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Mini Reviews in Medicinal Chemistry

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https://read.qxmd.com/read/30760188/synthesis-and-molecular-docking-of-new-thiophene-derivatives-as-lactate-dehydrogenase-a-inhibitors
#1
Abd El-Galil E Amr, Mohamed F El-Shehry, Alhussein A Ibrahim, Hanaa M Hosni, Mohamed A Al-Omar, Hazem A Ghabbour
A series of novel derivatives possessing the thiophene moiety were synthesized using ethyl 5'-amino-2,3'-bithiophene-4'-carboxylate as starting material. The new synthesized derivatives were screened as lactate dehydrogenase (LDH) inhibitors. LDH plays an important role in glucose metabolism in cancer cells and can affect tumor genesis and metastasis. 3-Substituted p-tolylthieno[2,3-d]pyrimidin-4(3H)-ones 4 were the most potent inhibitor in this study compared to Galloflavin reference drug. Molecular docking studies on Human Lactate Dehydrogenase active site was carried on the synthesized compounds and the MolDock scores are ranged between -127 to -171...
February 12, 2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30706809/molecular-understanding-of-the-cardiomodulation-in-myocardial-infarction-and-the-mechanism-of-vitamin-e-protection
#2
Khairul Anwar Zarkasi, Tan Jen-Kit, Zakiah Jubri
Myocardial infarction is a major cause of deaths globally. Modulation of several molecular mechanisms occur during the initial stages of myocardial ischemia prior to permanent cardiac tissue damage, which involve both pathogenic as well as survival pathways in the cardiomyocyte. Currently, there are increasing evidence regarding the cardioprotective role of vitamin E in alleviating the disease. This fat-soluble vitamin does not only act as a powerful antioxidant; it also has the ability to regulate several intracellular signalling pathways including HIF-1, PPAR-γ, Nrf-2, and NF-κB that influence the expression of a number of genes and their protein products...
January 30, 2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30706808/ultrasound-assisted-synthesis-of-3-het-aryl-isocoumarin-derivatives-and-their-in-vitro-pharmacological-evaluation
#3
Gutta Lakshmi Prasanna, V D Nagendra Kumar Abbaraju, Yarlagadda Bharath, Mandava V Basaveswara Rao, Manojit Pal
In view of numerous biological activities of 3-substituted isocoumarins a number of analogues based on this scaffold were synthesized for their in vitro pharmacological evaluation. Syntheses of these compounds were carried out via a Pd/C-catalyzed Suzuki-Miyaura coupling of 3-chloroisochromen-1-one with a range of boronic acid derivatives. This C-C bond forming reaction was facilitated by ultrasound irradiation to afford the desired products in good yields. A number of 3-(het)aryl isocoumarin derivatives were prepared by using this methodology and subsequently tested for their TNF-α inhibitory properties in vitro followed by cytotoxicities via the MTT assay...
January 30, 2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30686253/resveratrol-and-its-analogues-recent-advances-in-structural-modification-and-bioactivity
#4
Qing-Shan Li, Yao Li, Girdhar Singh Deora, Ban-Feng Ruan
Resveratrol is a non-flavonoid polyphenol compound containing terpenoid structure. It has been intensively studied because of its wide variety of promising biological properties, such as anticancer, antioxidant, antibacterial, neuroprotection and anti-inflammatory activities. However, the medicinal application of resveratrol is extremely constrained due to its poor bioavailability and stability. In the past decade, more attention has been focused in exploring resveratrol derivatives to improve its pharmacological activities or pharmacokinetics...
January 27, 2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30663566/phytochemical-profiles-and-antibacterial-activities-of-origanum-vulgare-and-hypericum-perforatum-and-carvacrol-and-hypericin-as-a-promising-anti-staphylococcus-aureus
#5
Mahmoud Bahmani, Morovat Taherikalani, Mojtaba Khaksarian, Setareh Soroush, Behnam Ashrafi, Rouhollah Heydari
OBJECTIVES: Staphylococcus aureus, a Gram-positive bacteria, is ranked second among the causes of hospital infections and is one of the three main causes of food poisoning. In recent times, the spread of antibiotic resistance in S. aureus has become very worrisome. Therefore, research for new effective drugs is important. The present study aims to investigate the phytochemical profiles and antibacterial effects of hydroalcoholic extracts of Origanum vulgare (Lamiaceae family) and Hypericum perforatum (Clusiaceae family) and their active compounds on S...
January 21, 2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30659537/research-progress-of-glycyrrhizic-acid-on-antiviral-activity
#6
Zhi-Gang Sun, Ting-Ting Zhao, Na Lu, Yong-An Yang, Hai-Liang Zhu
Glycyrrhizic acid (GA), a triterpene isolated from the roots and rhizomes of licorice, named Glycyrrhiza glabra, is the principal bioactive ingredient of anti-viral, anti-inflammatory and hepatoprotective effects. GA has been used in the clinical treatment of hepatitis, bronchitis, gastric ulcer, AIDS (acquired immunodeficiency syndrome), certain cancers and skin diseases. It has a direct effect on anti-HBV (hepatitis B virus) via affecting the HBsAg (hepatitis B surface antigen) to extracellular secretion, improving liver dysfunction in patients with chronic hepatitis B, and ultimately improving the immune status of HBV...
January 18, 2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30648508/chitosan-and-its-derivatives-biomaterials-with-diverse-biological-activity-for-manifold-applications
#7
Paulina Paul, Beata Kolesinska, Witold Sujka
Derived from chitin, chitosan a natural polycationic linear polysaccharide is the second the most abundant polymer next to cellulose. The main obstacle in the wide use of chitosan is its almost complete lack of solubility in water and alkaline solutions. To break this obstacles the structure of chitosan is subjected to modification, improving its physic-chemical properties and facilitating application as components of composites or hydrogels. Derivatives of chitosan are biomaterials useful for different purposes because of their lack of toxicity, low allergenicity, biocompatibility and biodegradability...
January 12, 2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30599108/design-synthesis-and-anticancer-activity-of-new-thiazole-tetrazole-or-triazole-hybrid-glycosides-targeting-cdk-2-via-structure-based-virtual-screening
#8
Asmaa F Kassem, Eman M H Abbas, Dina S El-Kady, Hanem M Awad, Wael A El-Sayed
The target tetrazole glycosides were synthesized by construction of ring system by cycloaddition reaction of benzothiazole-linked nitrile derivative and sodium azide followed by N-glycosylation process and deprotection. The triazole glycosides were resulted by applying click approach involving dipolar cycloaddition of benzothiazole possessing alkyne functionality and different glycosyl azides. The products incorporating acyclic analogs of sugar moieties were synthesized through alkylation using acyclic oxygenated halides...
December 31, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30588881/a-review-on-molecular-mechanism-of-flavonoids-as-antidiabetic-agents
#9
Jasmin, Vikas Jaitak
The development of drugs possessing anti-diabetic activities is a long pursual goal in drug discovery. It has been shown that deregulated insulin mediated signaling, oxidative stress, obesity, and β-cell dysfunction are the main factors responsible for the disease. With the advent of new and more powerful screening assays and prediction tools, the idea of a drug that can effectively treat diabetes by targeting different pathways has re-bloomed. Current anti-diabetic therapy is based on synthetic drugs that very often have side effects...
December 27, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30526457/hybrid-molecules-development-a-versatile-landscape-for-the-control-of-antifungal-drug-resistance-a-review
#10
C G Anusionwu, B A Aderibigbe, X Y Mbianda
Hybrid molecule approach of drug design has become popular due to advantages such as delayed resistance, reduced toxicity, ease of treatment of co-infection and lower cost of preclinical evaluation. Antifungal drugs currently available for the treatment of fungal diseases suffer a major side effect of drug resistance. Hybrid drugs development is one of the approaches that has been employed to control microbial resistance. Their antifungal activity is influenced by their design. This review is focused on hybrid molecules exhibiting antifungal properties to guide scientists in search of more efficient drugs for the treatment of fungal diseases...
December 10, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30526456/design-synthesis-and-therapeutic-potential-of-some-6-6-1-4-phenylene-bis-4-4-bromophenyl-pyrimidin-2-amine-analogues
#11
Sanjiv Kumar, Balasubramanian Narasimhan, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah
A library of 6, 6'-(1,4-phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine) derivatives has been synthesized by Claisen-Schmidt condensation and its chemical structure was confirmed by FT-IR, 1H/13C-NMR spectral and elemental analyses. The molecular docking study was carried to find the interaction between active bis-pyrimidine compounds with CDK-8 protein. The in vitro antimicrobial potential of the synthesized compounds was determined against Gram-positive and Gram-negative bacteria species as well fungal species by tube dilution technique...
December 10, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30484403/activation-of-ampk-by-medicinal-plants-and-natural-products-its-role-in-type-2-diabetes-mellitus
#12
Flavio Francini, Guillermo R Schinella, José-Luis Ríos
Type-2 diabetes (T2D) is a metabolic disease characterized by permanent hyperglycemia, whose development can be prevented or delayed by using therapeutic agents and implementing lifestyle changes. Some therapeutic alternatives include regulation of glycemia through modulation of different mediators and enzymes, such as AMP-activated protein kinase (AMPK), a highly relevant cellular energy sensor for metabolic homeostasis regulation, with particular relevance in the modulation of liver and muscle insulin sensitivity...
November 28, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30626312/preface
#13
George Perry
No abstract text is available yet for this article.
2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30626311/carbocyclic-analogues-of-distamycin-and-netropsin
#14
Karolina Arciszewska, Anna Pućkowska, Agnieszka Wróbel, Danuta Drozdowska
The DNA as the depository of genetic information is a natural target for chemotherapy. A lot of anticancer and antimicrobial agents derive their biological activity from their selective interaction with DNA in the minor groove and from their ability to interfere with biological processes such as enzyme catalysis, replication and transcription. The discovery of the details of minor groove binding drugs, such as netropsin and distamycin A, oligoamides built of 4-amino-1-methylpyrrole-2-carboxylic acid residues, allowed to develop various DNA sequence-reading molecules, named lexitropsins, capable of interacting with DNA precisely, strongly and with a high specificity, and at the same time exhibiting significant cytotoxic potential...
2019: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30444199/molecular-targets-anti-cancer-properties-and-potency-of-synthetic-indole-3-carbinol-derivatives
#15
Mojgan Karimabad Noroozi, Mehdi Mahmoodi, Abdolah Jafarzadeh, Ali Darekordi, Mohamad Reza Hajizadeh, Gholamhossein Hassanshahi
The indole-3-carbinol (I3C) displays anti-proliferative and anti-cancer activities against human cancer cells. Cellular proliferation is an important event associated with cancer development and continued progression. This manifest is described by altered expression and/or functions of cell cycle related proteins. The constitutive activation of many signal transduction pathways also stimulates cell growth. The immediate stages in tumor development are accompanied by a fibrogenic response and the progression of a hypoxic environment, is in favor of the survival and proliferatory functions of cancer stem cells...
November 16, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30426899/cannabis-associated-high-cardiovascular-morbidity-and-mortality-marijuana-smoke-like-tobacco-smoke-a-d%C3%A3-j%C3%A3-vu-d%C3%A3-j%C3%A3-v%C3%A3-cu-story
#16
Theodora A Manolis, Antonis A Manolis, Antonis S Manolis
BACKGROUND: Cannabis use has increased over the past several years as some countries have legalized its use for treatment of certain medical conditions and/or for recreational use. Thus, concerns have risen about potential adverse health effects. Increasing number of reports have associated cannabis use with serious cardiovascular (CV) complications. Furthermore, there appears to be a likeness in the harmful health effects, especially on the CV and respiratory systems, of cannabis smoking to those of tobacco smoking...
November 13, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30421673/halogenated-compounds-from-corals-chemical-diversity-and-biological-activities
#17
Yuanyuan Zhang, Junhong Liu, Dayong Shi, Zheng Li
As important marine biological resources, corals produce a large amount of active organic compounds in their secondary metabolic processes, including numerous brominated, chlorinated, and iodinated compounds. These compounds, with novel structures and unique activities, guide the discovery and research of important lead compounds and novel biological mechanisms. Through large numbers of literature survey, this paper summarized a total of 145 halogenated secondary metabolites which were roughly divided into four major classes of terpenes, prostaglandins, steroids and alkaloids...
November 13, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30387393/an-overview-of-synthesis-of-indole-alkaloids-and-biological-activities-of-secondary-metabolites-isolated-from-hyrtios-species
#18
S Kannadasan, K R Ethiraj
This review article is focused on the importance of marine sponges in pharmaceutical field by explaining the possible biological activities exhibited by the secondary metabolites, which were extracted from, one of the important class of marines sponges, Hyrtios sp. Marine sponges are the source for more than 50% of marine natural compounds have been isolated from marine organisms. Also, the review dealt with some of the reported synthetic routes to the indole alkaloids which are extracted from the marine sponge Hyrtios sp...
November 2, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30387392/drug-design-of-inhibitors-of-alzheimer-s-disease-ad-pom-and-dft-analyses-of-cholinesterase-inhibitory-activity-of-%C3%AE-amino-di-carbonyl-derivatives
#19
Taibi Ben Hadda, Abdur Rauf, Hsaine Zgou, Fatma Sezer Senol, Ilkay Erdogan Orhan, Yahia Nasser Mabkhot, Ismail I Althagafi, Thoraya A Farghaly
BACKGROUND: Since deficit of acetylcholine has been evidenced in the patients of Alzheimer's disease (AD), cholinesterase inhibitors are currently the most prescribed drug class for the treatment of AD. RESULTS: In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 µg/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity...
November 1, 2018: Mini Reviews in Medicinal Chemistry
https://read.qxmd.com/read/30370847/lemon-juice-mediated-reaction-under-ultrasound-irradiation-synthesis-of-indolofuroquinoxalines-as-potential-anticancer-agents
#20
Gutta Lakshmi Prasanna, Bodapati Veera Durga Rao, Alugubelli Gopi Reddy, Mandava V Basaveswara Rao, Manojit Pal
A non-hazardous synthetic methodology has been developed for the preparation of compounds based on indolofuroquinoxaline framework. The lemon juice that is known to play the role of a biocatalyst in various organic reactions was used for this purpose. A number of indolofuroquinoxaline derivatives were prepared via the lemon juice mediated condensation of methyl 2-(2-chloro-1H-indol-3-yl)-2-oxoacetate or its N-alkyl derivatives with 1,2-diamines under ultrasound irradiation. All the synthesized compounds were screened via an MTT assay for their potential anticancer properties in vitro using a number of cancerous cell lines including MDA-MB 231, and MCF7, K562, Colo-205 and IMR-32 and the non-cancerous HEK293 cell line...
October 28, 2018: Mini Reviews in Medicinal Chemistry
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