharide antioxidation and scavenging free radicals were analyzed. The research progresses on the preparation methods and antioxidant properties of polysaccharides and their derivatives were reviewed. Investigating the antioxidant activities of polysaccharides and their derivatives can find useful polysaccharides and their derivatives, which have great potential as natural antioxidants used in functional foods or medicines...
January 16, 2017: Mini Reviews in Medicinal Chemistry
Cecília Patrícia Popolin, Márcia Regina Cominetti
Cancer is one of the main causes of death worldwide. Breast cancer is the most prevalent type of cancer in women and the leading cause of cancer deaths due to its high metastasis to the lymph nodes, lungs bones and brain. Interactions with the stromal microenvironment surrounding tumor cells facilitate tumor cell migration and invasion of tissues and dissemination to other organs, to form metastasis. The development of antitumor metal-based drugs was originated with the discovery of cisplatin, however, its severe side effects represent a limitation for its clinical use...
6, 2017: Mini Reviews in Medicinal Chemistry
Abbas Ahmadi, Mohsen Khalili, Zahra Olama, Shirin Karami, Babak Nahri-Niknafs
Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most widely used drugs worldwide and represent a mainstay in the therapy of acute and chronic pain and inflammation. The traditional NSAIDs like ibuprofen (I) contain free carboxylic acid group which can produce gastro-intestinal (GI) damage in long-term using of them. In order to obtain the novel NSAIDs with less side effects; carboxylic acid moiety has been modified into various amide groups which is the most active area of research in this family...
December 26, 2016: Mini Reviews in Medicinal Chemistry
Dnyaneshwar D Subhedar, Mubarak H Shaikh, Santosh G Tupe, Mukund V Deshpande, Vijay M Khedkar, Prakash C Jha, Bapurao B Shingate
We have synthesized new quinolidinyl-thiazolidinones via knoevenagel condensation-alkylation catalyzed by [Et3NH][HSO4] has been developed. The present approach offers several advantages such as higher yields, eco-friendly reaction condition and economic availability of the catalyst. The synthesized compounds were evaluated for their in vitro antifungal activity against six fungal strains. Some of the synthesized conjugates were displays good to moderate antifungal activity. Again, the molecular docking study against the fungal sterol 14α-demethylase (CYP51) showed an excellent binding affinity towards the enzyme which could rationalize the promising antifungal activity portrayed by these derivatives and provides a platform for structure based drug design...
December 26, 2016: Mini Reviews in Medicinal Chemistry
Sharique A Ali, Ishrat Naaz, Kamal Uddin Zaidi, Ayesha Sharique Ali
Skin pigmentation is a broadly appearing phenomenon in nature which plays an important task of determining the appearance and biology of all vertebrates including human beings. Skin color is a crucial attribute, determined by the synthesis of melanin pigment within melanocytes by the process of melanogenesis and is regulated by many extrinsic as well as intrinsic factors. Tyrosinase catalyzes the key step of melanogenesis, dysfunction of tyrosinase leads to reduce melanin production which results in severe clinical and aesthetical problems of hypopigmentation...
December 23, 2016: Mini Reviews in Medicinal Chemistry
Sobhi M Gomha, Mohamad R Abdelaziz, Hassan M Abdel-Aziz, Shaimaa A Hassan
A series of novel thiazolederivatives were synthesized in a good yield via reaction of 2-(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)hydrazinecarbothioamide with hydrazonoyl halides. The reaction was performed in the presence of DABCO as an organocatalystin short reaction times, easy workup, good to excellent yields. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data and alternative routes whenever possible. Ten compounds were evaluated for their anti-cancer activity against the colon carcinoma cell line (HCT-116)...
December 23, 2016: Mini Reviews in Medicinal Chemistry
Blanka Klimova, Michal Novotny, Kamil Kuca
BACKGROUND: At present there are about 47.5 million people suffering from different types of dementia and by 2030 this number should reach 75.6 million. This obviously brings about serious social and economic burden for people suffering from any kind of dementia. OBJECTIVE: The purpose of this article is to explore only semantic dementia (SD) as one of the forms of frontotemporal dementia (FTD) and provide the latest information on its diagnosis and treatment which play a significant role in the maintenance of quality of life of both patients and their caregivers...
December 23, 2016: Mini Reviews in Medicinal Chemistry
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