abstract：:The activity of 17 beta-HSD type 1, the enzyme that converts estrone into its more potent metabolite estradiol, has been demonstrated in all classical steroidogenic tissues and almost all peripheral tissues from both rat and human. Since 17 beta-HSD is one of the most important enzymes involved in active steroid hormo...

journal_title：Bioorganic & medicinal chemistry

authors： Tremblay MR,Auger S,Poirier D

更新日期：1995-05-01 00:00:00

abstract：:Structure-activity relationship study and in vitro biochemical studies with human leukocyte elastase, cathepsin G and proteinase 3 were conducted using a series of succinimide derivatives. ...

journal_title：Bioorganic & medicinal chemistry

authors： Groutas WC,Brubaker MJ,Chong LS,Venkataraman R,Huang H,Epp JB,Kuang R,Hoidal JR

更新日期：1995-04-01 00:00:00

abstract：:We have prepared three conformationally restricted analogs of DuP753 in which one of the phenyl rings in the biphenyl moiety is fused to the imidazole ring, and have investigated the conformation-biological activity relationship of these compounds. Conformational analysis on DuP753 and these compounds confirms that a ...

journal_title：Bioorganic & medicinal chemistry

authors： Yoo SE,Shin YA,Lee SH,Kim NJ

更新日期：1995-03-01 00:00:00

abstract：:The pH-rate profile for the hydrolysis of 3'-phosphoadenosine 5'-phosphosulfate (PAPS) in aqueous solution has been measured. Comparison with other data suggests that hydrolysis occurs by almost complete unimolecular elimination of sulfur trioxide, with weak involvement of a molecule of water in the transition state. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bedford CT,Kirby AJ,Logan CJ,Drummond JN

更新日期：1995-02-01 00:00:00

abstract：:The chemistries of S-nitroso-DL-penicillamine (SNAP) and S-nitrosoglutathione (GSNO) in relation to their ability to relax vascular smooth muscle and prevent platelet aggregation have been investigated. Metal ion catalysis greatly accelerates the decomposition of SNAP, but has little effect on GSNO. Instead, NO releas...

journal_title：Bioorganic & medicinal chemistry

authors： Askew SC,Butler AR,Flitney FW,Kemp GD,Megson IL

更新日期：1995-01-01 00:00:00

abstract：:A series of beta-chloroethylamines, structural hybrids of WB 4101, a competitive alpha 1-adrenoreceptor antagonist, and phenoxybenzamine, an irreversible alpha-adrenoreceptor antagonist, has been synthesized and tested in isolated rat vas deferens alpha-adrenoreceptors. Although, for all compounds, apparent blocking p...

journal_title：Bioorganic & medicinal chemistry

authors： Giardinà D,Crucianelli M,Marucci G,Paparelli F,Melchiorre C

更新日期：1995-01-01 00:00:00

abstract：:Both the enantiomeric forms of DAU 5750, a novel muscarinic receptor antagonist, have been synthesized in order to assess the relevance of configurational/conformational features for high affinity binding to muscarinic receptor subtypes. The attribution of absolute stereochemistry and conformational analysis by means ...

journal_title：Bioorganic & medicinal chemistry

authors： Turconi M,Gozzo A,Schiavi G,Fronza G,Mele A,Bravo P

更新日期：1994-12-01 00:00:00

abstract：:A systematic synthesis of the N-methyl-1-deoxynojirimycin-containing oligosaccharides related to the Lewis x, Lewis a, sialyl-Lewis x and sialyl-Lewis a antigens has been achieved. The couplings of the suitably protected 1-deoxynojirimycin derivative 10 with methyl-1-thioglycosides (glycosyl donors) of L-fucose (11), ...

journal_title：Bioorganic & medicinal chemistry

authors： Kiso M,Furui H,Ando K,Ishida H,Hasegawa A

更新日期：1994-11-01 00:00:00

abstract：:The application of glycosyltransferases to the chemoenzymatic synthesis of neoglycosphingolipids and lipid-linked oligosaccharides allows the regio- and stereoselective formation of glycosidic bonds. In our laboratory galactosyl-, sialyl-, and fucosyltransferases have been used to assemble oligosaccharide headgroups d...

journal_title：Bioorganic & medicinal chemistry

authors： Flitsch SL,Goodridge DM,Guilbert B,Revers L,Webberley MC,Wilson IB

更新日期：1994-11-01 00:00:00

abstract：:Semiempirical quantum mechanical and molecular mechanics calculations were carried out to identify and characterize the steric and electronic properties that modulate ligand recognition and activation of the cerebellar GABAA/benzodiazepine (BDZ) receptor. For this hypothesis development, thirteen compounds belonging t...

journal_title：Bioorganic & medicinal chemistry

authors： Schove LT,Perez JJ,Loew GH

更新日期：1994-10-01 00:00:00

abstract：:A structural survey of protein Zn2+ binding geometries was instigated based upon the functional requirement of Ras farnesyltransferase for Zn2+. The Cys-X-X-Cys motif found in Zn(2+)-binding proteins such as aspartate transcarbamylase was used as a template to devise a bidentate-coordination model for Cys-A1-A2-X pept...

journal_title：Bioorganic & medicinal chemistry

authors： Marsters JC Jr,McDowell RS,Reynolds ME,Oare DA,Somers TC,Stanley MS,Rawson TE,Struble ME,Burdick DJ,Chan KS

更新日期：1994-09-01 00:00:00

abstract：:Electronic parameters (molecular electrostatic potential MEP, charge distribution on the nitrogen atoms, dipole moment mu and ionization potential IP) were calculated by semiempirical quantum chemistry methods for 2 sets (X = H and m-CF3, the syn- and anti-rotamers of the latter being considered separately) of the 6-a...

journal_title：Bioorganic & medicinal chemistry

authors： Karolak-Wojciechowska J,Lange J,Kwiatkowski W,Gniewosz M,Plenkiewicz J

更新日期：1994-08-01 00:00:00

abstract：:Aromatic alpha-amino-alpha-methyl acids and alpha-hydrazino-alpha-methyl acids are known aromatic amino acid decarboxylase inhibitors. Specific derivatives such as 2-amino-2-methyl-3-(3,4- dihydroxyphenyl)propanoate, Aldomet, and 2-hydrazino-2-methyl-3-(3,4- dihydroxyphenyl)propanoate, Lodosyn, have been developed as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kallwass HK,Yee C,Blythe TA,McNabb TJ,Rogers EE,Shames SL

更新日期：1994-07-01 00:00:00

abstract：:An efficient technique is presented which integrates cofactor dependent enzymic phosphorylation and dehydrogenation into a single, closed-loop system by employing phosphoenolpyruvate as the sacrificial reagent for sequential ATP and NAD+ recycling steps. Exemplary applications are developed for the synthesis of 6-phos...

journal_title：Bioorganic & medicinal chemistry

authors： Fessner WD,Sinerius G

更新日期：1994-07-01 00:00:00

abstract：:The bacterial strain Rhodococcus butanica (ATCC 21197), which exhibits nitrilase and nitrile hydratase/amidase activities, catalyses the enantioselective hydrolysis of racemic naproxen nitrile (R/S)-1 to furnish a moderate enantiomeric excess of (S)-naproxen (S)-3. Racemic naproxen amide (R/S)-2 is not a good substrat...

journal_title：Bioorganic & medicinal chemistry

authors： Effenberger F,Böhme J

更新日期：1994-07-01 00:00:00

abstract：:Racemic ethyl 2-benzyl-3-(tert-butylsulfonyl)propionate (1) and racemic ethyl 2-benzyl-3-[[1-methyl-1-((morpholin-4-yl)carbonyl)ethyl]sulfonyl] propionate (3) were enantioselectively hydrolyzed by subtilisin Carlsberg generating the respective (S)-acids used as building blocks for renin inhibitors. The esters were rea...

journal_title：Bioorganic & medicinal chemistry

authors： Doswald S,Estermann H,Kupfer E,Stadler H,Walther W,Weisbrod T,Wirz B,Wostl W

更新日期：1994-06-01 00:00:00

abstract：:The enzyme acetylesterase from the flavedo of oranges (EC 3.1.1.6) can advantageously be applied for the chemo- and regioselective deprotection of different types of carbohydrates. It displays a selectivity which in many cases is complementary to the application of other biocatalysts or classical chemical methods. ...

journal_title：Bioorganic & medicinal chemistry

authors： Waldmann H,Heuser A

更新日期：1994-06-01 00:00:00

abstract：:The synthesis of the ethylenediamine-connected cyclodextrin dimer is reported, together with the syntheses of several reference cyclodextrinylamines. Each compound displayed enhanced transacylation or transphosphorylation of activated substrates, with the primary amine-bearing monocyclodextrin compound showing the gre...

journal_title：Bioorganic & medicinal chemistry

authors： Beeson JC,Czarnik AW

更新日期：1994-04-01 00:00:00

abstract：:Bilirubin, biliverdin and their serum albumin complexes were tested as oxyradical scavengers (superoxide generated by the xanthine/xanthine oxidase system and peroxyl radical-trapping antioxidant ability). As superoxide scavengers the free bile pigments showed activities near to that of serum albumin, higher than the ...

journal_title：Bioorganic & medicinal chemistry

authors： Farrera JA,Jaumà A,Ribó JM,Peiré MA,Parellada PP,Roques-Choua S,Bienvenue E,Seta P

更新日期：1994-03-01 00:00:00

abstract：:Two types of structural variants of D-myo-inositol 1,4,5-trisphosphate [Ins(1,4,5)P3] were prepared by a chemoenzymatic route. These 6-O-substituted analogues retained the biological activity of Ins(1,4,5)P3, and were able to elicit Ca2+ release from porcine brain microsomes. Moreover, these derivatives allowed the pr...

journal_title：Bioorganic & medicinal chemistry

authors： Gou DM,Shieh WR,Lu PJ,Chen CS

更新日期：1994-01-01 00:00:00

abstract：:A facile synthesis of dl-6,10,14-trimethylpentadecan-2-ol (1) a pheromone component of rice moth, Corcyra cephalonica Stainton and 5,9,13-trimethyltetradecanoic acid (2) a component of marine sponge, Cinachyrella alloclada Uliczka, using a common, intermediate, hexahydrofarnesol is accomplished. The salient features f...

journal_title：Bioorganic & medicinal chemistry

authors： Rane SS,Chadha MS,Mamdapur VR

更新日期：1993-12-01 00:00:00

abstract：:We have prepared a series of potent antihypertensive 1-benzazepin-2-one calcium channel blockers (CCBs) 1 that are structurally related to diltiazem 2. Structural studies and the preparation of conformationally constrained analogs of 1-benzazepin-2-ones have led us to postulate a receptor-bound conformation for both 1...

journal_title：Bioorganic & medicinal chemistry

authors： Kimball SD,Hunt JT,Barrish JC,Das J,Floyd DM,Lago MW,Lee VG,Spergel SH,Moreland S,Hedberg SA

更新日期：1993-10-01 00:00:00

abstract：:Three soft drug analogs and a metabolite of methatropine based on phenylsuccinic structural moiety were synthesized and tested for activity. In an in vivo assay, the soft drugs were found to be two orders of magnitude less potent than methatropine while the carboxylate metabolite was found to be one order of magnitude...

journal_title：Bioorganic & medicinal chemistry

authors： Hammer RH,Gunes E,Kumar GN,Wu WM,Srinivasan V,Bodor NS

更新日期：1993-09-01 00:00:00

abstract：:(R)-Recifeiolide, a naturally occurring macrolactone, was synthesized in optically pure form by the aid of biocatalysts. Lipase-catalyzed lactonization of the racemic precursor afforded the desired compound with a concomitant kinetic resolution. The optically active acyclic precursor could be synthesized by the reduct...

journal_title：Bioorganic & medicinal chemistry

authors： Mochizuki N,Yamada H,Sugai T,Ohta H

更新日期：1993-07-01 00:00:00