Studies on some derivatives of oxamniquine.

abstract：:Optimization of the pharmacokinetic properties for a series of benzoxazolone derivatives led to the identification of 9b, which showed anxiolytic effect in a rat model. However, 9b, like known benzodiazepines, induced motor impairment. Investigation into the cause of this unexpected side effect and management of 9b of...

journal_title：Journal of medicinal chemistry

authors： Fukaya T,Ishiyama T,Baba S,Masumoto S

更新日期：2013-10-24 00:00:00

abstract：:A series of analogues of Pro-Leu-Gly-NH2 (PLG) in which the leucine residue has been replaced with the aliphatic amino acids L-isoleucine, L-2-aminohexanoic acid (Ahx), L-2-aminopentanoic acid, and L-2-aminobutanoic acid and the aromatic amino acids L-phenylalanine, L-phenylglycine, L- and D-2-amino-4-phenylbutanoic a...

journal_title：Journal of medicinal chemistry

authors： Johnson RL,Bontems RJ,Yang KE,Mishra RK

更新日期：1990-06-01 00:00:00

abstract：:Thiolactomycin inhibits bacterial cell growth through inhibition of the beta-ketoacyl-ACP synthase activity of type II fatty acid synthases. The effect of modifications of the 5-position isoprenoid side chain on both IC(50) and MIC were determined. Synthesis and screening of a structurally diverse set of 5-position an...

journal_title：Journal of medicinal chemistry

authors： Kim P,Zhang YM,Shenoy G,Nguyen QA,Boshoff HI,Manjunatha UH,Goodwin MB,Lonsdale J,Price AC,Miller DJ,Duncan K,White SW,Rock CO,Barry CE 3rd,Dowd CS

更新日期：2006-01-12 00:00:00

abstract：:A series of the anti-HIV nucleoside conjugates of either (1-O-alkyl) and thioether (1-S-alkyl) lipids linked by a pyrophosphate diester bond has been synthesized as micelle-forming prodrugs of the nucleosides to improve their therapeutic efficiency. These include AZT 5'-diphosphate-rac-1-S-octadecyl-2-O-palmitoyl-1-th...

journal_title：Journal of medicinal chemistry

authors： Hong CI,Nechaev A,Kirisits AJ,Vig R,West CR,Manouilov KK,Chu CK

更新日期：1996-04-26 00:00:00

abstract：:A series of O-alkylated analogs of 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-c]azepin-3-ol (THAO) were synthesized and characterized as ligands for muscarinic acetylcholine receptors (mAChRs). O-Methyl-THAO (4a), O-ethyl-THAO (4b), O-isopropyl-THAO (4c), and O-propargyl-THAO (4d) were shown to be potent inhibitors of the bi...

journal_title：Journal of medicinal chemistry

authors： Bräuner-Osborne H,Ebert B,Brann MR,Falch E,Krogsgaard-Larsen P

更新日期：1995-06-09 00:00:00

abstract：:In 1869, Crum Brown discovered the first structure-activity link by showing that alkaloids, even convulsive ones, were converted by N-methylation to muscle relaxants resembling curarine (itself a quaternary amine). This led to an attempt to link every type of drug action to its own cluster of atoms. This quest was jol...

journal_title：Journal of medicinal chemistry

authors： Albert A

更新日期：1982-01-01 00:00:00

abstract：:[4-Phenylalanine]oxytocin was prepared from Z-Cys(Bzl)-Tyr(Bzl)-Ile-Phe-Asn-Cys(Bzl)-Pro-Leu-Gly-NG2 (4) by deprotection with Na in NH3 followed by cyclization of the resulting disulfhydryl compound with ICH2CH2I. The protected peptide 4 was prepared from Boc-Asn-Cys(Bzl)-Pro-Leu-Gly-NH2 by the stepwise solution metho...

journal_title：Journal of medicinal chemistry

authors： Nestor JJ Jr,Ferger MF,Chan WY

更新日期：1975-10-01 00:00:00

abstract：:The synthesis of the benzothiopyranoindazoles, a new class of chromophore modified anthracenediones related to mitoxantrone, is described. In this structural class the quinone moiety, which is believed to be responsible for the cardiotoxicity of the anthracyclines, has been designed out. The synthesis of the benzothio...

journal_title：Journal of medicinal chemistry

authors： Showalter HD,Angelo MM,Berman EM,Kanter GD,Ortwine DF,Ross-Kesten SG,Sercel AD,Turner WR,Werbel LM,Worth DF

更新日期：1988-08-01 00:00:00

abstract：:In the course of further chemical modification of the novel antidiabetic pioglitazone (AD-4833, U-72,107), a series of 5-[4-(2- or 4-azolylalkoxy)benzyl- or -benzylidene]-2,4-thiazolidinediones was prepared and evaluated for hypoglycemic and hypolipidemic activities in insulin-resistant, genetically obese, and diabeti...

journal_title：Journal of medicinal chemistry

authors： Sohda T,Mizuno K,Momose Y,Ikeda H,Fujita T,Meguro K

更新日期：1992-07-10 00:00:00

abstract：:A series of trans-platinum(IV) complexes with functionalized aromatic carboxylate ligands, cis,cis,trans-Pt(NH3)2Cl2(CO2C6H4R)2 (R = H (3), p-vinyl (4), p-methoxy (5), p-iodo (6), p-cyano (7), or o-carboxyl (8)) was synthesized and characterized by spectroscopic methods. Crystal structures of 3, 4, 7, and 8 were obtai...

journal_title：Journal of medicinal chemistry

authors： Ang WH,Pilet S,Scopelliti R,Bussy F,Juillerat-Jeanneret L,Dyson PJ

更新日期：2005-12-15 00:00:00

abstract：:Four 11-(1-piperazinyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepines were prepared and evaluated as central nervous system agents. All were active psychotropic agents as determined by animal screening tests. The most interesting compound, 11-(1-piperazinyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine, showed dual activity as an ant...

journal_title：Journal of medicinal chemistry

authors： Wright WB Jr,Greenblatt EN,Day IP,Quinones NQ,Hardy RA Jr

更新日期：1980-04-01 00:00:00

abstract：:Learning and memory deficits in Alzheimer's disease (AD) result from synaptic failure and neuronal loss, the latter caused in part by excitotoxicity and oxidative stress. A therapeutic approach is described that uses NO-chimeras directed at restoration of both synaptic function and neuroprotection. 4-Methylthiazole (M...

journal_title：Journal of medicinal chemistry

authors： Qin Z,Luo J,VandeVrede L,Tavassoli E,Fa' M,Teich AF,Arancio O,Thatcher GR

更新日期：2012-08-09 00:00:00

abstract：:Caveolin-1 is a target for academic and pharmaceutical research due to its many cellular roles and associated diseases. We report peptide WL47 (1), a small, high-affinity, selective disrupter of caveolin-1 oligomers. Developed and optimized through screening and analysis of synthetic peptide libraries, ligand 1 has 75...

journal_title：Journal of medicinal chemistry

authors： Gilliam AJ,Smith JN,Flather D,Johnston KM,Gansmiller AM,Fishman DA,Edgar JM,Balk M,Majumdar S,Weiss GA

更新日期：2016-04-28 00:00:00

abstract：:The preparation of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid is described. This acid has good anti-inflammatory and analgesic activities without producing irritation in the gastrointestinal tract up to the highest tested dose. ...

journal_title：Journal of medicinal chemistry

authors： Boettcher I,Elger W,Kirsch G,Siegmund F,Wachtel H

更新日期：1984-03-01 00:00:00

abstract：:Acyl carrier protein synthase (AcpS) catalyzes the transfer of the 4'-phosphopantetheinyl group from the coenzyme A to a serine residue in acyl carrier protein (ACP), thereby activating ACP, an important step in cell wall biosynthesis. The structure-based design of novel anthranilic acid inhibitors of AcpS, a potentia...

journal_title：Journal of medicinal chemistry

authors： Joseph-McCarthy D,Parris K,Huang A,Failli A,Quagliato D,Dushin EG,Novikova E,Severina E,Tuckman M,Petersen PJ,Dean C,Fritz CC,Meshulam T,DeCenzo M,Dick L,McFadyen IJ,Somers WS,Lovering F,Gilbert AM

更新日期：2005-12-15 00:00:00

abstract：:Bitter thresholds of a total of 93 amino acids, peptides, and their derivatives were analyzed quantitatively by use of hydrophobicity parameters reported for amino acid side chains and those for the whole molecules estimated from partition coefficients obtained experimentally. We also explored the steric parameters th...

journal_title：Journal of medicinal chemistry

authors： Asao M,Iwamura H,Akamatsu M,Fujita T

更新日期：1987-10-01 00:00:00

abstract：:We have recently proposed a macromolecular prodrug strategy for improved cancer chemotherapy based on two features (Kratz, F.; et al. J. Med. Chem 2000, 43, 1253-1256.): (a) rapid and selective binding of thiol-reactive prodrugs to the cysteine-34 position of endogenous albumin after intravenous administration and (b)...

journal_title：Journal of medicinal chemistry

authors： Kratz F,Warnecke A,Scheuermann K,Stockmar C,Schwab J,Lazar P,Drückes P,Esser N,Drevs J,Rognan D,Bissantz C,Hinderling C,Folkers G,Fichtner I,Unger C

更新日期：2002-12-05 00:00:00

abstract：:Ring-constrained adenosine analogues have been designed to act as dual agonists at tissue-protective A(1) and A(3) adenosine receptors (ARs). 9-Ribosides transformed into the ring-constrained (N)-methanocarba-2-chloro-5'-uronamides consistently lost affinity at A(1)/A(2A)ARs and gained at A(3)AR. Among 9-riboside deri...

journal_title：Journal of medicinal chemistry

authors： Jacobson KA,Gao ZG,Tchilibon S,Duong HT,Joshi BV,Sonin D,Liang BT

更新日期：2005-12-29 00:00:00

abstract：:The S-adenosylmethionine (AdoMet) analogue S-(5'-deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cycl opentene (AdoMao) was synthesized in two of its four possible diastereomeric forms using a facile chemoenzymatic route. The trans-1R,4R- and trans-1S,4S-diastereomers of AdoMao, as well as the corresponding diastere...

journal_title：Journal of medicinal chemistry

authors： Guo J,Wu YQ,Rattendi D,Bacchi CJ,Woster PM

更新日期：1995-05-12 00:00:00

abstract：:There is currently no ideal radiotracer for imaging of protein synthesis rate (PSR) by positron emission tomography (PET). Existing fluorine-18-labeled amino acid-based radiotracers predominantly visualize amino acid transporter processes, and in many cases they are not incorporated into nascent proteins at all. Other...

journal_title：Journal of medicinal chemistry

authors： Betts HM,Milicevic Sephton S,Tong C,Awais RO,Hill PJ,Perkins AC,Aigbirhio FI

更新日期：2016-10-27 00:00:00

abstract：:Pleuromutilin is an antibiotic that binds to bacterial ribosomes and thereby inhibit protein synthesis. A new series of semisynthetic pleuromutilin derivatives were synthesized by a click chemistry strategy. Pleuromutilin was conjugated by different linkers to a nucleobase, nucleoside, or phenyl group, as a side-chain...

journal_title：Journal of medicinal chemistry

authors： Dreier I,Kumar S,Søndergaard H,Rasmussen ML,Hansen LH,List NH,Kongsted J,Vester B,Nielsen P

更新日期：2012-03-08 00:00:00

abstract：:Both HIV-EP1 (also called PRDII-BF1 or MBP-1), a zinc finger protein, and NF-kappa B, a Rel family protein, bind to kappa B site present in the enhancer of multiple cellular and viral genes involved in immune function and inflammatory response including HIV-1 LTR and human interferon beta gene. When cells are exposed ...

journal_title：Journal of medicinal chemistry

authors： Otsuka M,Fujita M,Aoki T,Ishii S,Sugiura Y,Yamamoto T,Inoue J

更新日期：1995-08-18 00:00:00

abstract：:3',4'-Dihydroxynomifensine, 8-amino-1,2,3,4-tetrahydro-4-(3,4-dihydroxyphenyl)-2-methylisoquinoli ne (1a), is an agonist of dopamine receptors in central and peripheral systems. Since this dopamine receptor agonist bears an asymmetric center at position 4, its synthesis and resolution were undertaken as part of a stud...

journal_title：Journal of medicinal chemistry

authors： Dandridge PA,Kaiser C,Brenner M,Gaitanopoulos D,Davis LD,Webb RL,Foley JJ,Sarau HM

更新日期：1984-01-01 00:00:00

abstract：:4-(Phenylamino)-5-phenyl-7-(5-deoxy-beta-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidine 1 and related compounds known as "diaryltubercidin" analogues are potent inhibitors of adenosine kinase (AK) and are orally active in animal models of pain such as the rat formalin paw model (GP3269 ED50= 6.4 mg/kg). However, the utility...

journal_title：Journal of medicinal chemistry

authors： Bookser BC,Ugarkar BG,Matelich MC,Lemus RH,Allan M,Tsuchiya M,Nakane M,Nagahisa A,Wiesner JB,Erion MD

更新日期：2005-12-01 00:00:00

abstract：:We synthesized 5-substituted pyrrolo[2,3-d]pyrimidine antifolates (compounds 5-10) with one-to-six bridge carbons and a benozyl ring in the side chain as antitumor agents. Compound 8 with a 4-carbon bridge was the most active analogue and potently inhibited proliferation of folate receptor (FR) α-expressing Chinese ha...

journal_title：Journal of medicinal chemistry

authors： Mitchell-Ryan S,Wang Y,Raghavan S,Ravindra MP,Hales E,Orr S,Cherian C,Hou Z,Matherly LH,Gangjee A

更新日期：2013-12-27 00:00:00

abstract：:5-Aroyl-6-substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carbo xylic acids were synthesized and assayed for analgesic and antiinflammatory activity. Several of these compounds, notably the 5-(4-fluoro- and 4-chlorobenzoyl)-6-methyl derivatives 25 and 26 and the 5-(4-methyl-, 4-fluoro-, 4-chloro-, and 4-methoxybenz...

journal_title：Journal of medicinal chemistry

authors： Muchowski JM,Cooper GF,Halpern O,Koehler R,Kluge AF,Simon RL,Unger SH,Van Horn AR,Wren DL,Ackrell J

更新日期：1987-05-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA) is an excellent biomarker for the early diagnosis of prostate cancer progression and metastasis. The most promising PSMA-targeted agents in the clinical phase are based on the Lys-urea-Glu motif, in which Lys and Glu are α-(l)-amino acids. In this study, we aimed to determine ...

journal_title：Journal of medicinal chemistry

authors： Kim K,Kwon H,Barinka C,Motlova L,Nam S,Choi D,Ha H,Nam H,Son SH,Minn I,Pomper MG,Yang X,Kutil Z,Byun Y

更新日期：2020-03-26 00:00:00

abstract：:The accessible surface, described by Lee and Richards (the L&R surface: J. Mol. Biol. 1971, 55, 379), has remarkably useful properties for displaying ligand-protein interactions. The surface is placed one van der Waals radius plus one probe radius away from the protein atoms. The ligands are displayed in skeletal form...

journal_title：Journal of medicinal chemistry

authors： Bohacek RS,McMartin C

更新日期：1992-05-15 00:00:00

abstract：:Di-tert-butyl (E)-4,4'-stilbenedicarboxylate and tert-butyl 4-vinylbenzoate were copolymerized with maleic anhydride and tert-butyl 4-maleimidobenzoate, individually and respectively. After conversion into polyanions, these four copolymers exhibited activity against four HIV-1 strains: IIIb, BaL, JR-CSF, and 92UG037. ...

journal_title：Journal of medicinal chemistry

authors： Savage AM,Li Y,Matolyak LE,Doncel GF,Turner SR,Gandour RD

更新日期：2014-08-14 00:00:00

abstract：:Doxazosin analogues 1-3 and 1a were synthesized and investigated at alpha1-adrenoceptors and PC-3, DU-145, and LNCaP human prostate cancer cells. Compound 1 (cyclodoxazosin) was a potent alpha(1B)-adrenoceptor antagonist displaying antiproliferative activity higher than that of doxazosin in cancer cells in vitro and i...

journal_title：Journal of medicinal chemistry

authors： Giardinà D,Martarelli D,Sagratini G,Angeli P,Ballinari D,Gulini U,Melchiorre C,Poggesi E,Pompei P

更新日期：2009-08-13 00:00:00