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Mini Reviews in Medicinal Chemistry

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
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
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
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
Amro Soliman, Seong Lin Teoh, Norzana Ghafar, Srijit Das
The incidence of diabetes mellitus (DM) is increasing worldwide. One of the main complications in DM is delayed wound healing which often requires amputation. Various drugs have been used to treat DM but they present with various complications and patients often do not comply with such treatment. This opens the door for complementary and alternative medicine. In the present review, we explore the molecular concept of wound healing occurring in different stages with special emphasis to DM. We also highlight potential herbal products such as NF3 (Chinese 2-Herb Formula), Zicao, Jing Wan Hong ointment, mixture of Adiantum capillus-veneris, Commiphora molmol, Aloe Vera, and henna, Aleo vera, Phenol-rich compound sweet gel, Jinchuang ointment, San-huang-sheng-fu (S) oil, Yi Bu A Jie extract, Astragali Radix (AR) and Rehmanniae Radix (RR), Yiqi Huayu, Tangzu yuyang ointment, Shengji Huayu recipe, Angelica sinensis, Lithospermun erythrorhison, Hippophae rhamnoides L...
October 25, 2018: Mini Reviews in Medicinal Chemistry
Lucia Pacifico, John F Osborn, Enea Bonci, Pasquale Pierimarchi, Claudio Chiesa
Nonalcoholic fatty liver disease (NAFLD), historically considered as the hepatic component of the metabolic syndrome, is a spectrum of fat-associated liver conditions in the absence of secondary causes that may progress to nonalcoholic steatohepatitis (NASH), fibrosis, and cirrhosis. Disease progression is closely associated with body weight or fatness, dyslipidemia, insulin resistance, oxidative stress, and inflammation. Recently, there has been a significant scientific interest into the relationship between vitamin D status and NAFLD...
October 25, 2018: Mini Reviews in Medicinal Chemistry
Li Wang, Min Yao, Wenjie Zheng, Miao Fang, Mengna Wu, Jianying Sun, Zhizhen Dong, Dengfu Yao
Human insulin-like growth factor (IGF) axis affects the molecular pathogenesis of hepatocellular carcinoma (HCC), especially in the abnormality of hepatic IGF-I receptor (IGF-IR) or IGF-II expression as key molecule in hepatocarcinogenesis. However, the over-expression of hepatic IGF-IR is associated with HCC progression with largely unknown mechanisms. Recently, the IGF-IR as one key molecule of the IGF signal pathway plays an important role in hepatocyte malignant transformation. Attaching importance to IGF-IR might improve the prognostic or therapeutic technique of HCC...
October 25, 2018: Mini Reviews in Medicinal Chemistry
Fathy M Abdelrazek, Sobhi M Gomha, Mohamed E B Shaaban, Kamal A Rabee, Heba N El-Shemy, Abanoub M Abdallah, Peter Metz
A novel series of 2-thiazolyl pyridines was prepared in a one-pot three-component reaction using 2-bromoacetyl pyridine as a starting precursor. The structure of all products was established on the bases of spectral data and elemental analyses and alternative synthesis if possible. The prepared compounds were screened for their in vitro antimicrobial activity and some derivatives showed promising activity. Molecular docking studies were carried out for the two synthesized compounds (4a and 4b) which exhibited the best activities against most of the tested microorganisms by using default parameters with MOE software...
October 19, 2018: Mini Reviews in Medicinal Chemistry
Nisha Chokkar, Sourav Kalra, Monika Chauhan, Raj Kumar
After restricting the proliferation of CD4+T cells, Human Immunodeficiency Virus (HIV) infection persists at a very fast rate causing Acquired Immunodeficiency Syndrome (AIDS). This demands the vigorous need of suitable anti-HIV agents, as existing medicines do not provide complete cure and exhibit drawbacks like toxicities, drug resistance, side-effects, etc. Even the introduction of Highly Active Antiretroviral Therapy (HAART) failed to combat HIV/AIDS completely. The major breakthrough in anti-HIV discovery is marked with the discovery of raltegravir in 2007, the first integrase (IN) inhibitor...
October 18, 2018: Mini Reviews in Medicinal Chemistry
Shadia A Elsayed, Entsar A Saad, Sahar I Mostafa
BACKGROUND: Due to the bad side effects of clinically approved anticancer drugs there is a great need to explore and develop new metal-based anticancer drug molecules of high efficiency with less or no side effects. OBJECTIVE: To synthesize new metal complexes of 2-hydrazinobenzothiazole (hbt) and to investigate their potential anticancer characteristics. METHOD: New five complexes; [VO(hbt)2SO4].4H2O (1), [Ru(hbt)2Cl3(H2O)] (2), [M(hbt)2Cl2] [M(II) = Pd (3), Pt (4)] and [Ag(hbt)2]...
October 17, 2018: Mini Reviews in Medicinal Chemistry
Vivek Kumar Singh, Mohane Selvaraj Coumar
Chronic myeloid leukemia (CML) is a myeloproliferative disease caused due to translocation between chromosome 9 and 22 leading to chimeric gene product known as Bcr-Abl. Bcr-Abl fusion protein has constitutively activated Abl tyrosine kinase activity which is responsible for the uncontrolled proliferation in CML The tyrosine kinase inhibitors (TKIs) such as Imatinib, Dasatinib, and Nilotinib are the current firstline treatments approved by the United States Food and Drug Administration (US FDA) for the treatment of the disease...
October 17, 2018: Mini Reviews in Medicinal Chemistry
Hamdi M Hassaneen, Fatma M Saleh, Tayseer A Abdallah, Magda F Mohamed, Yasmin Sh Mohamed, Enas M Awad, Ismail A Abdelhamid
Isobutyrohydrazonoyl bromide 1 was used as precursor for the synthesis of 4-imino-3-isopropyl-1-(4-nitrophenyl)-1,4-dihydro-5H-pyrazolo[3,4-d]pyrimidin-5-amine 4, which was converted to hydrazino derivative 5 by heating with hydrazine hydrate at reflux. Hydrazino as well as imino and amino derivatives undergo condensation and cyclization reactions to give pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[3,4-c]pyrimidine derivatives, respectively. Antimicrobial studies are performed using two-gram positive bacteria and two-gram negative bacteria...
October 17, 2018: Mini Reviews in Medicinal Chemistry
Yanling Zhao, Haotian Li, Shizhang Wei, Xuelin Zhou, Xiaohe Xiao
Infectious diseases caused by pathogenic bacteria seriously threaten human lives. Although antibiotic therapy is effective in the treatment of bacterial infections, the overuse of antibiotics has leaded to an increased risk of antibiotic resistance, putting forward urgent requirements for novel antibacterial drugs. Traditional Chinese herbal medicine (TCHM) and its constituents are considered to be potential sources of new antimicrobial agents. Currently, a series of chemical compounds purified from TCHM have been reported to fight against infections by drug-resistant bacteria...
October 17, 2018: Mini Reviews in Medicinal Chemistry
Armin Khomami, Mohammadamin Rahimi, Arash Tabei, Parastoo Saniee, Arash Mahboubi, Alireza Foroumadi, Nasrin Nassiri Koopaei, Ali Almasirad
BACKGROUND: Bacterial resistance to the available antibiotics is a life threatening issue and researchers are trying to find new drugs to overcome this problem. Amongst the different structural classes, thiazolidinone-4-one as a new effective pharmacophore against various bacteria has been introduced. OBJECTIVE: A new series of 2-(5-(5-nitrothiophene-2-yl)-1,3,4-thiadiazole-2-ylimino)-5-arylidenethiazolidin-4-one derivatives were designed and synthesized as new antibacterial agents...
October 17, 2018: Mini Reviews in Medicinal Chemistry
Ali Mohd Ganie, Ayaz Mahmood Dar, Fairooz Ahmad Khan, Bashir Ahmad Dar
Here in we report the number of strategies for the synthesis of differently substituted benzimidazole derivatives. The protocols involved in the syntheses of these derivatives were one-pot or multi-component. The characterization studies of these derivatives were carried by using different spectroscopic techniques (1H NMR, 13C NMR and MS) and elemental analyses. The biological screening studies revealed that these benzimidazole derivatives show potential antibacterial as well as antifungal behavior. These benzimidazole derivatives not only depicted potential antiulcer properties but also showed moderate to good anticancer/cytotoxic behavior against different cancer cell lines...
October 16, 2018: Mini Reviews in Medicinal Chemistry
Emiliya Nosova, Galina Lipunova, Valery Charushin, Oleg Chupakhin
Cyclocondensations based on 2-chlorobenzoamides or 2-halogenobenzoyl isothiocyanates appear to be effective synthetic approaches to 2-cycloalkylimino-substituted 1,3-benzothiazin-4-ones. Some 2-amino- or 2-heteryl-derivatives of 1,3-benzothiazin-4-one are accessible through transformations of 2-mercaptobenzoic acids or 2-chloro-1,3-benzothiazin-4-ones. Synthetic ways to wide range of fluorinated 1,3-benzothiazin-4-ones are summarized. 2-Piperazinyl- and 2-piperidinyl-1,3-benzothiazin-4-ones proved to be promising agents for treatment of tuberculosis, whereas 2-azinyl substituted 1,3-benzothiazin-4-ones have been found to activate antioxidant response of element-mediated gene expression; also these compounds are able to suppress oxidative stress-induced cardiomyocyte apoptosis...
October 15, 2018: Mini Reviews in Medicinal Chemistry
Maobin Xie, Man Xu, Xiaomig Chen, Yi Li
Clinical applications of natural active ingredient (NAI) are limited by their instability and poor water solubility, while micronization is one strategy to overcome these drawbacks. Supercritical carbon dioxide (sc-CO2) based nano techniques have drawn great attention in nanomedicinal area for many years, due to their unique characters such as fast mass transfer, near zero surface tension and effective solvents elimination. In terms of functions of sc-CO2, many modified sc-CO2 based techniques are developed to produce NAI nanoparticles...
October 15, 2018: Mini Reviews in Medicinal Chemistry
Seyithan Taysi, Ayse Saglam Tascan, Mete Gurol Uuro, Mustafa Demir
Oxygen is used by eukaryotic cells for metabolic transformations and energy production in mitochondria. Under physiological conditions, there is a constant endogenous production of free radicals that interact as signaling molecules in physiological mechanisms. Free radicals are neutral molecules, which are produced by separation of ions and molecules. In regular conditions production and disposal of free radicals are at equilibrium. However this equilibrium may not always be experienced, where these species are not eliminated by antioxidants or are excessively produced...
October 15, 2018: Mini Reviews in Medicinal Chemistry
Kelly Lynn Summers
Malaria is a potentially life-threatening disease, affecting approx. 214 million people world-wide. Malaria is caused by protozoan, Plasmodium falciparum, which is transmitted through the Anopheles mosquito. Malaria treatment is becoming more challenging due to rising resistance against the antimalarial drug, chloroquine. Novel compounds that target aspects of parasite development are being explored in attempts to overcome this wide-spread problem. Anti-malarial drugs target specific aspects of parasite growth and development within the human host...
October 15, 2018: Mini Reviews in Medicinal Chemistry
Garima Verma, Mohemmed Faraz Khan, Wasim Akhtar, Mohammad Mumtaz Alam, Mymoona Akhter, Mohammad Shaquiquzzaman
1,3,4-Oxadiazole ring is an important five-membered aromatic heterocycle widely present in a number of synthetic molecules. The unique structural feature of 1,3,4-oxadiazole ring with pyridine type of nitrogen atom is beneficial for 1,3,4-oxadiazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of 1,3,4-oxadiazole-based medicinal chemistry have become a rapidly developing and increasingly active topic...
October 15, 2018: Mini Reviews in Medicinal Chemistry
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