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Medicinal Chemistry Research

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https://www.readbyqxmd.com/read/30319238/phytochemical-study-of-piliostigma-thonningii-a-medicinal-plant-grown-in-nigeria
#1
Michael Afolayan, Radhakrishnan Srivedavyasasri, Olayinka T Asekun, Oluwole B Familoni, Abayomi Orishadipe, Fazila Zulfiqar, Mohamed A Ibrahim, Samir A Ross
Piliostigma thonningii (Schumach.) Milne-Redhead. (Leguminosae) is used for various medicinal purposes in African countries. Phytochemical investigation of P. thonningii yielded two compounds newly isolated from natural sources, 2 β -methoxyclovan-9 α -ol ( 1 ), and methyl- ent -3 β -hydroxylabd-8(17)-en-15-oate ( 2 ), along with 14 known compounds ( 3 - 16 ). Compounds 1 and 4 (alepterolic acid) showed potential selectivity towards Trypanosoma brucei brucei with IC50 7.89 and 3.42 μM, respectively. Compound 2 showed activity towards T...
October 2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29937677/dual-targeting-agents-for-a%C3%AE-plaque-p-glycoprotein-and-a%C3%AE-plaque-nicotinic-acetylcholine-%C3%AE-4%C3%AE-2-receptors-potential-approaches-to-facilitate-a%C3%AE-plaque-removal-in-alzheimer-s-disease-brain
#2
Gurleen K Samra, Kenneth Dang, Heather Ho, Aparna Baranwal, Jogeshwar Mukherjee
Alzheimer's disease (AD) affects 10% of people older than 65 and is characterized by a progressive loss of cognitive function with an abnormal accumulation of amyloid β (Aβ ) plaques and neurofibrillary tangles (NFT) in the brain. Efforts to reduce brain Aβ plaques continue to be investigated as a therapeutic approach for AD. We report here development of dual targeting agents with affinity for Aβ plaque/P-glycoprotein (Pgp) and Aβ plaque/α4β 2* nicotinic acetylcholine receptors (nAChR). These novel dual agents may be able to efflux Aβ plaques via the paravascular (glymphatic) pathways...
June 2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/30374214/evaluation-of-triazole-and-isoxazole-derivatives-as-potential-anti-infective-agents
#3
Amer H Tarawneh, Lo Ay A Al-Momani, Francisco León, Surenda K Jain, Anastassiya V Gadetskaya, Sultan T Abu-Orabi, Babu L Tekwani, Stephen J Cutler
A series of isoxazole and triazole derivatives, with interesting bioactive scaffolds, were examined for their in vitro antibacterial, antifungal, and antiprotozoal activities. These compounds exhibited antitrypanosomal activity comparable to difluoromethylornithine (DMFO), a drug used in the treatment of human African trypanosomiasis. Isoxazole analogues 1 , 3 and 4 , and triazole derivatives 16 , 17 , 28 , 37 , 40 and 42 showed the highest antitrypanosomal activity with IC50 values of 17.89, 1.82, 10.38, 10...
April 2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/30294193/activity-evaluation-of-some-psychoactive-drugs-with-the-application-of-qsar-qspr-modeling-methods
#4
Piotr Kawczak, Leszek Bober, Tomasz Bączek
A set of psychoactive drugs has been analyzed with the use of quantitative structure-activity/property relationships methods. The purpose of this study was to demonstrate both the common and differentiating characteristics of the above-mentioned chemical compounds, physicochemical as well as pharmacological based on the quantum chemical calculations and selected biological activity data and chromatographic retention parameters. During the study, the ab initio model of molecular modeling was performed and PCA, FA, and MLR as the types of chemometric approach...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/30220832/evaluation-of-the-effect-of-2-2-4-dihydroxyphenyl-4-h-benzofuro-3-2-d-1-3-thiazin-4-one-on-colon-cells-and-its-anticancer-potential
#5
Arkadiusz Czerwonka, Marta K Lemieszek, Monika Karpińska, Joanna Matysiak, Andrzej Niewiadomy, Wojciech Rzeski
In this paper, we present the biological effect of the newly synthesized 2-(2,4-dihydroxyphenyl)-4 H -benzofuro[3,2- d ][1,3]thiazin-4-one (DPBT) on human colon adenocarcinoma cell lines (HT-29 and LS180). Additionally, DPBT cytotoxicity was examined in human colon epithelial cells (CCD 841 CoTr) and human skin fibroblasts (HSF). The studies revealed a significant decrease in the proliferation of cancer cells after exposure to DPBT at concentrations in the range of 10-100 µM. Additionally, DPBT was not toxic to normal CCD 841 CoTr and HSF cells at concentrations that induced inhibition of cancer cell proliferation...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/30220831/thiazoles-with-cyclopropyl-fragment-as-antifungal-anticonvulsant-and-anti-toxoplasma-gondii-agents-synthesis-toxicity-evaluation-and-molecular-docking-study
#6
Krzysztof Z Łączkowski, Natalia Konklewska, Anna Biernasiuk, Anna Malm, Kinga Sałat, Anna Furgała, Katarzyna Dzitko, Adrian Bekier, Angelika Baranowska-Łączkowska, Agata Paneth
Synthesis and investigation of antifungal, anticonvulsant and anti- Toxoplasma gondii activities of ten novel (2-(cyclopropylmethylidene)hydrazinyl)thiazole 3a - 3j are presented. Among the derivatives, compounds 3a - 3d and 3f - 3j possess very high activity against Candida spp. ATCC with MIC = 0.015-7.81 µg/ml. Compounds 3a - 3d and 3f - 3j possess also very high activity towards most of strains of Candida spp. isolated from clinical materials with MIC = 0.015-7.81 µg/ml. The activity of these compounds is similar and even higher than the activity of nystatin used as positive control...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/30220830/novel-triazoles-of-3-acetylbetulin-and-betulone-as-anticancer-agents
#7
REVIEW
Ewa Bębenek, Monika Kadela-Tomanek, Elwira Chrobak, Małgorzata Latocha, Stanisław Boryczka
The CuAAC reaction of azides and acetylenic triterpenes was used for synthesis of new triazoles of 3-acetylbetulin and betulone. The triazole derivatives were evaluated for their anticancer activity in vitro against amelanotic melanoma C-32, ductal carcinoma T47D and glioblastoma SNB-19 cell lines. 28-[1-(3'-Deoxythymidine-5'-yl)-1 H -1,2,3-triazol-4-yl]carbonylbetulone 6e exhibited a significant IC50 value (0.17 µM) against the human glioblastoma SNB-19 cell line, an almost 5-fold higher potency while compared with reference cisplatin...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/30100693/synthesis-and-biological-investigations-of-3%C3%AE-aminotropane-arylamide-derivatives-with-atypical-antipsychotic-profile
#8
Jacek Stefanowicz, Tomasz Słowiński, Martyna Z Wróbel, Grzegorz Ślifirski, Maciej Dawidowski, Zdzisława Stefanowicz, Magdalena Jastrzębska-Więsek, Anna Partyka, Anna Wesołowska, Jadwiga Turło
This work is a continuation of our previous research, concentrating this time on lead structure modification to increase the 5-HT1A receptor affinity and water solubility of designed compounds. Therefore, the compounds synthesised within the present project included structural analogues of 3β-acylamine derivatives of tropane with the introduction of a methyl substituent in the benzyl ring and a 2-quinoline, 3-quinoline, or 6-quinoline moiety. A series of novel 3β - aminotropane derivatives was evaluated for their affinity for 5-HT1A , 5-HT2A , and D2 receptors, which allowed for the identification of compounds 12e , 12i , and 19a as ligands with highest affinity for the tested receptors; they were then subjected to further evaluation in preliminary in vivo studies...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29706750/synthesis-and-anticancer-activity-of-multisubstituted-purines-and-xanthines-with-one-or-two-propynylthio-and-aminobutynylthio-groups
#9
Alicja Kowalska, Krystian Pluta, Małgorzata Latocha
A synthesis of new 2,6-disubstituted and 2,6,8-trisubstituted 7-methylpurines as well as 8-substituted 3,7-dimethylxanthines containing a triple bond chain have been worked out. Purinethiones and xanthinethiones were converted into propynylthio derivatives, which were then further transformed via a Mannich reaction into aminobutynylthio derivatives (amine = pyrrolidine, piperidine, morpholine, and diethylamine). The products thus obtained represent various types of the purine and xanthine structure: 8-mono-, 2,6- and 6,8-dipropynylthio, 6- and 8-monoaminobutynylthio, 2,6- and 6,8-diaminobutynylthio derivatives...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29576721/comparative-molecular-field-analysis-and-molecular-dynamics-studies-of-the-dopamine-d-2-receptor-antagonists-without-a-protonatable-nitrogen-atom
#10
Agnieszka A Kaczor, Justyna Żuk, Dariusz Matosiuk
The dopaminergic hypothesis of schizophrenia is the main concept explaining the direct reasons of schizophrenia and the effectiveness of current antipsychotics. All antipsychotics present on the market are potent dopamine D2 receptor antagonists or partial agonists. In this work we investigate a series of dopamine D2 receptor antagonists which do not fulfill the criteria of the classical pharmacophore model as they do not possess a protonatable nitrogen atom necessary to interact with the conserved Asp(3.32)...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29576720/synthesis-molecular-docking-ctdna-interaction-dft-calculation-and-evaluation-of-antiproliferative-and-anti-toxoplasma-gondii-activities-of-2-4-diaminotriazine-thiazole-derivatives
#11
Krzysztof Z Łączkowski, Joanna Anusiak, Marta Świtalska, Katarzyna Dzitko, Joanna Cytarska, Angelika Baranowska-Łączkowska, Tomasz Plech, Agata Paneth, Joanna Wietrzyk, Joanna Białczyk
Synthesis, characterization, and investigation of antiproliferative activities against human cancer cell lines (MV4-11, MCF-7, and A549) and Toxoplasma gondii parasite of twelve novel 2,4-diaminotriazine-thiazoles are presented. The toxicity of the compounds was studied at three different cell types, normal mouse fibroblast (Balb/3T3), mouse fibroblast (L929), and human VERO cells. The structures of novel compounds were determined using 1 H and 13 C NMR, FAB(+)-MS, and elemental analyses. Among the derivatives, 4a - k showed very high activity against MV4-11 cell line with IC50 values between 1...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29527108/synthesis-and-antibacterial-activities-of-enamine-derivatives-of-dehydroacetic-acid
#12
Alex G Baldwin, Jonathan Bevan, David Brough, Ruth Ledder, Sally Freeman
Dehydroacetic acid is a common pyrone derivative used commercially as an antibacterial and antifungal agent. Based on the synthesis of dehydroacetic acid ( 1 ) from N -hydroxysuccinimdyl acetoacetate, a novel series of enamine-based derivatives were synthesised in order to improve the antibacterial activity of dehydroacetic acid. The antibacterial activities of the synthesised analogues were evaluated against Escherichia coli and Staphylococcus aureus . Derivative 4d (N-Ph) was identified as the most potent inhibitor of S...
2018: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29170613/an-efficient-synthesis-of-indolo-2-3-b-quinoline-guanidine-derivatives-with-their-in-vitro-and-in-vivo-study
#13
Katarzyna Sidoryk, Marta Świtalska, Piotr Rózga, Joanna Wietrzyk, Iwona Bujak, Bartłomiej Żerek, Łukasz Kaczmarek, Marcin Cybulski
An optimization of the guanidylation process by verifying the efficacy of common guanylation reagents in order to obtain the guanidine derivatives of indolo[2,3-b]quinoline has been performed. As a result, a high-yield procedure using N , N '-di-Boc- N ''-triflylguanidine was applied to synthesize the guanidine derivative of indolo[2,3-b]quinoline 1 in a gram scale for specific in vitro and in vivo biological research. Extensive studies on the antiproliferative activity against eight human tumor cell lines were completed...
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29104411/synthesis-and-preliminary-assessment-of-the-anticancer-and-wnt-%C3%AE-catenin-inhibitory-activity-of-small-amide-libraries-of-fenamates-and-profens
#14
Bini Mathew, Judith V Hobrath, Wenyan Lu, Yonghe Li, Robert C Reynolds
As part of an ongoing program to study the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) through generating diversity libraries of multiple NSAID scaffolds, we synthesized a series of NSAID amide derivatives and screened these sets against three cancer cell lines (prostate, colon and breast) and Wnt/β-catenin signaling. The evaluated amide analog libraries show significant anticancer activity/cell proliferation inhibition, and specific members of the sets show inhibition of Wnt/β-catenin signaling...
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/29051697/new-fluphenazine-analogue-with-antimutagenic-and-anti-multidrug-resistance-activity-degradation-profile-and-stability-indicating-method
#15
Agnieszka Sobczak, Artur Teżyk, Joanna Szyndlarewicz, Jan Ziarniak, Piotr Świątek, Wiesław Malinka
Hydrochloride of 10-{2-hydroxy-3-[ N , N -bis-(2-hydroxyethyl)amino]propyl}-2-trifluoromethylphenothiazine (Flu-A) is a analogue of neuroleptic fluphenazine. Flu-A exhibits anti-multidrug resistance, antimutagenic, proapoptopic, and cancer-chemopreventive activities in screening studies. To define identity, quality, and purity of new active substance it is necessary to develop a appropriate analytical method and to establish a degradation profile. Thus, a stability-indicating reversed-phase high-performance liquid chromatography method was developed and validated for quantitative determination of Flu-A in the presence of its degradation products generated under stress conditions...
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/28515623/antibacterial-properties-of-5-substituted-derivatives-of-rhodanine-3-carboxyalkyl-acids
#16
Waldemar Tejchman, Izabela Korona-Glowniak, Anna Malm, Marek Zylewski, Piotr Suder
A series of rhodanine 3-carboxyalkanoic acid derivatives possessing 4'-( N,N -dialkyl-amino or diphenylamino)-benzylidene moiety as a substituent at the C-5 position were synthesised and their antibacterial activity was screened. All the rhodanine derivatives showed bacteriostatic or bactericidal activity to the reference gram-positive bacterial strains, but lack of activity to the reference Gram-negative bacterial strains and yeast strains was observed.
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/28515622/the-influence-of-genistein-on-free-radicals-in-normal-dermal-fibroblasts-and-keloid-fibroblasts-examined-by-epr-spectroscopy
#17
Magdalena Jurzak, Paweł Ramos, Barbara Pilawa
Normal and keloid fibroblasts were examined using X-band (9.3 GHz) electron paramagnetic resonance spectroscopy. The effect of genistein on the concentration of free radicals in both normal dermal and keloid fibroblasts after ultraviolet irradiation was investigated. The highest concentration of free radicals was seen in keloid fibroblasts, with normal fibroblasts containing a lower concentration. The concentration of free radicals in both normal and keloid fibroblasts was altered in a concentration-dependent manner by the presence of genistein...
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/28163562/hydrazide-hydrazones-as-potential-antimicrobial-agents-overview-of-the-literature-since-2010
#18
REVIEW
Łukasz Popiołek
Hydrazide-hydrazone derivatives are present in many bioactive molecules and display a wide variety of biological activities, such as antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antiviral, and antiprotozoal action. Therefore, many medicinal chemists synthesize various hydrazide-hydrazones and evaluate them for biological activities. Among biological properties of this class of compounds, antimicrobial activity is the most frequently encountered in scientific literature...
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/28111515/cytotoxic-activity-of-genistein-8-c-glucoside-form-lupinus-luteus-l-and-genistein-against-human-sk-ov-3-ovarian-carcinoma-cell-line
#19
Agata Antosiak, Katarzyna Milowska, Katarzyna Maczynska, Sylwia Rozalska, Teresa Gabryelak
Genistein belongs to isoflavones, which are a subclass of flavonoids, a large group of polyphenolic compounds widely distributed in plants. Numerous in vitro studies suggest that isoflavones, particularly genistein, have both chemopreventive and chemotherapeutic potential in multiple tumor types. However, the molecular and cellular mechanisms of genistein effects on human ovarian cancer cells are still little known. In the present study, we investigated anticancer activity of genistein and its natural glucoside, genistein-8-C-glucoside isolated from flowers of Lupinus luteus L...
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/28111514/new-acetylenic-derivatives-of-betulin-and-betulone-synthesis-and-cytotoxic-activity
#20
REVIEW
Ewa Bębenek, Monika Kadela-Tomanek, Elwira Chrobak, Joanna Wietrzyk, Joanna Sadowska, Stanisław Boryczka
Betulin 1 and its semisynthetic derivatives exhibit a cytotoxic activity toward various cancer cell lines. These compounds are a promising and potential anticancer candidates. A series of betulin derivatives was prepared and tested for the antiproliferative activity in vitro against T47D breast cancer, CCRF/CEM leukemia, HL-60 promyelocytic leukemia, SW707 colorectal, murine P388 leukemia, as well as BALB3T3 normal fibroblasts cell lines. Cisplatin and betulin 1 were used as a reference compounds. Some derivatives of betulin showed a higher cytotoxic activity than the parent compound 1 ...
2017: Medicinal Chemistry Research
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