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Medicinal Chemistry

Cigdem Karaaslan, Yalcin Duydu, Aylin Ustundag, Can Ozgur Yalcin, Banu Kaskatepe, Hakan Goker
A series of new 2-(3,4-dimethoxyphenyl)-1H-benz(or pyrido)imidazoles 2, 4-25 were synthesized and evaluated for their anticancer and antimicrobial activities. The NMR assignments of the dimethoxy groups were established by the NOESY spectra. Compound 12 bearing two chlorine atoms at the 5(4) and 7(6) positions of the benzene moiety of benzimidazole was found the most potent analogue, against A549 cells with the GI50 value of 1.5 µg/mL. Moreover, compound 24 showed remarkable cell growth inhibition against MCF-7 and HeLa cells with the GI50 values of 7 and 5...
July 11, 2018: Medicinal Chemistry
Katharigatta N Venugopala, Sandeep Chandrashekharappa, Melendhran Pillay, Subhrajyoti Bhandary, Mahmoud Kandeel, Fawzi M Mahomoodally, Mohamed A Morsy, Deepak Chopra, Bandar E Aldhubiab, Mahesh Attimarad, Osama I Alwassil, Sree Harsha, Koleka Mlisana
BACKGROUND: Benzothiazole derivatives are known for anti-TB properties. Based on the known antiTB benzothiazole pharmacophore, in the present study, we described the synthesis, structural elucidation, and anti-tubercular screening of a series of novel benzothiazole (BNTZ) derivatives (BNTZ 1-7 and BNTZ 8-13). OBJECTIVE: Development of benzothiazole based anti-TB compounds. METHODS: Title compounds are synthesized by microwave method and purified by column chromatography...
July 3, 2018: Medicinal Chemistry
Gopiraja Geethaavacini, Go Poh Poh, Lim Yi Yan, Rajindran Deepashini, Sivadasan Shalini, Rajak Harish, Krishnan Sureshkumar, Veerasamy Ravichandran
BACKGROUND: The development of severe drug resistance caused by the extensive use of anti-HIV agents have resulted in greatly extensive reduction in these drugs efficacy. OBJECTIVES: To identify the important pharmacophoric features and correlate 3Dchemical structure of benzothiazinimines with their anti-HIV potential using 2D, 3D-QSAR and pharmacophore modeling studies. METHODS: QSAR and pharmacophore mapping studies have been used to relate structural features...
May 28, 2018: Medicinal Chemistry
Do Thi Mai Dung, Nguyen Van Huan, Do Manh Cam, Dao Cam Hieu, Pham-The Hai, Le-Thi-Thu Huong, Jisung Kim, Jeong Eun Choi, Jong Soon Kang, Sang-Bae Han, Nguyen-Hai Nam
BACKGROUND: Histone deacetylases (HDAC) enzymes are emerging as potential targets for cancer treatments. In this study several series of novel hydroxamic acids incorporating 1-((1H-1,2,3-triazol-4-yl)methyl)-3-substituted-2-oxoindolines was explored. METHODS: The compounds were designed using Autodock Vina program, then synthesized and evaluated in vitro and in silico for their inhibitory activity against HDACs. The cytotoxicity was measured by SRB method. The enzyme inhibitory effects of the compounds were evaluated by fluorescent assay...
May 27, 2018: Medicinal Chemistry
Zahra Heydari, Maryam Mohammadi-Khanaposhtani, Somaye Imanparast, Mohammad Ali Faramarzi, Mohammad Mahdavi, Parviz Rashidi Ranjbar, Bagher Larijani
BACKGROUND: Pyrano[3,2-c]quinoline derivatives 6a-n were synthesized via simple two-step reactions and evaluated for their in vitro α-glucosidase inhibitory activity. METHODS: Pyrano[3,2-c]quinoline derivatives 6a-n derivatives were prepared from a two-step reaction: cycloaddition reaction between 1-naphthyl amine 1 and malonic acid 2 to obtain benzo[h]quinoline-2(1H)-one 3 and reaction of 3 with aryl aldehydes 4 and Meldrum's acid 5. The anti- α-glucosidase activity and kinetic study of the synthesized compounds were evaluated using α-glucosidase from Saccharomyces cerevisiae and p-nitrophenyl-a-D-glucopyranoside as substrate...
May 27, 2018: Medicinal Chemistry
Fady N Akladios, Scott D Andrew, Samantha J Boog, Carmen de Kock, Richard K Haynes, Christopher J Parkinson
Bis-thiosemicarbazones containing a central pyridyl core display potent antimalarial activity in vitro. The absence of the pyridyl core results in inactive compounds. It is likely that metal ion sequestration and subsequent reactive oxygen generation plays a role in the antimalarial activity of the series, the redox activity of the iron complexes of bis-thiosemicarbazones paralleling antimalarial activity. The activity of this series compares favourably to that of previously reported iron sequestering compounds...
May 25, 2018: Medicinal Chemistry
Shabnam Farzaneh, Soraya Shahhosseini, Hadi Arefi, Bahram Daraei, Marjan Esfahanizadeh, Afshin Zarghi
BACKGROUND: Prostaglandins are a family of eicosanoids biosynthesized from arachidonic acid through cyclooxygenase (COX) pathway. Two isoforms of COX are well established: COX-1, COX-2. Evidence supports the notion that cyclooxygenase-2, plays a crucial role in some pathological conditions such as inflammation and cancer. OBJECTIVE: A new group of 1,3-diphenyl-3-(phenylamino)propan-1-ones was designed and synthesized to investigate for their COX-2 inhibitory activity and inhibition of platelet aggregation...
May 25, 2018: Medicinal Chemistry
Sarosh Iqbal, Nimra Naveed Shaikh, Khalid Mohammed Khan, Sehrish Naz, Zaheer-Ul-Haq Qasmi, Shahnaz Perveen, M Iqbal Choudhary
BACKGROUND: Glucuronidation is essential for the metabolism and excretion of toxic substances. β-Glucuronidase enzyme slows down the process of glucuronidation, and thus plays an important role in the on-set of colorectal carcinoma, and many other diseases. Inhibition of β-glucuronidase activity is thus identified as an important approach for the treatment of related diseases. OBJECTIVE: Current study was aimed to synthesize a library of 2-oxo-1,2,3,4-tetrahydropyrimidine and to evaluate their of β-glucuronidase inhibitory activity, as well as to investigate their mode of enzyme inhibition...
May 24, 2018: Medicinal Chemistry
Carolina Campos-Rodriguez, Jose G Trujillo-Ferrara, Ameyali Alvarez-Guerra, Iran M Cumbres Vargas, Roberto I Cuevas-Hernandez, Erik Andrade-Jorge, Sergio Zamudio, Eduardo Ramirez-San Juan
BACKGROUND: Thalidomide, the first synthesized phthalimide, has demonstrated sedative-hypnotic and antiepileptic effects on the central nervous system. N-substituted phthalimides have an interesting chemical structure that confers important biological properties. OBJECTIVE: Non-chiral (ortho and para bis-isoindoline-1,3-dione, phthaloylglycine) and chiral phthalimides (N-substituted with aspartate or glutamate) were synthesized and the sedative, anxiolytic and anticonvulsant effects were tested...
May 24, 2018: Medicinal Chemistry
Maheshkumar R Borkar, Santosh Nandan, M N Harish Kumar, Jayashree Puttur, M Jisha, Dipankar Chatterji, Evans C Coutinho
BACKGROUND: The treatment of a bacterial infection when the bacterium is growing in a biofilm is a vexed issue. This is because the bacteria in a biofilm behaves differently compared to the individual planktonic free-form. As a result, traditional antibacterial agents lose their activity. OBJECTIVE: Presently, there are not many drugs that are effective against bacteria growing in biofilms. Based on literature reports, we have sought to develop novel derivatives of 4-hydroxy-2-pyridone as both antimycobacterial and antibiofilm agents...
May 24, 2018: Medicinal Chemistry
Carolina S Bortolot, Luana da S M Forezi, Roberta K F Marra, Marcelo I P Reis, Barbara V F E Sa, Ricardo Imbroisi Filho, Zeinab Ghasemishahrestani, Mauro Sola-Penna, Patricia Zancan, Vitor F Ferreira, Fernando de C da Silva
BACKGROUND: Low molecular weight 1,2,3-triazoles and naphthoquinones are endowed with various types of biological activity, such as against cancer, HIV and bacteria. However, in some cases, the conjugation of these two nuclei considerably increases their biological activities Objective: In this work, we decided to study the synthesis and screening of bis-naphthoquinones and xanthenes tethered to 1,2,3-triazoles against cancer cell lines, specifically the human breast cancer cell line MCF-7...
May 23, 2018: Medicinal Chemistry
Burcu Kilic, Merve Erdogan, Hayrettin O Gulcan, Fatma Aksakal, Nihan Oruklu, E Umit Bagriacik, Deniz S Dogruer
Backround: With respect to the increase in the average life expectancy, Alzheimer Disease (AD), the most common form of age-related dementia, has become a major threat to the population over the age of 65 during the past several decades. The majority of AD treatments are focused on cholinergic and amyloid hypotheses. OBJECTIVE: In this study, three series of diphenyl-2-(2-(4-substitutedpiperazin-1-yl)ethyl)pyridazin-3(2H)-one derivatives were designed, synthesized and investigated for their ability to inhibit both cholinesterase enzymes and amyloid-β aggregation...
May 23, 2018: Medicinal Chemistry
Vikrant Patil, Siddappa A Patil, Renukadevi Patil, Alejandro Bugarin, Kenneth Beaman, Shivaputra A Patil
BACKGROUND: Search for new antiviral and anticancer agents are essential because of the emergence of drug resistance in recent years. In continuation of our efforts in identifying the new small molecule antiviral and anticancer agents, we identified chalcones as potent antiviral and anticancer agents. OBJECTIVE: With the aim of identifying the broad acting antiviral and anticancer agents, we discovered substituted aryl/heteroaryl derived thienyl chalcones as antiviral and anticancer agents...
May 23, 2018: Medicinal Chemistry
Janaina M de Avila, Ionara I Dalcol, Alessandra O Pereira, Eveline W Santos, Adriano Ferraz, Maura Z Santos, Marco Aurelio Mostardeiro, Ademir F Morel
BACKGROUND: Several species of the genus Erythrina have been used as sedative, antidepressant, and anticonvulsant. Erythrina crista-galli is native to the Pampa Biome and is widely used for medicinal purposes. Erythrinan alkaloids exhibit a range of pharmacological properties. OBJECTIVE: The aim of this study was to evaluate the basic fractions and the alkaloids isolated from E. crista-galli bark against a collection of bacteria and fungi for the first time. METHODS: Erythrina crista-galli stem bark was extracted with MeOH under reflux...
May 23, 2018: Medicinal Chemistry
Qi Huang, Qiong Liu, Dongsheng Ouyang
BACKGROUND: Aldose reductase (AR) is involved in pathogenesis of diabetes, which is one of the major threats to global public health. OBJECTIVE: In this review article, we have discussed the role of sorbinil, an AR inhibitor (ARI), in preventing diabetic complications. RESULTS: AR contributes in diabetes by generating excess intracellular superoxide and other mediators of oxidative stress through polyol pathway. Inhibition of AR activity thus might be potential approach for the management of diabetic complications...
May 23, 2018: Medicinal Chemistry
Elda Meta, Chiara Brullo, Michele Tonelli, Scott G Franzblau, Yuehong Wang, Rui Ma, Wan Baojie, Beatrice Silvia Orena, Maria Rosalia Pasca, Olga Bruno
BACKGROUND: We screened a large library of differently decorated imidazo-pyrazole and pyrazole derivatives as possible new antitubercular agents and this preliminary screening showed that many compounds are able to totally inhibit Mycobacterium growth (>90 %). Among the most active compounds, we selected some new possible hits based on their similarities and, at the same time, their novelty respect to the pipeline drugs. METHODS: In order to increase the potency and obtain more information about structure activity relationship (SAR), we design and synthesized three new series of compounds (2a-e, 3a-e, and 4a-l)...
May 23, 2018: Medicinal Chemistry
Arturo Coaviche-Yoval, Hector Luna, Ricardo Tovar-Miranda, Marvin Antonio Soriano-Ursua, Jose G Trujillo-Ferrara
BACKGROUND: Benzofurans are heterocyclic compounds with neurotropic activity. Some have been developed for the treatment of acute and degenerative neuronal injuries. OBJECTIVE: To evaluate the in silico binding of some promising benzofurans on the GABA receptors, and the in vivo neurotropic activity of benzofuran analogues (BZF 6-10) of gamma-aminobutyric acid (GABA) on a seizure model. METHODS: The ligands with the best physicochemical attributes were docked on two GABA receptors (the alpha-1 subunit of GABAA-R and GBR1 subunit of GABAB-R)...
May 23, 2018: Medicinal Chemistry
Fangrui Wu, Gang Cheng, Yuan Yao, Mari Kogiso, Hong Jiang, Xiao-Nan Li, Yongcheng Song
BACKGROUND: R132H mutation of isocitrate dehydrogenase 1 (IDH1) are found in ~75% of low-grade gliomas and secondary glioblastomas as well as in several other types of cancer. More chemotypes of inhibitors of IDH1(R132H) are therefore needed. OBJECTIVE: To develop a new class of IDH1(R132H) inhibitors as potent antitumor agents. METHOD: A biochemical assay was developed to find inhibitors of IDH1(R132H) mutant enzyme. Chemical synthesis and structure activity relationship studies were used to find compounds with improved potency...
May 23, 2018: Medicinal Chemistry
B S Rahul, Bindu Saraswati, C Shiju, Gopal Gupta, Nand Lal
BACKGROUND: In our previous work, several piperazine derived bis(dialkylaminethiocarbonyl) disulfides and disulfide esters of dithiocarbamic acid have been synthesized and evaluated for their spermicidal and microbicidal efficacy. These studies have provided some promising compounds for developing a dually active vaginal microbicidal contraceptive which are under pre-clinical stage [1, 16, 17]. OBJECTIVE: The main objective of this study was to design, synthesis and biological evaluation of bis(dialkylaminethiocarbonyl) disulfides (4-15) and 2,2'-disulfanediylbis (3-(substituted- 1-yl) propane-2,1-diyl) disubstituted-1-carbodithioates (19-28) as non-surfactant molecules capable of eliminating Trichomonas vaginalis as as well as irreversibly immobilizing 100% human sperm promptly...
May 23, 2018: Medicinal Chemistry
Malik Shoaib Ahmad, Saima Rasheed, Sven Falke, Binish Khaliq, Markus Perbandt, M Iqbal Choudhary, Wojciech T Markiewicz, Jan Barciszewski, Christian Betzel
BACKGROUND: Viscum album (the European mistletoe) is a semi-parasitic plant, which is of high medical interest. It is widely found in Europe, Asia and North America. It contains at least three distinct lectins (i.e. ML-I, II, and III), varying in molecular mass and specificity. Among them ML-I is in focus of medical research for various activities, including anti-cancer activities. To understand the molecular basis for such medical applications a few studies have already addressed the structural and functional analysis of ML-I in complex with ligands...
May 23, 2018: Medicinal Chemistry
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