Facile radiosynthesis of fluorine-18 labeled beta-blockers. Synthesis, radiolabeling, and ex vivo biodistribution of [18F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol.

abstract：:Using reported glutathione S-transferase omega 1 (GSTO1-1) cocrystal structures, we designed and synthesized acrylamide-containing compounds that covalently bind to Cys32 on the catalytic site. Starting from a thiazole derivative 10 (GSTO1-1 IC50 = 0.6 μM), compound 18 was synthesized and cocrystallized with GSTO1. Mo...

journal_title：Journal of medicinal chemistry

authors： Dai W,Samanta S,Xue D,Petrunak EM,Stuckey JA,Han Y,Sun D,Wu Y,Neamati N

更新日期：2019-03-28 00:00:00

abstract：:We report the synthesis and antiviral activity of a new family of non-nucleoside antivirals, derived from the 4-keto-1,2-oxathiole-2,2-dioxide (beta-keto-gamma-sultone) heterocyclic system. Several 4- and 5-substituted-5H-1,2-oxathiole-2,2-dioxide derivatives were found to have a selective inhibitory activity against ...

journal_title：Journal of medicinal chemistry

authors： De Castro S,García-Aparicio C,Andrei G,Snoeck R,Balzarini J,Camarasa MJ,Velázquez S

更新日期：2009-03-26 00:00:00

abstract：:The N- and C-terminal domains of human somatic angiotensin I converting enzyme (sACE-1) demonstrate distinct physiological functions, with resulting interest in the development of domain-selective inhibitors for specific therapeutic applications. Herein, the activity of lisinopril-coupled transition metal chelates was...

journal_title：Journal of medicinal chemistry

authors： Hocharoen L,Joyner JC,Cowan JA

更新日期：2013-12-27 00:00:00

abstract：:The interaction between β-catenin and B-cell CLL/lymphoma 9 (BCL9), critical for the transcriptional activity of β-catenin, is mediated by a helical segment from BCL9 and a large binding groove in β-catenin. Design of potent, metabolically stable BCL9 peptides represents an attractive approach to inhibit the activity ...

journal_title：Journal of medicinal chemistry

authors： Kawamoto SA,Coleska A,Ran X,Yi H,Yang CY,Wang S

更新日期：2012-02-09 00:00:00

abstract：:The natural abundance 13C magnetic resonance spectra of a series of sulfonamide drugs(sulfanilamide, sulfaguanidine,sulfathiazole, sulfasuxidine, sulfadiazine, sulfamerazine, sulfamethiazine, and sulfapyridine) have been determined at 25.15 MHz employing the pulse Fourier transform technique. The chemical shefts have ...

journal_title：Journal of medicinal chemistry

authors： Chang C,Floss HG,Peck GE

更新日期：1975-05-01 00:00:00

abstract：:Antivirulence strategies are now attracting interest for the inherent mechanism of action advantages. In our previous work, diapophytoene desaturase (CrtN) was identified to be an attractive and drugable target for fighting pigmented S. aureus infections. In this research, we developed a series of effective benzocyclo...

journal_title：Journal of medicinal chemistry

authors： Wang Y,Di H,Chen F,Xu Y,Xiao Q,Wang X,Wei H,Lu Y,Zhang L,Zhu J,Lan L,Li J

更新日期：2016-05-26 00:00:00

abstract：:The understanding of the physiological role of the G-protein coupled serotonin 5-HT(7) receptor is largely rudimentary. Therefore, selective and potent pharmacological tools will add to the understanding of serotonergic effects mediated through this receptor. In this report, we describe two compound classes, chromans ...

journal_title：Journal of medicinal chemistry

authors： Holmberg P,Sohn D,Leideborg R,Caldirola P,Zlatoidsky P,Hanson S,Mohell N,Rosqvist S,Nordvall G,Johansson AM,Johansson R

更新日期：2004-07-29 00:00:00

abstract：:Interaction of 2-iodoaniline or 5-fluoro-2-iodoaniline with a range of arylsulfonyl chlorides affords sulfonamides that undergo Sonogashira couplings under thermal or microwave conditions with the alkyne 4-ethynyl-4-hydroxycyclohexa-2,5-dien-1-one followed by cyclization to 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxy...

journal_title：Journal of medicinal chemistry

authors： McCarroll AJ,Bradshaw TD,Westwell AD,Matthews CS,Stevens MF

更新日期：2007-04-05 00:00:00

abstract：:Z-D-Phe-Pro-boroMpg-OPin (9a)1,2 has been shown previously to be a highly specific inhibitor of thrombin in spite of lacking an arginine-like guanidino group at the P1 site. A range of compounds have been synthesized based upon this lead compound, varying the neutral side chain at the P1 site. Of the 20 examples based...

journal_title：Journal of medicinal chemistry

authors： Deadman JJ,Elgendy S,Goodwin CA,Green D,Baban JA,Patel G,Skordalakes E,Chino N,Claeson G,Kakkar VV

更新日期：1995-04-28 00:00:00

abstract：:Four subtypes of adenosine receptors are currently known, that is, A(1), A(2A), A(2B), and A(3) receptors. Interestingly, quite substantial species differences exist especially between human and rat A(3) receptors. As a result, ligands such as CCPA, which are very selective for the rat A(1) receptor versus the human A...

journal_title：Journal of medicinal chemistry

authors： Beukers MW,Wanner MJ,Von Frijtag Drabbe Künzel JK,Klaasse EC,IJzerman AP,Koomen GJ

更新日期：2003-04-10 00:00:00

abstract：:The proto-oncogenes NTRK1/2/3 encode the tropomyosin receptor kinases TrkA/B/C which play pivotal roles in neurobiology and cancer. We describe herein the discovery of [11C]-(R)-3 ([11C]-(R)-IPMICF16), a first-in-class positron emission tomography (PET) TrkB/C-targeting radiolabeled kinase inhibitor lead. Relying on e...

journal_title：Journal of medicinal chemistry

authors： Bernard-Gauthier V,Bailey JJ,Mossine AV,Lindner S,Vomacka L,Aliaga A,Shao X,Quesada CA,Sherman P,Mahringer A,Kostikov A,Grand'Maison M,Rosa-Neto P,Soucy JP,Thiel A,Kaplan DR,Fricker G,Wängler B,Bartenstein P,Schirrm

更新日期：2017-08-24 00:00:00

abstract：:Carbonates containing an iodinated aromatic ring on one side of the carbonate linkage and an alkyl group on the other were prepared. The aromatic side consisted of p-iodophenyl, p-iodobenzyl, m-iodobenzyl, 3,5-diiodobenzyl, m-amino-2,4,6-triiodobenzyl, m-acetamido-2,4,6-triiodobenzyl, p-iodophenethyl, p-iodo-sec-phene...

journal_title：Journal of medicinal chemistry

authors： Newton BN

更新日期：1976-12-01 00:00:00

abstract：:The photolabile (diazomethyl)carbonyl function was introduced into the 8-position of 2-(N,N-di-n-propyl-amino)-1,2,3,4-tetrahydronaphthalene in three ways, resulting in the ether 8-[[(diazomethyl)carbonyl]methoxy]-2-(N,N-di-n-propylamino)-1,2,3,4- tetrahydronaphthalene (2), the ester 8-(diazoacetoxy)-2-(N,N-di-n-propy...

journal_title：Journal of medicinal chemistry

authors： Kline TB,Nelson DL,Namboodiri K

更新日期：1990-03-01 00:00:00

abstract：:A series of modifications of the CCK7 analogue (des-NH2)Tyr(SO3-)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 was prepared and tested for binding to guinea pig CCK-A and CCK-B receptors and in CCK-A-mediated functional assays. Selected analogues also were tested for appetite suppressant activity in rats. Several conformationally rest...

journal_title：Journal of medicinal chemistry

authors： Holladay MW,Bennett MJ,Tufano MD,Lin CW,Asin KE,Witte DG,Miller TR,Bianchi BR,Nikkel AL,Bednarz L

更新日期：1992-08-07 00:00:00

abstract：:Autophagy is a lysosome-dependent mechanism of intracellular degradation for maintaining cellular homeostasis. Dysregulation of autophagy has been verified to be closely linked to a number of human diseases. Consequently, targeting autophagy has been highlighted as a novel therapeutic strategy for clinical utility. Mo...

journal_title：Journal of medicinal chemistry

authors： He S,Li Q,Jiang X,Lu X,Feng F,Qu W,Chen Y,Sun H

更新日期：2018-06-14 00:00:00

abstract：:The synthesis of new meridianin derivatives is described. The indolic ring system was substituted at the C-4 to C-7 positions either by a bromine atom or by nitro or amino groups. Additionally, an iodine atom or various aryl groups were introduced at the C-5 position of the 2-aminopyrimidine ring. These compounds as w...

journal_title：Journal of medicinal chemistry

authors： Giraud F,Alves G,Debiton E,Nauton L,Théry V,Durieu E,Ferandin Y,Lozach O,Meijer L,Anizon F,Pereira E,Moreau P

更新日期：2011-07-14 00:00:00

abstract：:We have reported that [methyl- (11)C] (3 R,5 R)-5-(3-methoxyphenyl)-3-[(R)-1-phenylethylamino]-1-(4-trifluoromethylphenyl)pyrrolidin-2-one ([(11)C] 8, [(11)C]MePPEP) binds with high selectivity to cannabinoid type-1 (CB 1) receptors in monkey brain in vivo. We now describe the synthesis of 8 and four analogues, namely...

journal_title：Journal of medicinal chemistry

authors： Donohue SR,Krushinski JH,Pike VW,Chernet E,Phebus L,Chesterfield AK,Felder CC,Halldin C,Schaus JM

更新日期：2008-09-25 00:00:00

abstract：:The iodinated analogue of 1-[2-(4-aminophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperazine (PAPP), IPAPP (4), and the corresponding azido compound azido-IPAPP (5) were synthesized. The corresponding no-carrier-added 125I (T1/2 = 60 days, 35-60 keV) labeled compounds were also prepared. High specific binding was obse...

journal_title：Journal of medicinal chemistry

authors： Chumpradit S,Kung HF,Billings J,Guo YZ,Wu Y,Shih J

更新日期：1989-03-01 00:00:00

abstract：:The objective of this study is the measurement of the rates of hydrolysis of a series of chloroethyl sulfide derivatives, under stimulated physiological conditions. Interferences encountered with the conventional spectrophotometric method prompted the use of a rapid-response, chloride selective electrode. This probe w...

journal_title：Journal of medicinal chemistry

authors： Wright JE,Hayes MJ,Subramanyam V,Soloway AH

更新日期：1977-12-01 00:00:00

abstract：:A high-throughput, cell-based screen was used to identify chemotypes as inhibitors for human respiratory syncytial virus (hRSV). Optimization of a sulfonylpyrrolidine scaffold resulted in compound 5o that inhibited a virus-induced cytopathic effect in the entry stage of infection (EC₅₀ = 2.3 ± 0.8 μM) with marginal cy...

journal_title：Journal of medicinal chemistry

authors： Moore BP,Chung DH,Matharu DS,Golden JE,Maddox C,Rasmussen L,Noah JW,Sosa MI,Ananthan S,Tower NA,White EL,Jia F,Prisinzano TE,Aubé J,Jonsson CB,Severson WE

更新日期：2012-10-25 00:00:00

abstract：:G-Quadruplexes, noncanonical nucleic acid structures, act as silencers in the promoter regions of human genes; putative G-quadruplex forming sequences are also present in promoters of other mammals, yeasts, and prokaryotes. Here we show that also the HIV-1 LTR promoter exploits G-quadruplex-mediated transcriptional re...

journal_title：Journal of medicinal chemistry

authors： Perrone R,Nadai M,Frasson I,Poe JA,Butovskaya E,Smithgall TE,Palumbo M,Palù G,Richter SN

更新日期：2013-08-22 00:00:00

abstract：:This report describes the syntheses and structure-activity relationships of 8-(4-methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazine corticotropin releasing factor receptor-1 (CRF(1)) receptor antagonists. CRF(1) receptor antagonists may be potential anxiolytic or antidepressant drugs. This research culminated in the discove...

journal_title：Journal of medicinal chemistry

authors： Gilligan PJ,He L,Clarke T,Tivitmahaisoon P,Lelas S,Li YW,Heman K,Fitzgerald L,Miller K,Zhang G,Marshall A,Krause C,McElroy J,Ward K,Shen H,Wong H,Grossman S,Nemeth G,Zaczek R,Arneric SP,Hartig P,Robertson DW,T

更新日期：2009-05-14 00:00:00

abstract：:HIV-1 replication has been inhibited by using a compound able to target the human cellular cofactor DEAD-box ATPase DDX3, essential for HIV-1 RNA nuclear export. This compound, identified by means of a computational protocol based on pharmacophoric modeling and molecular docking calculations, represents the first smal...

journal_title：Journal of medicinal chemistry

authors： Maga G,Falchi F,Garbelli A,Belfiore A,Witvrouw M,Manetti F,Botta M

更新日期：2008-11-13 00:00:00

abstract：:Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme that is involved in the de novo synthesis of purine nucleotides. Novel 2-aminooxazoles were synthesized and tested for inhibition of IMPDH catalytic activity. Multiple analogues based on this chemotype were found to inhibit IMPDH with low nanomolar potency. O...

journal_title：Journal of medicinal chemistry

authors： Dhar TG,Shen Z,Guo J,Liu C,Watterson SH,Gu HH,Pitts WJ,Fleener CA,Rouleau KA,Sherbina NZ,McIntyre KW,Shuster DJ,Witmer MR,Tredup JA,Chen BC,Zhao R,Bednarz MS,Cheney DL,MacMaster JF,Miller LM,Berry KK,Harper TW,

更新日期：2002-05-23 00:00:00

abstract：:Success in discovering bioactive peptide mimetics is often limited by the difficulties in correctly transposing known binding elements of the active peptide onto a small and metabolically more stable scaffold while maintaining bioactivity. Here we describe a scanning approach using a library of pyranose-based peptidom...

journal_title：Journal of medicinal chemistry

authors： Abbenante G,Becker B,Blanc S,Clark C,Condie G,Fraser G,Grathwohl M,Halliday J,Henderson S,Lam A,Liu L,Mann M,Muldoon C,Pearson A,Premraj R,Ramsdale T,Rossetti T,Schafer K,Le Thanh G,Tometzki G,Vari F,Verquin G,

更新日期：2010-08-12 00:00:00

abstract：:The synthesis and structure-activity relationships of a new class of vinylcephalosporins substituted with a lactamyl residue are described. These compounds show excellent activity against enterococci and retain the broad spectrum activity of third-generation cephalosporins such as ceftriaxone. ...

journal_title：Journal of medicinal chemistry

authors： Heinze-Krauss I,Angehrn P,Guerry P,Hebeisen P,Hubschwerlen C,Kompis I,Page MG,Richter HG,Runtz V,Stalder H,Weiss U,Wei CC

更新日期：1996-04-26 00:00:00

abstract：:A series of [(3-aryl-1,2-benzisoxazol-6-yl)oxy]acetic acids was synthesized and tested for diuretic activity in saline-loaded mice and in conscious, water-loaded dogs. The structural requirements for good diuretic activity in both mice and dogs were found to be very specific. In summary, the compounds with the best di...

journal_title：Journal of medicinal chemistry

authors： Shutske GM,Setescak LL,Allen RC,Davis L,Effland RC,Ranbom K,Kitzen JM,Wilker JC,Novick WJ Jr

更新日期：1982-01-01 00:00:00

abstract：:Indolic N-benzylation of naltrindole reportedly extends the duration of delta-opioid receptor (DOR) antagonism. Similar modification of the kappa-opioid receptor (KOR) antagonist norBNI (1a) and its 17,17'-diNMe analogue (1d), a low potency mu-opioid receptor (MOR) partial agonist, was found to affect predominantly th...

journal_title：Journal of medicinal chemistry

authors： Chauvignac C,Miller CN,Srivastava SK,Lewis JW,Husbands SM,Traynor JR

更新日期：2005-03-10 00:00:00

abstract：:A three-dimensional structure of the complex of human renin and the scissile site P4 Pro to P1' Val of angiotensinogen was deduced in order to design potent human renin inhibitors rationally. On the basis of this structure, an orally potent human renin inhibitor (1a) was designed from the angiotensinogen transition st...

journal_title：Journal of medicinal chemistry

authors： Iizuka K,Kamijo T,Harada H,Akahane K,Kubota T,Umeyama H,Ishida T,Kiso Y

更新日期：1990-10-01 00:00:00

abstract：:The chemical structures of sweet compounds are very different, ranging from sugars to amino acids and peptides or other compounds such as saccharin. The biological mechanism underlying the generation of sweet taste is still unknown, although in the past few years much research has provided evidence for the existence o...

journal_title：Journal of medicinal chemistry

authors： Bassoli A,Drew MG,Merlini L,Morini G

更新日期：2002-09-26 00:00:00