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Chemistry & Biodiversity

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https://www.readbyqxmd.com/read/30019534/biology-oriented-drug-synthesis-biods-approach-towards-synthesis-of-ciprofloxacin-dithiocarbamate-hybrids-and-their-antibacterial-potential-both-in-vitro-and-in-silico
#1
Ensieh Nasli Esfahani, Maryam Mohammadi-Khanaposhtani, Zahra Rezaei, Yosef Valizadeh, Ramazan Rajabnia, Meghdad Bagheri, Fatemeh Bandarian, Mohammad Ali Faramarzi, Nasrin Samadi, Mohammad Reza Amini, Mohammad Mahdavi, Bagher Larijani
A novel series of ciprofloxacin-dithiocarbamate hybrids 7a-l were designed, synthesized, and evaluated against Gram-positive and Gram-negative bacteria. A significant part of the title compounds showed considerable antibacterial activity against Gram-positive species. The most potent compound against Gram-positive bacteria was 2-chloro derivative 7h and the most potent derivative against Gram-negative bacteria was 3-chloro compound 7i. In vitro antibacterial evaluation of compound 7h against clinically isolated bacteria methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA) showed that this compound acted better than ciprofloxacin against the latter bacteria...
July 17, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/30019425/chemical-constituents-from-chloranthus-anhuiensis-and-their-cytotoxic-activities
#2
Hui-Lin Zhu, Wei Qu, Jie Zhang, Wen-Yuan Cao, Er-Yan Guo, Tao Du, Wen-Yuan Liu, Feng Feng, Jian Xu
Three hiherto unknown phenylpropanoid compounds, namely (7S,8R)-1-(1-ethoxy-2-hydroxypropyl)-2-methoxy-3,4-methyl-enedioxybenzene (1), (7S,8S)-1-(1-ethoxy-2-hydroxypropyl)-2-methoxy-3,4-methylenedioxybenzene (2), and (7S,8R)-1-(1-methoxy-2-hydroxypropyl)-2-methoxy-3,4-methylenedioxybenzene (3), along with 12 known compounds (4 - 15) were obtained from the extract of whole plant of Chloranthus anhuiensis. Among them, (7) and (13) were obtained from nature for the first time. The structures of these natural compounds were characterized by extensive spectroscopic analysis and calculated electronic circular dichroism (ECD) data...
July 17, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/30007108/insight-into-the-chemical-diversity-of-late-ice-harvest-gew%C3%A3-rztraminer-wine
#3
Igor Jerković, Zvonimir Marijanović, Gabriele Serreli, Carlo Ignazio Giovanni Tuberoso
Late harvest (LHW) and ice harvest (IHW) Gewürztraminer wine samples from Croatia (Ilok) were investigated. Their technological parameters, chromaticity coordinates, total phenols content, and antioxidant capacity were determined. 5-Hydroxymethylfurfural, xanthine, and trans-caftaric acid were analyzed in the samples by high performance liquid chromatography (HPLC-DAD). Headspace solid-phase microextraction (HS-SPME) followed by gas chromatography and mass spectrometry (GC-MS) analysis revealed isoamyl alcohol as predominant compound (21...
July 14, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29999602/novel-catechol-derivatives-of-arylimidamides-as-antileishmanial-agents
#4
Foroogh Rezaei, Lotfollah Saghaei, Razieh Sabet, Afshin Fassihi, Gholamreza Hatam
Two novel bis-arylimidamide derivatives with terminal catechol moieties (9a and 10a) and two parent compounds with terminal phenyl groups (DB613 and DB884) were synthesized as dihydrobromide salts (9b and 10b). The designed compounds were hybrid molecules consisting of a catechol functionality embedded in an arylimidamide moiety. All compounds were examined for in vitro antiparasitic activity upon promastigotes of Leishmania major and L. infantum as well as axenic amastigotes of L. major. It was shown that conversion of terminal phenyl groups into catechol moieties resulted in more than 10-fold improvement in potency, coupled with lower cytotoxicity against fibroblast cells, compared to the corresponding parent compounds...
July 12, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29996001/the-chemical-compositions-of-angelica-pubescens-oil-and-its-prevention-of-uv-b-radiation-induced-cutaneous-photoaging
#5
Dingkang Chen, Zhiyun Du, Zhirong Lin, Ping Su, Hanyi Huang, Zhirong Ou, Wanyi Pan, Shiya Huang, Kun Zhang, Xi Zheng, Li Lin, Lanyue Zhang
Angelica pubescens, a plant of the family Umbelliferae, has been widely used as traditional Chinese medicine for the treatment of many diseases; however, there has been minimal modern research focused on the pharmacological activity of oils extracted from Angelica pubescens, in particular, the potential anti-photoaging effects. Therefore, in the present study, we analyzed the chemical composition of Angelica pubescens oil (AO) and evaluated its bioactivity against photoaging in ultraviolet (UV) -B radiation-induced hairless mice...
July 11, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29989350/chemotaxonomic-considerations-of-the-n-alkane-composition-in-pinus-heldreichii-p-nigra-and-p-peuce
#6
Biljana M Nikolić, Zorica S Mitić, Vele V Tešević, Iris Ž Đorđević, Marina M Todosijević, Srdjan R Bojović, Petar D Marin
The n-alkane composition in the leaf cuticular waxes of natural populations of Bosnian pine (Pinus heldreichii), Austrian pine (P. nigra) and Macedonian pine (P. peuce) was compared for the first time. The range of n-alkanes was wider in P. nigra (C16 -C33 ) than in P. heldreichii and P. peuce (C18 -C33 ). Species also diverged in abundance and range of dominant n-alkanes (P. heldreichii: C23 , C27 , and C25 ; P. nigra: C25 , C27 , C29 , and C23 ; P. peuce: C29 , C25 , C27 , and C23 ). Multivariate statistical analyses (PCA, DA and CA) generally pointed out separation of populations of P...
July 10, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29989308/thermodynamics-of-the-interactions-of-aminobisphosphonates-and-their-calcium-complexes-with-bovine-serum-albumin
#7
J Gałęzowska, E Chmielewska
Binding of bisphosphonates (BPs) to plasma proteins was investigated in the 1990s as a pharmacokinetic issue in order to fully understand bio-distribution of BP drugs which are successfully used for the treatment of several bone-related diseases. It has been hypothesized that binding to these proteins occurs with low to moderate affinity despite of unfavorable hydrophilicity of BPs, and Ca2+ was identified as a strong catalyst of this binding. However, these studies mainly consisted in the separation and quantification of bound and unbound drug or protein fractions using chromatographic techniques without an outcome on the molecular level...
July 10, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29987907/design-synthesis-and-antibacterial-evaluation-of-1-1r-2s-2-fluorocyclopropyl-ciprofloxacin-1-2-4-triazole-5-4h-thione-hybrids
#8
Yang Gao, Lu-Xin Na, Zhi Xu, Shu Zhang, A-Peng Wang, Kai Lv, Hui-Yuan Guo, Ming-Liang Liu
A new class of 1-[(1R, 2S)-2-fluorocyclopropyl]ciprofloxacin (CPFX)-1,2,4-triazole-5(4H)-thione hybrids 6a-o was designed, synthesized and evaluated for their in vitro antibacterial activities against a panel of clinically important drug-sensitive and drug-resistant Gram-positive and Gram-negative pathogens. Our results revealed that all hybrids 6a-o have great potency against the tested strains, especially Gram-negative pathogens. The synthesized hybrids were more potent than the parent 1-[(1R, 2S)-2-fluorocyclopropyl]CPFX 5, and were comparable to CPFX and levofloxacin against the majority of the tested pathogens, worth to be further investigated...
July 10, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29987893/two-new-chromone-glycosides-from-roots-of-saposhnikovia-divaricata
#9
Si-Yuan Ma, Ling-Gao Shi, Zheng-Bing Gu, Yu-Lan Wu, Liu-Bin Wei, Qi-Qiu Wei, Xing-Ling Gao, Na Liao
Five chromone glycosides were isolated from water-soluable portions of 70% EtOH extract of roots of Saposhnikovia divaricata, including two new chromone glycosides 1 and 2. The structures of the chromone glycosides were identified as (3'S)-3'-O-β-D-apiofuranosyl-(1 → 6)-O-β-D-glucopyranosylhamaudol (1), (2'S)- 4'-O-β-D-apiofuranosyl-(1 → 6)-O-β-D-glucopyranosylvisamminol (2), sec-O-glucosylhamaudol (3), 4'-O-β-D-glucopyranosylvisamminol (4), and 4'-O-β-D-glucopyranosyl-5-O-methylvisamminol (5) on the basis of extensive spectroscopic methods, and the absolute configurations of the new compounds were elucidated by the electronic circular dichroism (ECD) calculation and acid hydrolysis...
July 10, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29981528/design-synthesis-and-antifungal-activities-of-novel-1-2-4-triazole-schiff-base-derivatives
#10
Ruyi Jin, Jingli Liu, Guanghui Zhang, Jiajia Li, Shuan Zhang, Hui Guo
With the aim to find new compounds with high antifungal activity, 21 4-amino-5-substitute-1,2,4-triazole Schiff bases (2a-2g, 3a-3g and 4a-4g) were designed and synthesized. Their antifungal activities against Pythium solani, Gibberlla nicotiancola, Fusarium oxysporium f. sp. niveum, Gibberlla saubinetii, Alternaria iycopersici, Phytophthora capsici, Physalospora piricola, Cercospora arachidicola hori, and Fusarium oxysporium f. sp. cucumber were tested, parts of the compounds exhibited excellent antifungal activity...
July 7, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29969533/pumilol-a-diterpenoid-with-a-rare-strobane-skeleton-from-pinus-pumila-pinaceae
#11
Moses K Langat, Andreas Helfenstein, Claire Horner, Päivi Tammela, Heikki Hokkanen, Denis Izotov, Dulcie A Mulholland
Pumilol (1), a strobane diterpenoid, reported herein for the first time was isolated from the bark of Pinus pumila (Pall.) Regel (Siberian Dwarf Pine or Japanese Stone Pine), along with seventeen known compounds including serratane triterpenoids, not previously reported from this species, and four ferulate derivatives. The stereostructure of pumilol was established using HRESIMS, NMR, the DP4+ probabilities and by comparison of the experimental and calculated electronic circular dichroim (ECD) spectra. Labda-8(17),13-dien-15-oic acid (4), bornyl trans-4-hydroxycinnamate (14) and E-bornyl ferulate (15) showed activity against S...
July 3, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29963758/diversity-of-secondary-metabolites-in-the-liverwort-syzygiella-rubricaulis-nees-steph-jamesoniellaceae-marchantiophyta-from-neotropical-high-mountains
#12
Denise P Costa, Gilberto M Amado-Filho, Renato C Pereira, Wladimir C Paradas, Hideki Miyataka, Yasuko Okamoto, Yoshinori Asakawa
In order to evaluate the chemical diversity of Syzygiella rubricaulis (Nees) Steph., a species with a disjunct distribution in the neotropical high mountains, a phytochemical study was carried out with samples from twelve different populations of different altitudes from four South American countries. The chemical profiles of lipophilic extracts were analyzed by GC/MS for each population and 50 different compounds were found, with the predominance and richness of sesquiterpenes. The majority of the compounds were found only in one population and the total number of substances ranged from 1 to 15 among the populations, but these numbers were not correlated with altitude, characterize each population as distinct, based on similarity analysis...
July 2, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29959828/interpopulation-variability-in-the-essential-oil-composition-of-cistus-creticus-subspecies-eriocephalus-from-sardinia
#13
Patrizia Monica Mastino, Mauro Marchetti, Jean Costa, Marianna Usai
Cistus genus is widespread in the Mediterranean regions with several species and is traditionally known as a natural remedy, but few previous phytochemical researches have been reported on Cistus species growing in Sardinia. The aim of this work was to study the interpopulation variability of the volatiles of C. creticus subsp. eriocephalus to find out the natural chemotypes of this taxon for chemotaxonomic purposes. Plant material was collected from seven wild populations in Sardinia. The oils from aerial part were obtained by hydrodistillation and analyzed by GC-MS enabling to identify 185 compounds...
June 29, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29956891/chemical-composition-cytotoxic-and-antibacterial-activities-of-essential-oils-of-cultivated-clones-of-juniperus-communis-and-wild-juniperus-species
#14
Antim K Maurya, Renuka Devi, Ashish Kumar, Rajkesh Koundal, Soni Thakur, Anamika Sharma, Dharmesh Kumar, Rakshak Kumar, Yogendra S Padwad, Gopi Chand, Bikram Singh, Vijai K Agnihotri
Needles of seven cultivated clones (C1-C7) of Juniperus communis at lower altitude and three wild Juniperus species (J. communis, J. recurva and J. indica) of higher altitudes were investigated comparatively for their essential oils (EOs) yields, chemical composition, cytotoxic, and antibacterial activities. The EOs yields were varied from 0.26 to 0.56% (v/w) among samples. Sixty-one volatile components were identified by gas chromatography-mass spectrometry (GC-MS) and quantified using gas chromatography GC (FID) representing 82...
June 29, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29956887/synthesis-biological-evaluation-and-molecular-docking-of-novel-thiazoles-and-1-3-4-thiadiazoles-incorporating-sulfonamide-group-as-dhfr-inhibitors
#15
Sayed M Riyadh, Shojaa A El-Motairi, Hany E A Ahmed, Khaled D Khalil, El-Sayed E Habib
2-{1-[4-((4-Methylphenyl)sulfonamide)phenyl]ethylidine}thiosemicarbazide (3) was exploited as a starting material for synthesis of two novel series of 5-arylazo-2-hydrazonothiazoles 6a-j and 2-hydrazono[1,3,4]thiadiazoles 10a-d, incorporating sulfonamide group, through its reactions with appropriate hydrazonoyl halides. The structures of the newly synthesized products were confirmed by spectral and elemental analyses. Also, the antimicrobial, anticancer, and DHFR inhibition potency for two series of thiazoles and [1,3,4]thiadiazoles were evaluated and explained by molecular docking studies and SAR analysis...
June 29, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29956885/discovery-of-a-new-class-of-inhibitors-of-vaccinia-virus-based-on-borneol-from-%C3%A3-bies-sib%C3%A3-rica-and-camphor
#16
Anastasiya S Sokolova, Olga I Yarovaya, Nikolay I Bormotov, Larisa N Shishkina, Nariman F Salakhutdinov
A series of the bornyl ester/amide derivatives with N-containing heterocycles were designed and synthesised as Vaccinia virus (VV) inhibitors. Bioassay results showed that among the designed compounds, derivatives 6, 13, 14, 34, 36 and 37 showed the best inhibitory activity against VV with IC50 values of 12.9, 17.9, 3.4, 2.5, 12.5 and 7.5 μM, respectively, and good cytotoxicity. The primary structure-activity relationship (SAR) study suggested that the combination of a saturated N-heterocycle, such as morpholine or 4-methylpiperidine, and a 1,7,7-trimethylbicyclo[2...
June 29, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29953725/a-small-library-of-1-2-3-triazole-analogues-of-cap-55-synthesis-and-binding-affinity-at-nicotinic-acetylcholine-receptors
#17
Luca Rizzi, Cecilia Gotti, Marco De Amici, Clelia Dallanoce, Carlo Matera
Alpha7 nicotinic acetylcholine receptor is emerging as a central regulator in inflammatory processes, as documented by increasing studies reported in the literature. For instance, the activation of this nicotinic receptor subtype in resident macrophages inhibits the production of pro-inflammatory cytokines, thereby attenuating local inflammatory responses, and may open a new window in the treatment of chronic inflammatory disease, such as Crohn's disease, rheumatoid arthritis, psoriasis and asthma. In continuation of our ongoing research for the development of new cholinergic drug candidates, we selected the nicotine derivative CAP55, which was previously shown to exert anti-inflammatory effects via nicotinic stimulation, as a suitable compound for lead optimization...
June 28, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29935105/synthesis-of-3-methylidene-1-tosyl-2-3-dihydroquinolin-4-1h-ones-as-potent-cytotoxic-agents
#18
Jacek Koszuk, Tomasz Bartosik, Jakub Wojciechowski, Wojciech Wolf, Anna Janecka, Joanna Drogosz, Angelika Długosz, Urszula Krajewska, Marek Mirowski, Tomasz Janecki
An efficient synthetic strategy to 3-methylidene-2,3-dihydroquinolin-4(1H)-ones variously substituted in position 2 has been developed. The title compounds were synthesized in the reaction sequence involving reaction of diethyl methylphosphonate with methyl 2-(tosylamino)benzoate, condensation of thus formed diethyl 2-(2-N-tosylphenyl)2-oxoethylphosphonate with various aldehydes followed by successful application of the obtained 3-diethoxyphosphoryl-1,2-dihydroquinolin-4-ols as Horner-Wadsworth-Emmons reagents for the olefination of formaldehyde...
June 23, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29935095/structure-based-design-and-synthesis-of-fluorene-derivatives-as-novel-ror%C3%AE-t-inverse-agonists
#19
Moustafa T Gabr, Mohammed S Abdel-Raziq
A new series of fluorene derivatives was designed and synthesized as novel retinoic acid receptor-related orphan receptor gamma t (RORγt) inverse agonists utilizing a molecular hybridization approach. The new compounds 10-15 were evaluated for their RORγt activity using biochemical FRET and cellular reporter gene assays. Moreover, the inhibitory activity of the fluorene derivatives 10-15 in mouse Th17 cell differentiation assay was assessed. The hybrid compound 15 that combines both fluorene and arylsulfone moieties displayed promising RORγt activity with IC50 values of 68...
June 23, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29933520/bioactivity-guided-isolation-of-anti-inflammatory-constituents-of-the-rare-mushroom-calvatia-nipponica-in-lps-stimulated-raw264-7-macrophages
#20
Seulah Lee, Dahae Lee, Joo Chan Lee, Ki Sung Kang, Rhim Ryoo, Hyun-Ju Park, Ki Hyun Kim
Calvatia species, generally known as puffball mushrooms, are used both as sources of food as well as traditional medicine. Among the Calvatia genus, Calvatia nipponica (Agaricaceae) is one of the rarest species. Using bioassay-guided fractionation based on anti-inflammatory effects, five alkaloids (1 - 5), two phenolics (6 - 7) and a fatty acid methyl ester (8) were isolated from the fruiting bodies of C. nipponica. Compound 8 was identified from C. nipponica for the first time, and all isolates (1 - 8) were tested for inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264...
June 22, 2018: Chemistry & Biodiversity
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