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Marcin Mielczarek et al.
Bioorganic & medicinal chemistry, 23(8), 1763-1775 (2015-03-18)
Our ongoing research focused on targeting transcription initiation in bacteria has resulted in synthesis of several classes of mono-indole and mono-benzofuran inhibitors that targeted the essential protein-protein interaction between RNA polymerase core and σ(70)/σ(A) factors in bacteria. In this study...
Sohail Anjum Shahzad et al.
Bioorganic chemistry, 60, 37-41 (2015-04-29)
Thymidine phosphorylase (TP) inhibitors have attracted great attention due to their ability to suppress the tumors formation. In our ongoing research, a series of 1,3,4-oxadiazole-2-thione (1-12) has been synthesized under simple reaction conditions in good to excellent yields (86-98%) and...
Bradford A Paik et al.
Soft matter, 11(9), 1839-1850 (2015-01-23)
Polymer-peptide conjugates were produced via the copper-catalyzed azide-alkyne cycloaddition of poly(tert-butyl acrylate) (PtBA) and elastin-like peptides. An azide-functionalized polymer was produced via atom transfer radical polymerization (ATRP) followed by conversion of bromine end groups to azide groups. Subsequent reaction of...
Anna Maria Waszkielewicz et al.
Acta poloniae pharmaceutica, 72(1), 89-99 (2015-04-09)
A series of new N-(2,5-dimethylphenoxy)- and N-(2,3,5-trimethylphenoxy)alkylaminoalkanols [I-XVII] was synthesized and evaluated for anticonvulsant activity. Pharmacological tests included maximal electroshock (MES) and subcutaneous pentetrazole seizure threshold (scMet) assays as well as neurotoxicity (TOX) evaluation in mice after intraperitoneal (i.p.) administration...
G V Mokrov et al.
Bioorganic & medicinal chemistry, 23(13), 3368-3378 (2015-05-06)
A series of 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamides were designed and synthesized as 18kDa translocator protein (TSPO) ligands. Anxiolytic-like activity of compounds was evaluated in the open field test and elevated plus maze test. Compounds 1a and 1b demonstrated high anxiolytic-like effect in the...
Papawee Suabjakyong et al.
PloS one, 10(3), e0122733-e0122733 (2015-03-27)
The basidiomycetous mushroom Phellinus igniarius (L.) Quel. has been used as traditional medicine in various Asian countries for many years. Although many reports exist on its anti-oxidative and anti-inflammatory activities and therapeutic effects against various diseases, our current knowledge of...
Yan-Jun Sun et al.
Molecules (Basel, Switzerland), 20(6), 9671-9685 (2015-05-29)
In the present work, a quantitative 1H Nuclear Magnetic Resonance (qHNMR) was established for purity assessment of six aryltetralin lactone lignans. The validation of the method was carried out, including specificity, selectivity, linearity, accuracy, precision, and robustness. Several experimental parameters...
Kai-Ling Wang et al.
Marine biotechnology (New York, N.Y.), 17(5), 624-632 (2015-08-05)
In the present study, eight natural products that belonged to di(1H-indol-3-yl)methane (DIM) family were isolated from Pseudovibrio denitrificans UST4-50 and tested for their antifouling activity against larval settlement (including both attachment and metamorphosis) of the barnacle Balanus (=Amphibalanus) amphitrite and...
Mariana Trujillo et al.
Journal of agricultural and food chemistry, 62(42), 10297-10303 (2014-09-30)
A series of nitroderivatives has been synthesized from hydroxytyrosol, the natural olive oil phenol, to increase the assortment of compounds with putative effects against Parkinson's disease. Nitrohydroxytyrosyl esters were obtained from nitrohydroxytyrosol using a chemoselective one-step, high-yield, transesterification procedure. The...
Zaman Ashraf et al.
European journal of medicinal chemistry, 98, 203-211 (2015-05-31)
The present studies reports the synthesis of hydoxylated thymol analogues (4a-e) and (6a-c) as mushroom tyrosinase inhibitors. The title compounds were obtained in good yield and characterized by FTIR, (1)H NMR, (13)C NMR, Mass spectral data and X-ray crystallography in...
Sahng Hyuck Woo et al.
ACS applied materials & interfaces, 7(30), 16466-16477 (2015-07-15)
This study proposes a method to prepare a crack-free poly(vinylidene fluoride) (PVDF) microfiltration (MF) membrane with enhanced antifouling property. In the study, blending 4% poly(vinylidene fluoride)-graft-poly(sulfopropyl methacrylate) (PVDF-g-PSPMA) and 1.5% potassium perchlorate (KClO4) led to crack prevention during membrane preparation...
Zengyan Wei et al.
Nature communications, 5, 3870-3870 (2014-05-16)
The shape-controlled synthesis of nanoparticles was established in single-phase solutions by controlling growth directions of crystalline facets on seed nanocrystals kinetically; however, it was difficult to rationally predict and design nanoparticle shapes. Here we introduce a methodology to fabricate nanoparticles...
Matshawandile Tukulula et al.
Pharmaceutical research, 32(8), 2713-2726 (2015-03-01)
There is significant interest in the application of nanoparticles to deliver immunostimulatory signals to cells. We hypothesized that curdlan (immune stimulating polymer) could be conjugated to PLGA and nanoparticles from this copolymer would possess immunostimulatory activity, be non-cytotoxic and function...
Yan-ping Li et al.
Cancer chemotherapy and pharmacology, 75(4), 773-782 (2015-02-15)
To find novel potential and less toxic benquinone anamycin heat shock protein 90 (Hsp90) inhibitors as anticancer agents, a limited series of 17-substituted or 17,19-disubstituted 17-demethoxygeldanamycin analogs were synthesized and tested for anti-proliferation activity against human cancer cells. Liver toxicity...
Li Lin et al.
Dalton transactions (Cambridge, England : 2003), 44(12), 5867-5874 (2015-02-27)
A zinc phthalocyanine (ZnPc) derivative (Zn-tri-PcNc-8) containing tri-benzonaphtho-condensed porphyrazine with one carboxylic and six diphenylphenoxy peripheral substitutions was designed and synthesized as a sensitizer for dye-sensitized solar cells (DSSCs). For the purpose of extending the absorption spectra while minimizing the...
Dengfeng Zhang et al.
Journal of pharmaceutical and biomedical analysis, 99, 22-27 (2014-07-23)
Retigabine was the first neuronal potassium channel opener for the treatment of epilepsy. During the manufacture of retigabine, two unknown impurities were present in laboratory batches in the range of 0.05-0.1% based upon HPLC analysis. These unknown impurities were obtained...
Atif Sarwar et al.
PloS one, 10(4), e0123084-e0123084 (2015-05-01)
Recently, the attention of researchers has been drawn toward the synthesis of chitosan derivatives and their nanoparticles with enhanced antimicrobial activities. In this study, chitosan derivatives with different azides and alkyne groups were synthesized using click chemistry, and these were...
Radhika Sharma et al.
European journal of medicinal chemistry, 90, 342-350 (2014-12-02)
Type 2 diabetes (T2D) is a lifestyle disease affecting millions of people worldwide. Various therapies are available for the management of T2D and dipeptidyl peptidase-IV (DPP-IV) inhibition has emerged as a promising therapy for the treatment of type 2 diabetes...
Riyadh Ahmed Atto AL-Shuaeeb et al.
Organic & biomolecular chemistry, 13(44), 10904-10916 (2015-09-16)
An efficient synthesis of thioglycosylated benzo[e][1,4]oxathiepin-5-one and benzothiazepinone derivatives by a sequence of palladium-catalyzed glycosyl thiol arylation followed by deprotection-lactonization reactions has been reported. This diversity-oriented strategy enabled access to unknown complex cyclic scaffolds with polyhydroxylated appendages of biological interest.
Irene Briguglio et al.
European journal of medicinal chemistry, 105, 63-79 (2015-10-20)
Linear aromatic N-tricyclic compounds with promising antiviral activity and minimal cytotoxicity were prepared and analyzed in the last years. Specifically, the pyrido[2,3-g]quinoxalinone nucleus was found endowed with high potency against several pathogenic RNA viruses as etiological agents of important veterinary...
Gaolei Wang et al.
Journal of agricultural and food chemistry, 63(31), 6883-6889 (2015-07-07)
A series of novel 1,2,3-benzotriazin-4-one derivatives were synthesized by the reaction of 3-bromoalkyl-1,2,3-benzotriazin-4-ones with potassium salt of 2-cyanoimino-4-oxothiazolidine in the presence of potassium iodide. Nematicidal assays in vivo showed that some of them exhibited good control efficacy against the cucumber...
Ravi Rapolu et al.
Journal of pharmaceutical and biomedical analysis, 107, 488-494 (2015-02-14)
Forced degradation of Ebastine (1-(4-(1,1-dimethylethyl)phenyl)-4-(4-(diphenylmethoxy) piperidin-1-yl)butan-1-one) drug substance in ultraviolet light condition resulted into an unknown significant degradation product. This degradation product was analyzed using a newly developed reverse-phase HPLC, where it was eluted at 2.73 relative retention time to...
Rajni Khajuria et al.
Organic & biomolecular chemistry, 13(21), 5944-5954 (2015-05-01)
A wide range of 4,6-diarylated/heterylated pyridin-2(1H)-one derivatives were synthesized in good to excellent yields from 1,3-diarylated/heterylated-2-propen-1-ones (chalcones) in one pot under metal and base-free conditions. This domino reaction suggests a novel mechanism comprising of Michael addition followed by amination, subsequent...
Wen Lu et al.
Bioorganic & medicinal chemistry, 23(5), 1044-1054 (2015-02-01)
VEGFR-2 plays an essential role in angiogenesis and is a central target for anticancer drug discovery. In order to develop novel VEGFR-2 inhibitors, we designed and synthesized 33 biphenyl amides based on our previously reported lead compound. The biological results...
Faiz-Ur Rahman et al.
Dalton transactions (Cambridge, England : 2003), 44(5), 2166-2175 (2014-12-17)
A series of novel Pt(ii) complexes [cis- and trans-Pt(ii)(salicylaldimine)(DMSO)Cl (), trans-Pt(ii)(salicylaldimine)(4-picoline)Cl (), Pt(ii)(salicylaldimine)Cl (), trans- and cis/trans-Pt2(ii)(salicylaldimine)(DMSO)2Cl2 (), trans-Pt2(ii)(salicylaldimine)(4-picoline)2Cl2 () was synthesized and characterized. The structures of -cis, -trans and were determined using a single crystal X-ray analysis. This class...
Amol Patil et al.
Molecular diversity, 19(3), 435-445 (2015-03-21)
A library of quinazolinones was prepared by the one-pot three-component reaction of isatoic anhydride, ammonium salts/amines, and various electrophiles using aqueous hydrotropic solution as an efficient, economical, reusable, and green medium giving good to excellent yields of products in very...
Eva Vavříková et al.
International journal of molecular sciences, 16(6), 11983-11995 (2015-05-29)
A panel of lipases was screened for the selective acetylation and alcoholysis of silychristin and silychristin peracetate, respectively. Acetylation at primary alcoholic group (C-22) of silychristin was accomplished by lipase PS (Pseudomonas cepacia) immobilized on diatomite using vinyl acetate as...
Xue Wang et al.
Scientific reports, 5, 16127-16127 (2015-11-05)
The human β-amyloid (Aβ) cleaving enzyme (BACE-1) is a target for Alzheimer's disease (AD) treatments. This study was conducted to determine if acacetin extracted from the whole Agastache rugosa plant had anti-BACE-1 and behavioral activities in Drosophila melanogaster AD models...
Chun Yang et al.
Zeitschrift fur Naturforschung. C, Journal of biosciences, 70(3-4), 65-69 (2015-05-30)
A series of novel arylmethylamine derivatives of honokiol (5a-m) was prepared. Their insecticidal activity was tested against the pre-third-instar larvae of the oriental armyworm (Mythimna separata Walker), a typical lepidopteran pest. Compounds 5a, 5b, 5e, 5h, and 5k exhibited insecticidal...
Danning Zhang et al.
Environmental science & technology, 48(21), 12645-12653 (2014-10-15)
The formation of reactive oxygen species (ROS) from effluent organic matter (EfOM) was investigated under simulated solar irradiation. In this study, EfOM was isolated into three different fractions based on hydrophobicity. The productivity of ROS in EfOM was measured and...
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