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Mini Reviews in Medicinal Chemistry

Fei Ding, Yongmin Zhang
Glycans expressed on the forefront surface of cells participate in many key biological processes via forming various glycoconjugates. The recognition of complex glycoconjugates as mediators of important biological processes has stimulated investigation into their therapeutic potential. As the increasing accessibility of glycoconjugates, it has been widely applied in the field of drug delivery. This review particularly refers to the constitutive glycoconjugates of receptor-mediated binding of glycoprotein, glycolipids and glycopeptides for cell-selective drug delivery, in order to broaden the future therapeutic scope of drug delivery system and effective cancer therapy...
May 17, 2018: Mini Reviews in Medicinal Chemistry
Margarita Gutierrez, Francisco Valdes, Victor Luna, Barbara Arevalo, Nelson Brown
Since 1929, several researchers have conducted studies in relation the nucleoside of adenosine (1) mainly distribution identifying, characterizing their biological importance and synthetic chemistry to which this type of molecule has been subjected to obtain multiple of its derivatives. The receptors that interact with adenosine and its derivatives, called purinergic receptors, are classified as A1, A2A, A2B and A3. In the presence of agonists and antagonists, these receptors are involved in various physiological processes and diseases...
May 16, 2018: Mini Reviews in Medicinal Chemistry
Jinyun Dong, Qijing Zhang, Qingqing Meng, Zengtao Wang, Shaoshun Li, Jiahua Cui
Thioflavone derivatives are the thio analogs of the core constituent of the natural product class of flavones. Based on the position and oxidation level of sulfur, they can be divided into three major categories: 4-thioflavones, 1-thioflavones and 1-thioflavones 1,1-dioxide. In recent years, great efforts have been made to develop an approach to thioflavones, especially 1-thioflavones with high functional group compatibility, high yields, low toxicity as well as proceeding under a mild condition, and a variety of synthetic protocols have been developed, the method of choice being dependent on the nature of substrates...
May 15, 2018: Mini Reviews in Medicinal Chemistry
Shalki Choudhary, Om Silakari, Pankaj Kumar Singh
Heterocyclic compounds bearing nitrogen and sulphur have drawn strong attention due to their useful biological and pharmacological properties. Thiazine is a promising scaffold among these heterocyclic compounds which has been widely utilized in synthesis of compounds that possess interesting biological activities, such as anti-tumour, anti-microbial, antipsychotic, antifungal, antiviral, analgesic and anti-inflammatory. Present review focuses on the chemistry of thiazine and its derivatives as well as potential pharmacological activities reported in scientific literature...
April 27, 2018: Mini Reviews in Medicinal Chemistry
Atul N Khadse, Mayank Kumar Sharma, Prashant R Murumkar, Sadhana J Rajput, Mange Ram Yadav
Development of new anticoagulants has been in constant demand throughout the world due to increasing rate of morbidity and mortality caused by thrombotic diseases. Factor Xa (FXa), one of the enzymes and validated target for anticoagulation, regulates the production of thrombin in the coagulation cascade. The importance of oral FXa inhibitors like rivaroxaban, apixaban and edoxaban in thromboembolic conditions is well supported by increasing number of patents and research publications during the recent years...
April 24, 2018: Mini Reviews in Medicinal Chemistry
Nehad Ahmed Abdel Latif, Rasha Zakaria Batran, Salwa F Mohamed, Mohamed A Khedr, Mohamed Kobeasy, Sara Al-Shehri, Hanem Awad
METHOD: Two new series of 4-styryl-7-oxycoumarin derivatives 3a-i and 4-styryl-7-oxycoumarin-8-Mannich bases 6a-r were designed and synthesized. Ten compounds were evaluated for their antioxidant activity in vitro against DPPH and in vivo against lipid peroxidation, superoxide dismutase (SOD), glutathione-s-transferase (GST) and catalase (CAT) activities. Molecular modeling study was performed to predict the mode of binding of the target compounds in the binding site. RESULTS & CONCLUSION: Although the tested compounds showed moderate to low dose dependent DPPH inhibition activities in vitro, most of them displayed remarkable antioxidant effects in vivo...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Anna Katarzyna Szczepanska, Katarzyna Malinowska, Ireneusz Majsterek
The incidence of head and neck cancer increases every year, and represents a significant problem for Molecular Biology at the beginning of the twenty-first Century. Despite advances in treatment, most studies still strive to deepen the understanding of the mechanisms of cancerogenesis. In order to develop more effective methods of diagnosis and therapy, it is necessary to understand the molecular basis of the neoplastic transformation process. Such findings obtained by research into Molecular Biology, Molecular Epidemiology and Genetics have brought significant progress in understanding the complex, multi-step process which takes place during tumor formation...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Yichao Ge, Kui-Wu Wang
As a kind of common compositions in plants, there are many characteristic features of researches about aporphine alkaloids, which exhibit various biological activities: anti-tumor, anti-viral, anti-microbial, anti-inflammatory etc. The review gives information on aporphine alkaloids and their derivatives and provide an overview of the latest progress in the structural diversity and the biological activity of the aporphine alkaloids isolated from natural resource in recent years. The synthetic approaches to aporphine alkaloids are also presented...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Nawal Serradji, V U Thi Huyen, Hyunjoon Kim, Jayanth Panyam, Philippe Verbeke
Chlamydia trachomatis is responsible for the most frequent sexually transmitted bacterial infection in the world and for trachoma, the world's leading infectious cause of blindness. Genital chlamydial infection is very common among sexually active young people, and when untreated, leads to serious complications. No vaccine is available. Although Chlamydia resistance to antibiotics is rarely observed in vivo, studies showed that 10-20% of patients remain infected at the end of antibiotherapy, without being reinfected...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Paulo Andre Teixeira De Moraes Gomes, Lindomar Jose Pena, Ana Cristina Lima Leite
Arboviruses have been spreading rapidly throughout the Western Hemisphere in recent decades. Among the arboviruses with high morbidity and mortality are members of the Alphavirus and Flavivirus genera. Within the first genus, Chikungunya virus (CHIKV) is considered one of the most challenging human arboviral infections with global significance and without any specific antiviral agent. Flaviviruses are some of the most important causes of encephalitis, haemorrhagic disease, and developmental defects. Japanese encephalitis virus (JEV), West Nile virus (WNV), dengue virus (DENV) and Zika virus (ZIKV) are examples of flaviviruses without clinically approved antiviral agents...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Yang Li, Yanpeng Li, Jun He, Ding Liu, Qizhi Zhang, Kang Li, Xing Zhang, Guotao Tang, Yu Guo, Yunmei Liu
Chrysin show many different physiological activities, including anti-oxidant, anti-inflammatory, anti-bacterial, anti-allergic, anti-diabetic and so on. In recent years, with the expection to develop more active drug for clinic, the many scholars at home and abroad focused on the synthesis and biological activities of its derivatives. This review summarizes a large number of chrysin derivatives and analyzes their biological structure-activity relationships.
April 23, 2018: Mini Reviews in Medicinal Chemistry
Nasimossadat Banarouei, Asghar Davood, Hamed Shafaroodi, Ghazaleh Saeedi, Abbas Shafiee
BACKGROUND AND OBJECTIVE: N-aryl derivatives of phthalimide and 4-nitro phthalimide have demonstrated cyclooxygenase inhibitory activity. Also they possess an excellent analgesic and anti-inflammatory activity. In this work, a new series of N-arylmethylideneamino derivatives of phthalimide and 4-nitro phthalimide were designed and synthesized. METHODS: The designed compounds were synthesized by condensation of the appropriate aldehyde and N-aminophthalimide in ethanol at room temperature at PH around 3...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Yuefei L Wang, Qianfei Huang, Dedong Kong, Ping Xu
Proteins are present in a wide range of our everyday foods and complex macromolecules made up of one or more polypeptide chains. From these common food, large amount of bioactive peptides can be produced. An array of biological health effects have been attributed to these peptides, including antioxidative, antihypertensive, antidiabetic, anticoagulant, antithrombotic, anti-inflammatory, hypocholesterolemic and immunomodulating. The chemical structure of biological active peptides were closely related with its specific biological activity...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Sobhi M Gomha, Abdou Osman Abdelhamid, Omaima Kandil, Saher Kandeel, Nadia Abdelriheem
A series of novel thiazole-pyranochromene and thiadiazole-pyranochromene derivatives were synthesized via heterocyclization of varies hydrazonoyl halides with methyl pyrano[3,2-g] chromen-3-yl)ethylidene)hydrazine-1-carbodithioate and pyrano[3,2-g]chromen-3-yl)ethylidene) hydrazine-1-carbothioamide, respectively. All the newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, 1H and 13C NMR, Mass). Moreover, all the products were evaluated for their anticancer activity against HEPG2-1...
April 23, 2018: Mini Reviews in Medicinal Chemistry
Priyankar Paira, S K Ashok Kumar, Sourav De, Subhasis Banerjee
Dipeptidyl Peptidase is one of the novel targets for antidiabetic and anticancer drugs. The dipeptidyl amminopeptidase IV, expressed in mammalian, releases X-Pro/Ala dipeptides from the N-terminus of peptides. It is responsible for the degradation of the incretin hormones which regulate blood glucose level. At present several DPP-IV inhibitors are approved for type-2 diabetes mellitus. These enzymes are also expressed in dimeric form on the surface of different cells (mature thymocytes, activated T cells, B cells, NK cells, macrophages, renal, prostate, liver and small intestinal epithelium, biliary canaliculae, and splenic sinus lining cells)...
April 22, 2018: Mini Reviews in Medicinal Chemistry
Zhao-Peng Liu, Yan Wang
Statins are currently the major therapeutic strategies to lower low-density lipoprotein cholesterol (LDL-C) levels. However, a number of hypercholesterolemia patients still have a residual cardiovascular disease (CVD) risk despite taking the maximum-tolerated dose of statins. Proprotein convertase subtilisin/kexin type 9 (PCSK9) binds to low-density lipoprotein receptor (LDLR), inducing its degradation in the lysosome and inhibiting LDLR recirculating to the cell membranes. The gain-of-function mutations in PCSK9 elevate the LDL-C levels in plasma...
April 22, 2018: Mini Reviews in Medicinal Chemistry
Barbara Cacciari, Stephanie Federico, Giampiero Spalluto
In the past decades, many efforts were done to develope ligands for the adenosine receptors, with the purpose to individuate agonists and antagonists affine and selective for each subtypes , named A1, A2A, A2B, and A3. These intense studies allowed a deeper and deeper knowledge of the nature and, moreover, of the pathophysiological roles of all the adenosine receptor subtypes. In particular, the involvment of the A2A adenosine receptor subtype in some physiological mechanisms in the brain, that could be related to important diseases such as the Parkinson's disease, encouraged the research in this field...
April 22, 2018: Mini Reviews in Medicinal Chemistry
Gangliang Huang, Fang Chen
At present, the polysaccharide antitumor research is focused on how to further improve the antitumor activity of polysaccharides. The structural modification of polysaccharides can enhance their antitumor activity to a certain extent. Herein, the common methods of polysaccharide modification, such as sulfation, carboxymethylation, phosphorylation and acetylation, were summarized. The antitumor mechanisms of polysaccharide derivatives mainly contain the inducing apoptosis of tumor cells, effecting on the cycle of tumor cells, enhancing the antioxidant activity of organism, activating the body's immune response, and inhibiting the tumor angiogenesis...
April 16, 2018: Mini Reviews in Medicinal Chemistry
Shalki Choudhary, Pankaj Kumar Singh, Om Silakari
Nitrogen and sulphur based heterocyclic molecules have gained significant attention owing to their broad spectrum pharmacological profiles. Thiazine is one of such promising scaffolds which has been widely utilized in the synthesis of compounds that possess interesting biological profile including anti-proliferative, anti-bacterial, antipsychotic, analgesic, anti-inflammatory, antifungal and antiviral activities. The current review focus on the chemistry of thiazine and its derivatives along with potential pharmacological activities reported for them in scientific literature...
April 16, 2018: Mini Reviews in Medicinal Chemistry
Sarel Francois Malan, Rajan Sharma, Jacques Joubert
The free radical nitric oxide (NO) is considered one of the most versatile endogenous molecules and is a crucial signalling molecule in numerous biochemistry pathways of the human body. NO is directly related to pathological processes and plays an important role in many different and interrelated physiological processes. In some cases, a depletion of NO or an attenuation of its effector system could exist as in hypertension, angina and impotence; in others, an overproduction of NO may be a major cause of damage, as in circulatory shock, sepsis, neurodegenerative disorders and inflammatory responses...
April 16, 2018: Mini Reviews in Medicinal Chemistry
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