Synthesis of egonol derivatives and their antimicrobial activities.

abstract：:Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. We generated two series of esters by multi-step synthesis with substituted 6-aminohexanoic acid as potential transdermal penetration enhancers by multi-step synthesis. Th...

journal_title：Bioorganic & medicinal chemistry

authors： Brychtova K,Opatrilova R,Raich I,Kalinowski DS,Dvorakova L,Placek L,Csollei J,Richardson DR,Jampilek J

更新日期：2010-12-15 00:00:00

abstract：:Twelve thiorhodamine derivatives have been examined for their ability to stimulate the ATPase activity of purified human P-glycoprotein (P-gp)-His(10), to promote uptake of calcein AM and vinblastine into multidrug-resistant, P-gp-overexpressing MDCKII-MDR1 cells, and for their rates of transport in monolayers of mult...

journal_title：Bioorganic & medicinal chemistry

authors： Orchard A,Schamerhorn GA,Calitree BD,Sawada GA,Loo TW,Claire Bartlett M,Clarke DM,Detty MR

更新日期：2012-07-15 00:00:00

abstract：:In this study, a number of 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs were designed and synthesized. Their thermal stability, nuclease resistance and gene silencing properties against cultured mammalian cells were evaluated and compared with those of natural siRNAs. The 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs (...

journal_title：Bioorganic & medicinal chemistry

authors： Abdur Rahman SM,Sato H,Tsuda N,Haitani S,Narukawa K,Imanishi T,Obika S

更新日期：2010-05-15 00:00:00

abstract：:A series of 2-sec-amino-3H-quinazolin-4-ones (4a-p) and 4-sec-amino-2-chloroquinazolines (5a-b) have been synthesized by nucleophilic substitution reaction of 2-chloro-4(3H)-quinazolones (3) and 2,4-dichloroquinazolines (2) with amines, respectively. Most of the synthesized compounds were evaluated for antihyperglycem...

journal_title：Bioorganic & medicinal chemistry

authors： Ram VJ,Farhanullah,Tripathi BK,Srivastava AK

更新日期：2003-05-29 00:00:00

abstract：:Carbonic anhydrases (CAs) are essential and ubiquitous enzymes. Thus far, there are no articles on characterization of Drosophila melanogaster α-CAs. Data from invertebrate CA studies may provide opportunities for anti-parasitic drug development because α-CAs are found in many parasite or parasite vector invertebrates...

journal_title：Bioorganic & medicinal chemistry

authors： Syrjänen L,Tolvanen ME,Hilvo M,Vullo D,Carta F,Supuran CT,Parkkila S

更新日期：2013-03-15 00:00:00

abstract：:A new series of selective PDE4D inhibitors has been designed and synthesized by replacing 3-methoxy group with 3-difluoromethoxy isoster moiety in our previously reported cathecolic structures. All compounds showed a good PDE4D3 inhibitory activity, most of them being inactive toward other PDE4 isoforms (PDE4A4, PDE4B...

journal_title：Bioorganic & medicinal chemistry

authors： Brullo C,Massa M,Villa C,Ricciarelli R,Rivera D,Pronzato MA,Fedele E,Barocelli E,Bertoni S,Flammini L,Bruno O

更新日期：2015-07-01 00:00:00

abstract：:The fluorescent intercalator displacement assay using thiazole orange has been adapted to the study of RNA-binding helix-threading peptides (HTPs). This assay is highly sensitive with HTP-binding RNAs and provides binding affinity data in good agreement with quantitative ribonuclease footprinting without the need for ...

journal_title：Bioorganic & medicinal chemistry

authors： Krishnamurthy M,Schirle NT,Beal PA

更新日期：2008-10-01 00:00:00

abstract：:γ-Aminobutyric acid (GABA) receptors are important targets of parasiticides/insecticides. Several 4-substituted analogs of the partial GABAA receptor agonist 5-(4-piperidyl)-3-isothiazolol (Thio-4-PIOL) were synthesized and examined for their antagonism of insect GABA receptors expressed in Drosophila S2 cells or Xeno...

journal_title：Bioorganic & medicinal chemistry

authors： Liu G,Furuta K,Nakajima H,Ozoe F,Ozoe Y

更新日期：2014-09-01 00:00:00

abstract：:Pyridine-based compounds have been playing a crucial role as agrochemicals or pesticides including fungicides, insecticides/acaricides and herbicides, etc. Since most of the agrochemicals listed in the Pesticide Manual were discovered through screening programs that relied on trial-and-error testing and new agrochemic...

journal_title：Bioorganic & medicinal chemistry

authors： Guan AY,Liu CL,Sun XF,Xie Y,Wang MA

更新日期：2016-02-01 00:00:00

abstract：:A series of novel benzofuran-dihydropyridine hybrids were designed by molecular hybridization approach and evaluated for bone anabolic activities. Among the screened library, ethyl 4-(7-(sec-butyl)-2-(4-methylbenzoyl)benzofuran-5-yl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate (compound 21) significant...

journal_title：Bioorganic & medicinal chemistry

authors： Modukuri RK,Choudhary D,Gupta S,Rao KB,Adhikary S,Sharma T,Siddiqi MI,Trivedi R,Sashidhara KV

更新日期：2017-12-15 00:00:00

abstract：:Six novel N(4)-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines and their N(2)-trimethylacetyl substituted analogs were synthesized as receptor tyrosine kinase (RTK) inhibitors. A microwave-mediated Sonogashira reaction was used as a key step for the synthesis of these compounds. Biol...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Namjoshi OA,Yu J,Ihnat MA,Thorpe JE,Bailey-Downs LC

更新日期：2013-03-01 00:00:00

abstract：:Sortases catalyze the attachment of surface proteins to the peptidoglycan layer of gram-positive bacteria and further represent powerful tools of protein chemistry. During catalysis sortases cleave a donor substrate containing the LPxTG (x=any amino acid) sorting motif under formation of an enzyme-bound thioester and ...

journal_title：Bioorganic & medicinal chemistry

authors： Schmohl L,Bierlmeier J,von Kügelgen N,Kurz L,Reis P,Barthels F,Mach P,Schutkowski M,Freund C,Schwarzer D

更新日期：2017-09-15 00:00:00

abstract：:2-Amino-6-fluoro-9-(4-hydroxy-3-hydroxymethylbut-1-yl)purine (7), and its mono- and diesters 8-15 were prepared and evaluated for their potential as prodrugs of penciclovir. Treatment of 2-amino-6-chloro-9-(4-hydroxy-3-hydroxymethylbut-1-yl)purine (5) with trimethylamine in THF followed by a reaction of the resulting ...

journal_title：Bioorganic & medicinal chemistry

authors： Kim DK,Lee N,Kim HT,Im GJ,Kim KH

更新日期：1999-03-01 00:00:00

abstract：:The synthesis and anticonvulsant properties of new N-Mannich bases of 3-phenyl- (9a-d), 3-(2-chlorophenyl)- (10a-d), 3-(3-chlorophenyl)- (11a-d) and 3-(4-chlorophenyl)-pyrrolidine-2,5-diones (12a-d) were described. The key synthetic strategies involve the formation of 3-substituted pyrrolidine-2,5-diones (5-8), and th...

journal_title：Bioorganic & medicinal chemistry

authors： Kamiński K,Obniska J,Chlebek I,Wiklik B,Rzepka S

更新日期：2013-11-01 00:00:00

abstract：:The binding stoichiometry, binding constants, and inclusion mode of some water-soluble negatively charged cyclodextrin derivatives, i.e. heptakis-[6-deoxy-6-(3-sulfanylpropanoic acid)]-β-cyclodextrin(H1), heptakis-[6-deoxy-6-(2-sulfanylacetic acid)]-β-cyclodextrin(H2), mono-[6-deoxy-6-(3-sulfanylpropanoic acid)]-β-cyc...

journal_title：Bioorganic & medicinal chemistry

authors： Cheng JG,Yu HJ,Chen Y,Liu Y

更新日期：2018-05-15 00:00:00

abstract：:AKR1C3 is a promising therapeutic target for castration-resistant prostate cancer. Herein, an evaluation of in-house library discovered substituted pyranopyrazole as a novel scaffold for AKR1C3 inhibitors. Preliminary SAR exploration identified its derivative 19d as the most promising compound with an IC50 of 0.160 μM...

journal_title：Bioorganic & medicinal chemistry

authors： Zheng X,Jiang Z,Li X,Zhang C,Li Z,Wu Y,Wang X,Zhang C,Luo HB,Xu J,Wu D

更新日期：2018-12-01 00:00:00

abstract：:Novel 2-phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones (PQs) endowed with high affinity for central benzodiazepine receptor (BzR) were synthesized. In particular, 9-fluoro-2-(2-fluorophenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one (2(2)) showed binding affinity in the subnanomolar concentration range and p...

journal_title：Bioorganic & medicinal chemistry

authors： Carotti A,Altomare C,Savini L,Chiasserini L,Pellerano C,Mascia MP,Maciocco E,Busonero F,Mameli M,Biggio G,Sanna E

更新日期：2003-11-17 00:00:00

abstract：:The 6-desfluoroquinolones which have been developed by our group represent a promising class of compounds for the treatment of HIV infection since they act on transcriptional regulation, a crucial step in the replication cycle that has not been clinically exploited, yet. Focussing attention on the N-1 and C-6 position...

journal_title：Bioorganic & medicinal chemistry

authors： Massari S,Daelemans D,Manfroni G,Sabatini S,Tabarrini O,Pannecouque C,Cecchetti V

更新日期：2009-01-15 00:00:00

abstract：:A methanolic extract and its ethyl acetate-soluble fraction from Sri Lankan curry-leaf, the leaves of Murraya koenigii, inhibited melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. Two new carbazole alkaloids, karapinchamines A and B, were isolated from the ethyl acetate-soluble fraction together ...

journal_title：Bioorganic & medicinal chemistry

authors： Nakamura S,Nakashima S,Oda Y,Yokota N,Fujimoto K,Matsumoto T,Ohta T,Ogawa K,Maeda S,Nishida S,Matsuda H,Yoshikawa M

更新日期：2013-03-01 00:00:00

abstract：:The physiology of the oxytocin receptor has increasingly become a focus of scientific investigation due to its connection with social behavior and psychiatric disorders with impairments in social funciton. Experimental utilization of small molecule and peptide antagonists for the oxytocin receptor has played a role in...

journal_title：Bioorganic & medicinal chemistry

authors： Smith AL,Walum H,Connor-Stroud F,Freeman SM,Inoue K,Parr LA,Goodman MM,Young LJ

更新日期：2017-01-01 00:00:00

abstract：:Flavonoids are an interesting group of natural products ubiquitously present in human diet. Their consumption has been associated with various and differing beneficial health effects. However, several flavonoids have been reported to inhibit the breast cancer resistance protein (BCRP) encoded by the ABCG2 gene. Thus, ...

journal_title：Bioorganic & medicinal chemistry

authors： Pick A,Müller H,Mayer R,Haenisch B,Pajeva IK,Weigt M,Bönisch H,Müller CE,Wiese M

更新日期：2011-03-15 00:00:00

abstract：:Poly(ADP-ribose) glycohydrolase (PARG) plays an essential role in poly(ADP-ribose) (PAR) turnover, and thereby regulating DNA transactions, such as DNA repair, replication, transcription and recombination. Here, we examined the inhibitory activities of 6-hydroxy-3H-xanthene-3-one (HXO) derivatives and analyzed their b...

journal_title：Bioorganic & medicinal chemistry

authors： Shibui Y,Oyama T,Okazawa M,Yoshimori A,Abe H,Uchiumi F,Tanuma SI

更新日期：2020-02-01 00:00:00

abstract：:The synthesis of a neoglycopeptide building block is described. The key step is a cycloaddition where the chemistry is orthogonal to standard glycosyl transfer methodology. Also described is some exploratory chemistry of the building block. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bartolozzi A,Li B,Franck RW

更新日期：2003-07-03 00:00:00

abstract：:Use of herbal plant remedies to treat infectious diseases is a common practice in many countries in traditional and alternative medicine. However to date there are only few antimicrobial agents derived from botanics. Based on microbiological screening tests of crude plant extracts we identified four compounds derived ...

journal_title：Bioorganic & medicinal chemistry

authors： Artini M,Papa R,Barbato G,Scoarughi GL,Cellini A,Morazzoni P,Bombardelli E,Selan L

更新日期：2012-01-15 00:00:00

abstract：:Compound libraries comprise an integral component of drug discovery in the pharmaceutical and biotechnology industries. While in-house libraries often contain millions of molecules, this number pales in comparison to the accessible space of drug-like molecules. Therefore, care must be taken when adding new compounds t...

journal_title：Bioorganic & medicinal chemistry

authors： An Y,Sherman W,Dixon SL

更新日期：2012-09-15 00:00:00

abstract：:The most common lysosomal storage disorder, Gaucher disease, is caused by inefficient folding and trafficking of certain variants of lysosomal beta-glucosidase (beta-Glu, also known as beta-glucocerebrosidase). Recently, Sawker et al. reported that the addition of subinhibitory concentrations (10 microM) of the pharma...

journal_title：Bioorganic & medicinal chemistry

authors： Yu L,Ikeda K,Kato A,Adachi I,Godin G,Compain P,Martin O,Asano N

更新日期：2006-12-01 00:00:00

abstract：:In analogy to antiviral acyclic nucleoside phosphonates, a series of 5-amino-3-oxo-1,2,4-thiadiazol-3(2H)-ones bearing a 2-phosphonomethoxyethyl (PME) or 3-hydroxy-2-(phosphonomethoxy)propyl (HPMP) group at the position 2 of the heterocyclic moiety has been synthesized. Diisopropyl esters of PME- and HPMP-amines have ...

journal_title：Bioorganic & medicinal chemistry

authors： Pomeislová A,Otmar M,Rubešová P,Benýšek J,Matoušová M,Mertlíková-Kaiserová H,Pohl R,Poštová Slavětínská L,Pomeisl K,Krečmerová M

更新日期：2021-01-06 00:00:00

abstract：:A concise and efficient synthesis of cyclopentitols as a scaffold for a two-dimensional compound library for drug discovery is described. Starting from d-mannose, the key steps are Wittig olefination and ring-closing metathesis (RCM) followed by a [3,3]-sigmatropic Overmann rearrangement to form an sp(3)-rich, natural...

journal_title：Bioorganic & medicinal chemistry

authors： Padwal JD,Filippov DV,Narhe BD,Aertssen S,Beuving RJ,Benningshof JC,van der Marel GA,Overkleeft HS,van der Stelt M

更新日期：2015-06-01 00:00:00

abstract：:Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. In vertebrates, the hh gene encodes three different unique proteins: sonic hedgehog (Shh), desert hedgehog (Dhh) and indian hedgehog (Ihh). Disruption of the Hh signaling pathway leads to severe dis...

journal_title：Bioorganic & medicinal chemistry

authors： Büttner A,Seifert K,Cottin T,Sarli V,Tzagkaroulaki L,Scholz S,Giannis A

更新日期：2009-07-15 00:00:00

abstract：:Synthetic derivatives of 1,4-benzoxazin-3-ones have been shown to possess promising antimicrobial activity, whereas their natural counterparts were found lacking in this respect. In this work, quantitative structure-activity relationships (QSAR) of natural and synthetic 1,4-benzoxazin-3-ones as antimicrobials were est...

journal_title：Bioorganic & medicinal chemistry

authors： de Bruijn WJC,Hageman JA,Araya-Cloutier C,Gruppen H,Vincken JP

更新日期：2018-12-15 00:00:00