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：:Three series of new N-substituted 1,2,3,4-tetrahydroisoquinolines with 2-, 3-, and 4-membered alkyl chains (a, b, and c, respectively) were synthesized, and the effect of some structural modifications on their 5-HT1A receptor affinities and functional properties was discussed. It was found that the volume of the termi...

journal_title：Bioorganic & medicinal chemistry

authors： Mokrosz MJ,Bojarski AJ,Duszyńska B,Tatarczyńska E,Kłodzińska A,Dereń-Wesołek A,Charakchieva-Minol S,Chojnacka-Wójcik E

更新日期：1999-02-01 00:00:00

abstract：:The effect of 7,8-diacetoxy-4-methylcoumarin (DAMC) has been studied on hepatic NADPH cytochrome C reductase-- an enzyme participating in the microsomal electron transport. The preincubation of liver microsomes with DAMC resulted in a time-dependent activation of NADPH cytochrome C reductase. The catalytic activity of...

journal_title：Bioorganic & medicinal chemistry

authors： Raj HG,Parmar VS,Jain SC,Goel S,Singh A,Tyagi YK,Jha HN,Olsen CE,Wengel J

更新日期：1999-02-01 00:00:00

abstract：:Recent knowledge about the determinants of beta-sheet formation and stability has notably been improved by the structural analysis of model peptides with beta-hairpin structure in aqueous solution. Several experimental studies have shown that the turn region residues can not only determine the stability, but also the ...

journal_title：Bioorganic & medicinal chemistry

authors： Ramírez-Alvarado M,Kortemme T,Blanco FJ,Serrano L

更新日期：1999-01-01 00:00:00

abstract：:A novel series of indole and benzimidazole derivatives were synthesized and evaluated for their inhibitory activity of rat prostatic 5alpha-reductase. Among these compounds, 4-¿2-[1-(4,4'-dipropylbenzhydryl)indole-5-carboxamido]phenoxy¿buty ric acid (15) and its benzimidazole analogue 25 showed potent inhibitory activ...

journal_title：Bioorganic & medicinal chemistry

authors： Takami H,Kishibayashi N,Ishii A,Kumazawa T

更新日期：1998-12-01 00:00:00

abstract：:A tetracyclic, conformationally constrained analogue of delta8-THC (2) has been synthesized in which a two carbon bridge exists between C2 and C2'. Two conceptually related syntheses of 2 are described, both of which employ 5,7-dimethoxy-4-oxo-1,2,3,4-tetrahydronaphthoic acid (11) as starting material. This substrate ...

journal_title：Bioorganic & medicinal chemistry

authors： Huffman JW,Yu S

更新日期：1998-12-01 00:00:00

abstract：:Our present report deals with the preparation of hitherto unreported 7-([carbonyl-14C]-acetyl)paclitaxel 4 and two new bioactive 7-substituted fluorescent taxoids (FITC 9 and rhodamine 11), as well as evaluation towards their applications as biological probes. The results in this report demonstrate that (a) the new pa...

journal_title：Bioorganic & medicinal chemistry

authors： Rao CS,Chu JJ,Liu RS,Lai YK

更新日期：1998-11-01 00:00:00

abstract：:The high-pressure Diels-Alder reaction of N-carbomethyoxypyrroles and phenyl vinyl sulfone affords versatile intermediates for the palladium-catalyzed preparation of new epibatidine analogues. Structure-activity relationships of new epibatidine analogues are presented. High affinities of Ki = 0.81 and 2.6 nM for the [...

journal_title：Bioorganic & medicinal chemistry

authors： Seerden JP,Tulp MT,Scheeren HW,Kruse CG

更新日期：1998-11-01 00:00:00

abstract：:A new brassinolide inhibitor, named KM-01, was isolated from the culture filtrates of two fungal species, Drechslera avenae and Pycnoporus coccineus, and the structure with absolute stereochemistry was elucidated as the fatty acid ester of an eremophilane sesquiterpene, bipolaroxin, based on spectroscopic analysis, ch...

journal_title：Bioorganic & medicinal chemistry

authors： Kim SK,Hatori M,Ojika M,Sakagami Y,Marumo S

更新日期：1998-11-01 00:00:00

abstract：:We examined effects of alpha-, beta-galactosylceramides (CalCers) and alpha-, beta-glucosylceramides (GlcCers) on the syngeneic mixed leukocyte reaction (MLR) using spleen cells (responder cells) and dendritic cells (DC, stimulator cells). The DC pretreated with these alpha-monoglycosylceramides markedly stimulated th...

journal_title：Bioorganic & medicinal chemistry

authors： Iijima H,Kimura K,Sakai T,Uchimura A,Shimizu T,Ueno H,Natori T,Koezuka Y

更新日期：1998-10-01 00:00:00

abstract：:Protein-tyrosine phosphatase (PTP) inhibitors are attractive as potential signal transduction-directed therapeutics which may be useful in the treatment of a variety of diseases. We have previously reported the X-ray structure of 1,1-difluoro-1-(2-naphthalenyl)methyl] phosphonic acid (4) complexed with the human the p...

journal_title：Bioorganic & medicinal chemistry

authors： Yao ZJ,Ye B,Wu XW,Wang S,Wu L,Zhang ZY,Burke TR Jr

更新日期：1998-10-01 00:00:00

abstract：:Some epimeric 20-hydroxy, 20-oxime, 16 alpha, 17 alpha-, 17,20- and 20,21-aziridine derivatives of progesterone were synthesized and evaluated as inhibitors of human 17 alpha-hydroxylase/C17,20-lyase (P450(17) alpha) and 5 alpha-reductase (5 alpha-R). The reduction of 16-dehydropregenolone acetate (3a) was reinvestiga...

journal_title：Bioorganic & medicinal chemistry

authors： Ling YZ,Li JS,Kato K,Liu Y,Wang X,Klus GT,Marat K,Nnane IP,Brodie AM

更新日期：1998-10-01 00:00:00

abstract：:The indolocarbazole antibiotics staurosporine and rebeccamycin (1) are potent antitumor drugs targeting protein kinase C and topoisomerase I, respectively. To obtain staurosporine analogues from rebeccamycin, different structural modifications were performed: coupling of the sugar moiety to the second indole nitrogen,...

journal_title：Bioorganic & medicinal chemistry

authors： Anizon F,Moreau P,Sancelme M,Voldoire A,Prudhomme M,Ollier M,Sevère D,Riou JF,Bailly C,Fabbro D,Meyer T,Aubertin AM

更新日期：1998-09-01 00:00:00

abstract：:The conformational profiles of a selected group of a new series of small linear and cyclic penta- and hexapeptides, inspired on the C-terminal segment of second-generation bradykinin (BK) antagonists, were independently computed in order to assess the chemical and geometrical requirements necessary for BK antagonism. ...

journal_title：Bioorganic & medicinal chemistry

authors： Filizola M,Llorens O,Cartení-Farina M,Perez JJ

更新日期：1998-09-01 00:00:00

abstract：:The proteolytic release, or shedding, of a cell surface protein can serve a regulatory role; the process liberates a soluble form of the protein into circulation while downregulating its cell surface concentration. The characteristics that render a protein susceptible to proteolytic cleavage are not known. We hypothes...

journal_title：Bioorganic & medicinal chemistry

authors： Gordon EJ,Strong LE,Kiessling LL

更新日期：1998-08-01 00:00:00

abstract：:The substitution of the sterically hindered carbon of the potent thyroid hormone agonist, GC-1, was effected by a reaction based on the solvolysis of the benzylic hydroxyl group. The reaction was found to proceed in high yield with a variety of nucleophiles including alcohols, thiols, allyl silanes and electron-rich a...

journal_title：Bioorganic & medicinal chemistry

authors： Yoshihara HA,Chiellini G,Mitchison TJ,Scanlan TS

更新日期：1998-08-01 00:00:00

abstract：:The design, synthesis, and biological evaluation of a series of pyrrole and pyrazole congeners 2 of suramin, directed toward the development and identification of new ligands that complex the human fibroblast growth factor (bFGF), thereby inhibiting tumor-promoted angiogenesis, is reported. Compounds 2 were evaluated ...

journal_title：Bioorganic & medicinal chemistry

authors： Manetti F,Cappello V,Botta M,Corelli F,Mongelli N,Biasoli G,Borgia AL,Ciomei M

更新日期：1998-07-01 00:00:00

abstract：:We have previously found that T22 ([Tyr(5,12), Lys7]-polyphemusin II) has strong anti-human immunodeficiency virus (HIV) activity, and that T22 inhibits T cell-line-tropic HIV-1 infection mediated by CXCR4/fusin. T22 is an 18-residue peptide amide, which takes an antiparallel beta-sheet structure that is maintained by...

journal_title：Bioorganic & medicinal chemistry

authors： Tamamura H,Imai M,Ishihara T,Masuda M,Funakoshi H,Oyake H,Murakami T,Arakaki R,Nakashima H,Otaka A,Ibuka T,Waki M,Matsumoto A,Yamamoto N,Fujii N

更新日期：1998-07-01 00:00:00

abstract：:This review summarises current knowledge on adenosine receptors, an important G protein-coupled receptor. The four known adenosine receptor subtypes A1, A2A, A2B, and A3 are discussed with special reference to the opportunities for drug development. ...

journal_title：Bioorganic & medicinal chemistry

authors： Poulsen SA,Quinn RJ

更新日期：1998-06-01 00:00:00

abstract：:3-(4-Piperidinyl)-5-arylpyrazoles, such as 1, were selective for the cloned human dopamine D4 receptor (hD4), but also showed affinity at voltage sensitive calcium, sodium and potassium ion channels. A combination of substituent changes to reduce the basicity of the piperidine nitrogen and conformational restriction t...

journal_title：Bioorganic & medicinal chemistry

authors： Collins I,Rowley M,Davey WB,Emms F,Marwood R,Patel S,Patel S,Fletcher A,Ragan IC,Leeson PD,Scott AL,Broten T

更新日期：1998-06-01 00:00:00

abstract：:The intestinal absorption of an intact oligopeptide was investigated in rats using a synthetic cationic peptide, 001-C8 (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH2). The peptide was coupled with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) to prepare a fluorescence-labeled derivative 001-C8-NBD (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH-NB...

journal_title：Bioorganic & medicinal chemistry

authors： Sai Y,Kajita M,Tamai I,Kamata M,Wakama J,Wakamiya T,Tsuji A

更新日期：1998-06-01 00:00:00

abstract：:Continuing work on the bioactivity-directed fractionation of the bark of Annona squamosa has resulted in the discovery of three new Annonaceous acetogenins, (2,4-cis and trans)-squamolinone (1), (2,4-cis and trans)-9-oxoasimicinone (2), and bullacin B (3). Compounds 1-3 are all adjacent bis-THF ring acetogenins with 2...

journal_title：Bioorganic & medicinal chemistry

authors： Hopp DC,Alali FQ,Gu ZM,McLaughlin JL

更新日期：1998-05-01 00:00:00

abstract：:T22 ([Tyr5,12,Lys7]-polyphemusin II) has been shown to have strong anti-human immunodeficiency virus (HIV) activity comparable to that of 3'-azido-2',3'-dideoxythymidine (AZT). T22, an 18-residue peptide amide, takes an antiparallel beta-sheet structure that is maintained by two disulfide bridges. Herein we synthesize...

journal_title：Bioorganic & medicinal chemistry

authors： Tamamura H,Waki M,Imai M,Otaka A,Ibuka T,Waki K,Miyamoto K,Matsumoto A,Murakami T,Nakashima H,Yamamoto N,Fujii N

更新日期：1998-04-01 00:00:00

abstract：:Deoxyhypusine synthase catalyzes the first step in the posttranslational biosynthesis of the unusual amino acid hypusine [N epsilon-(4-amino-2-hydroxybutyl)lysine] in eukaryotic translation initiation factor 5A (eIF-5A). eIF-5A and its single hypusine residue are essential for cell proliferation. Two series of 1,7-dia...

journal_title：Bioorganic & medicinal chemistry

authors： Lee YB,Folk JE

更新日期：1998-03-01 00:00:00

abstract：:The synthesis of a series of 2,4-disubstituted morpholines is described and their affinities at human dopamine receptors reported. The orally bioavailable 7-azaindole compound 11 has nanomolar affinity at the hD4 receptor with > 1000-fold selectivity over the hD2 receptor. ...

journal_title：Bioorganic & medicinal chemistry

authors： Showell GA,Emms F,Marwood R,O'Connor D,Patel S,Leeson PD

更新日期：1998-01-01 00:00:00

abstract：:Highly chemo- and regioselective de-esterification has been observed in the deacetylation of peracetylated enolic forms of polyphenolic benzyl phenyl ketones by lipase from porcine pancreas (PPL) suspended in tetrahydrofuran (THF). The enzyme selectively deacetylates the enolic acetoxy over the phenolic acetoxy group(...

journal_title：Bioorganic & medicinal chemistry

authors： Parmar VS,Pati HN,Azim A,Kumar R,Himanshu,Bisht KS,Prasad AK,Errington W

更新日期：1998-01-01 00:00:00

abstract：:2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide was synthesized and evaluated for in vitro/in vivo antagonistic activity at the strychnine insensitive glycine binding site on the NMDA receptor revealing it to be a useful tool to evaluate the effectiveness of glycine antagonists in vivo. ...

journal_title：Bioorganic & medicinal chemistry

authors： Micheli F,Cugola A,Donati D,Missio A,Pecunioso A,Reggiani A,Tarzia G

更新日期：1997-12-01 00:00:00

abstract：:The synthesis and binding affinities of 32 X3Gly4 dual-substitution analogues of the natural opioid heptapeptides deltorphin I and II are reported. A multiple regression QSAR analysis was performed using those results along with literature data for the X3Asp4 and Phe3X4 side chain analogues. Fitting to a three-term po...

journal_title：Bioorganic & medicinal chemistry

authors： Schullery SE,Mohammedshah T,Makhlouf H,Marks EL,Wilenkin BS,Escobar S,Mousigian C,Heyl DL

更新日期：1997-12-01 00:00:00

abstract：:For the purpose of rational modification of the TRH molecule, we were pursuing an approach that consists of two steps: (1) 'obligatory' replacement of histidine with glutamine in TRH and (2) the application of conformational constraints for putative bioactive conformation I stabilized by an intramolecular hydrogen bon...

journal_title：Bioorganic & medicinal chemistry

authors： Mazurov AA,Andronati SA,Korotenko TI,Sokolenko NI,Dyadenko AI,Shapiro YE,Gorbatyuk VYa,Voronina TA

更新日期：1997-11-01 00:00:00

abstract：:Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field. ...

journal_title：Bioorganic & medicinal chemistry

authors： Arredondo Y,Moreno-Mañas M,Pleixats R,Palacín C,Raga MM,Castelló JM,Ortiz JA

更新日期：1997-10-01 00:00:00

abstract：:The okadaic acid class of naturally occurring toxins is a structurally diverse group of molecules that inhibit the protein phosphatases PP1 and PP2A. Studies providing information about the mode of binding between the toxins and the phosphatases contribute to an overall understanding of the signal transduction pathway...

journal_title：Bioorganic & medicinal chemistry

authors： Sheppeck JE 2nd,Gauss CM,Chamberlin AR

更新日期：1997-09-01 00:00:00

abstract：:The synthesis of N-[7-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl) -6-formyl-1-oxo-heptyl]-L-glutamic acid (2, abenzyl 10-formyl-5,8,10-trideazafolic acid) as a potential enzyme-assembled tight binding inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) or aminoimidazole carboxamide ribonucleotide transf...

journal_title：Bioorganic & medicinal chemistry

authors： Boger DL,Haynes NE,Warren MS,Ramcharan J,Marolewski AE,Kitos PA,Benkovic SJ

更新日期：1997-09-01 00:00:00

abstract：:2-Guanadino-3-cyanopyridines 8-33 and pyrido[2,3-d]-pyrimidines 35-52 were synthesized by nucleophilic displacement and cyclization of the chloroamidines 6a-d easily obtained by reaction of 2-aminocyanopyridines 5a-d with phosgene iminium chloride and their action on the release of histamine by mast cells examined und...

journal_title：Bioorganic & medicinal chemistry

authors： Quintela JM,Peinador C,Botana L,Estévez M,Riguera R

更新日期：1997-08-01 00:00:00

abstract：:The synthesis and in vitro antibacterial activity of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido] cephalosporins bearing various 2-alkyl-3-aminopyrazolium groups at the 3-position are described. Antibacterial activity against MRSA was affected by the nature of the substituent at the 2-position on the 3...

journal_title：Bioorganic & medicinal chemistry

authors： Ohki H,Kawabata K,Inamoto Y,Okuda S,Kamimura T,Sakane K

更新日期：1997-08-01 00:00:00

abstract：:An iduronic acid-containing trisaccharide, methyl-O-(4-O-methyl-2,3,6-tri-O-sulfo-alpha-D-glucopyranosyl-(1-->4)-O- (2-O-sulfo-alpha-L-idopyranosyluronic acid)-(1-->4)-O-2,6-di-O-sulfo-alpha-D-glucopyranoside, related to antithrombotic heparin fragments has been subjected to a combined NMR and molecular modeling inves...

journal_title：Bioorganic & medicinal chemistry

authors： Cros S,Petitou M,Sizun P,Pérez S,Imberty A

更新日期：1997-07-01 00:00:00

abstract：:In order to study structure-activity relationships of the previously reported dual histamine H2 and gastrin receptor antagonists and also to improve their low oral absorbability, we tried two chemical modifications. One tried to decrease the high hydrophobicity of the parent hybrid compounds to an appropriate level by...

journal_title：Bioorganic & medicinal chemistry

authors： Kawanishi Y,Ishihara S,Tsushima T,Hagishita S,Ishikawa M,Ishihara Y

更新日期：1997-07-01 00:00:00

abstract：:RNA stem-loop microhelices with helix sequences based on tRNA acceptor stems can be charged with specific amino acids. Experiments were designed to test the possibility that microhelices could laterally associate through complementary loop sequences and thereby bring their attached aminoacyl groups close enough togeth...

journal_title：Bioorganic & medicinal chemistry

authors： Henderson BS,Schimmel P

更新日期：1997-06-01 00:00:00

abstract：:Selective targeting of RNA has become a recent priority in drug design strategies due to the emergence of retroviruses, the need for new antibiotics to counter drug resistance, and our increased awareness of the essential role RNA and RNA structures play in the progression of disease. Most organic compounds known to s...

journal_title：Bioorganic & medicinal chemistry

authors： Li K,Fernandez-Saiz M,Rigl CT,Kumar A,Ragunathan KG,McConnaughie AW,Boykin DW,Schneider HJ,Wilson WD

更新日期：1997-06-01 00:00:00

abstract：:The boranophosphate ester nucleotides are a new class of nucleic acid analogues that are isoelectronic and isostructural to normal phosphodiester nucleic acids and that maintain the anionic charge of the nucleic acid backbone. The two P-diastereoisomers of dithymidine boranomonophosphates were separated using reverse ...

journal_title：Bioorganic & medicinal chemistry

authors： Li H,Huang F,Shaw BR

更新日期：1997-05-01 00:00:00

abstract：:A series of the 9-acetoxy enediyne compounds, 6a-k which were simplified from natural dynemicin A, and designed to be equipped with various aryl carbamate moieties, was synthesized and evaluated for DNA-cleaving ability, in vitro cytotoxicity, and in vivo antitumor activity. As a result of this study of the structure-...

journal_title：Bioorganic & medicinal chemistry

authors： Unno R,Michishita H,Inagaki H,Suzuki Y,Baba Y,Jomori T,Nishikawa T,Isobe M

更新日期：1997-05-01 00:00:00