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Mini Reviews in Medicinal Chemistry

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https://www.readbyqxmd.com/read/30009707/novel-opioid-receptor-agonists-with-reduced-morphine-like-side-effects
#1
Lianghan Zhu, Zhiying Cui, Qihua Zhu, Xiaoming Zha, Yungen Xu
Opioid analgesics, such as morphine, are wildly employed in the treatment of moderate to severe pain. However, they are notorious for abuse liability and respiratory depression. Therefore circumventing the side effects, such as euphoria, addiction, respiratory depression and gastrointestinal adverse reactions, is of extensive importance. Recently, a large number of research results have revealed that such morphine-like side effects are not inevitable, and they focus on the novel approaches to disconnecting the analgesics from adverse effects...
July 16, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/30009706/substituted-aminobenzothiazole-derivatives-of-tacrine-synthesis-and-study-on-learning-and-memory-impairment-in-scopolamine-induced-model-of-amnesia-in-rat
#2
Abbas Ahmadi, Mehrdad Roghani, Sanaz Noori, Babak Nahri-Niknafs, Hengameh Bakhtiar
BACKGROUND: Currently, there is no conclusive cure for Alzheimer's disease (AD) and existing treatments mainly offer symptomatic relief. Dysfunction of the cholinergic system plays an important role in pathogenesis of AD. Tacrine (1, 2, 3, 4-tetrahydroacridin-9-amine, I) was the first approved agent for the palliative therapy of AD but its use is associated with some complications. Development of novel multi target derivatives of Tacrine with lower complications is strongly warranted...
July 16, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/30003859/the-role-of-sensing-peptides-in-the-cross-talk-between-microbiota-and-human-cancer-cells
#3
Anna Lucia Tornesello, Luigi Buonaguro, Maria Lina Tornesello, Franco Maria Buonaguro
The epithelium of the gastrointestinal tract is densely populated by complex microbial communities which exert both local and distant effects in the human body with relevant consequences on the metabolic status, immune system and overall health. A dynamic equilibrium between the many bacterial species and the host intestinal epithelium is maintained through the release of a large number of small molecules and peptides. The quorum sensing peptides are mainly secreted by Gram-positive bacteria and are able to "communicate" with human cells...
July 12, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29962341/development-of-thiazole-5-carboxylate-derivatives-as-selective-inhibition-of-monoacylglycerol-lipase-as-a-target-in-cancer
#4
Md Rahmat Ali, Suresh Kumar, Nishtha Shalmali, Obaid Afzal, Sabir Azim, Damini Chanana, Ozair Alam, Yamnath Paudel, Manju Sharma, Sandhya Bawa
The signalling function of 2-arachidonoylglycerol (2-AG) in endocannabinoid system is delineated by Monoacylglycerol lipase (MAGL). MAGL readdresses the lipid stores in the direction of pro-tumorigenic signalling lipids in cancer cells. Selective as well as potent MAGL inhibitors are limited in number hence their continuous development may lead to a breakthrough invention in the field of MAGL inhibitors. In succession of the above, we have synthesised 2-amino-4-methylthiazole-5-carboxylate derivatives and characterized them by collective use of IR, 1H-NMR, 13C-NMR, Mass spectral data and elemental analysis...
July 1, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29956627/pharmacological-effects-and-chemical-constituents-of-bupleurum
#5
Peng Sun, Yijie Li, Sheng Wei, Tingting Zhao, Yang Wang, Chunhong Song, Ling Xue, Fushun Wang, Lingyun Xiao, Jibiao Wu, Mingqi Qiao
Radix Bupleuri is commonly used in traditional Chinese medicine for thousands of years with confirmed curative effects. Except for medicine, it is also used in healthy food, and cosmetics for its specifc activities. Therefore, the chemical constituents, mainly including flavonoids, lignins, Phenyl propanol derivatives, triterpenoid saponins, and volatile oils, and pharmacological effects have been well studied by many scholars in recent years and a comprehensive and systematic review on chemical constituents and pharmacological effects of Radix Bupleuri is indispensable...
June 28, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29943701/asymmetric-finite-size-of-ions-and-orientational-ordering-of-water-in-electric-double-layer-theory-within-lattice-model
#6
Ekaterina Gongadze, Veronika Kralj-Iglic, Ales Iglic
In the present short communication, a brief historical survey of the mean-field theoretical description of electric double layer (EDL) is presented. A special attention is devoted to asymmetric finite size of ions and orientational ordering of water dipoles. A model of Wicke and Eigen, who were first to explicitly derive the ion distribution functions for finite size of ions, is discussed. Arguments are given in favour of changing the recently adopted name of the mean-field EDL model for finite size of ions from Bikerman model to Bikerman-Wicke-Eigen model...
June 25, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29848275/design-synthesis-and-in-vivo-anti-inflammatory-activity-of-new-celecoxib-analogues-as-nsaid
#7
Naglaa A Abdel Hafez, Korany A Ali, Alhussein A Ibrahim, Dina H Elnaggar, Amany A Sleem
A new series of celecoxib analogues were easily synthesized via reactions of 4-(2-(1-chloro-2-oxopropylidene)hydrazinyl)benzene sulfonamide (1) with active methylene compounds and dialkyl malonate. In addition, Compound 1 was reacted also with thiourea derivatives and thiosemicarbazone derivatives to afford thiazole derivatives 9 and 11, respectively. Furthermore, triazolo pyrimidine derivatives 13 were prepared via reaction of compound 1 with pyrimidine thione derivatives. The structures of the newly compounds were assigned by elemental analysis and spectroscopic data...
May 30, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29792145/1-2-4-oxadiazole-as-a-privileged-scaffold-for-anti-inflammatory-and-analgesic-activities-a-complete-review
#8
Gita Chawla, Chanda Ranjan, Anees A Siddiqui
1,2,4-Oxadiazole is one of the important heterocycles used by medicinal chemists in designing a new therapeutic molecule. The compounds containing this nucleus are reported to have a wide range of pharmaceutical and biological applications including anti-inflammatory and analgesic activities. The fused and pendent 1,2,4-oxadiazole moiety has been traced in a number of well established, commercially available drugs. This review article provides an up to date information about techniques adopted for the synthesis of 1,2,4-oxadiazoles, and their therapeutic importance as an anti-inflammatory and analgesic agents...
May 23, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29792144/biomedical-applications-of-aromatic-azo-compounds-from-chromophore-to-pharmacophore
#9
Yousaf Ali, Shafida Abd Hamid, Umer Rashid
Azo dyes are widely used in textile, fiber, cosmetic, leather, paint and printing industries. Besides their characteristic coloring function, biological properties of certain azo compounds including antibacterial, antiviral, antifungal and cytotoxic are also reported. Azo compounds can be used as drug carriers, either by acting as a 'cargo' that entrap therapeutic agents or by prodrug approach. The drug is released by internal or external stimuli in the region of interest, as observed in colon-targeted drug delivery...
May 23, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29773059/biomedical-applications-of-glycoconjugates
#10
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
https://www.readbyqxmd.com/read/29769005/adenosine-synthetic-methods-of-its-derivatives-and-antitumor-activity
#11
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
https://www.readbyqxmd.com/read/29766803/chemistry-and-pharmacology-of-thioflavones
#12
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
https://www.readbyqxmd.com/read/29692238/advances-in-the-development-of-novel-factor-xa-inhibitors-a-patent-review
#13
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
https://www.readbyqxmd.com/read/29692247/synthesis-molecular-docking-and-dynamics-simulation-studies-of-new-7-oxycoumarin-derivatives-as-potential-antioxidant-agents
#14
Nehad Ahmed Abdel Latif, Rasha Zakaria Batran, Salwa F Mohammed, 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
https://www.readbyqxmd.com/read/29692246/an-evaluation-of-the-antioxidant-and-anticancer-properties-of-complex-compounds-of-copper-ii-platinum-ii-palladium-ii-and-ruthenium-iii-for-use-in-cancer-therapy
#15
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
https://www.readbyqxmd.com/read/29692245/new-analogues-of-aporphine-alkaloids
#16
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
https://www.readbyqxmd.com/read/29692244/inhibition-of-chlamydia-trachomatis-growth-during-the-last-decade-a-mini-review
#17
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
https://www.readbyqxmd.com/read/29692243/isatin-derivatives-and-their-antiviral-properties-against-arboviruses-a-review
#18
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
https://www.readbyqxmd.com/read/29692242/the-pharmacological-properties-and-structure-activity-relationships-of-chrysin-derivatives
#19
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
https://www.readbyqxmd.com/read/29692241/n-arylmethylideneaminophthalimide-design-synthesis-and-evaluation-as-analgesic-and-anti-inflammatory-agents
#20
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
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