Intramolecular aldol cyclization of L-lyxo-hexos-5-ulose derivatives: a new diastereoselective synthesis of D-chiro-inositol.

abstract：:Methyl bacteriopheophorbide-f was prepared from methyl bacteriopheophorbide-d with retention of the 3(1)-chirality. The transformation of the methyl to the formyl group at the 7-position of the chlorin moiety will provide an alternative route for the synthesis of bacteriochlorophylls-e and f. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamiaki H,Omoda M,Kubo M

更新日期：1999-06-21 00:00:00

abstract：:Esculentoside A (EsA) has been reported to possess anti-inflammatory activity and selective inhibitory activity towards cyclooxygenase-2. A series of derivatives of EsA were synthesized by converting the C-28 carboxylic acid group into amides. The haemolytic activity and inhibitory activity towards cyclooxygenase-2 we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wu F,Yi Y,Sun P,Zhang D

更新日期：2007-12-01 00:00:00

abstract：:The P13K/Akt pathway is a growth-regulating cellular signaling pathway that is over-activated in numerous human cancers. A novel series of Akt pathway inhibitors were identified using iterative pharmacophore modeling, energy-based calculations, and property predictions of known Akt inhibitors. Inhibitory effects on ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Uko NE,Güner OF,Barnett LMA,Matesic DF,Bowen JP

更新日期：2018-10-15 00:00:00

abstract：:From an easily available partially protected formal derivative of 1-deoxymannojirimycin, by hydroxymethyl chain-branching and further elaboration, lipophilic analogs of the powerful β-d-galactosidase inhibitor 4-epi-isofagomine have become available. New compounds exhibit improved inhibitory activities comparable to b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thonhofer M,Weber P,Santana AG,Fischer R,Pabst BM,Paschke E,Schalli M,Stütz AE,Tschernutter M,Windischhofer W,Withers SG

更新日期：2016-03-01 00:00:00

abstract：:Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2' p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cumming JN,Le TX,Babu S,Carroll C,Chen X,Favreau L,Gaspari P,Guo T,Hobbs DW,Huang Y,Iserloh U,Kennedy ME,Kuvelkar R,Li G,Lowrie J,McHugh NA,Ozgur L,Pan J,Parker EM,Saionz K,Stamford AW,Strickland C,Tadesse D,

更新日期：2008-06-01 00:00:00

abstract：:The synthesis, anti-Pneumocystis carinii activity and DNA binding properties of eight new N,N'-bis[4-(N-alkylamidino)phenyl]homopiperazines are reported. Compounds 2 and 8 were the most potent and caused about 70% inhibition of Pneumocystis carinii growth in a cell culture model at 1 microM concentrations. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang TL,Tao B,Quarshie Y,Queener SF,Donkor IO

更新日期：2001-10-22 00:00:00

abstract：:We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR) up to 10 microM concentration. Recent studies have indicated that agonizing this receptor may promote resolution of in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bürli RW,Xu H,Zou X,Muller K,Golden J,Frohn M,Adlam M,Plant MH,Wong M,McElvain M,Regal K,Viswanadhan VN,Tagari P,Hungate R

更新日期：2006-07-15 00:00:00

abstract：:Structure-activity studies on benzamide 1 obtained from library screening led to the discovery of a novel series of potent and selective glycine transporter type-2 inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ho KK,Appell KC,Baldwin JJ,Bohnstedt AC,Dong G,Guo T,Horlick R,Islam KR,Kultgen SG,Masterson CM,McDonald E,McMillan K,Morphy JR,Rankovic Z,Sundaram H,Webb M

更新日期：2004-01-19 00:00:00

abstract：:The synthesis and inhibitory activities of 10 potential inhibitors of Pfmrk, a Plasmodium falciparum cyclin-dependent protein kinase, are described. The most potent inhibitor is a 3-phenyl-quinolinone compound with an IC(50) value of 18 microM. It is the first compound reported to inhibit Pfmrk at the micro molar rang...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao Z,Waters NC,Woodard CL,Li Z,Li PK

更新日期：2001-11-05 00:00:00

abstract：:A series of new imines and amines have been synthesized by condensation of 1H-3-ferrocenyl-1-phenylpyrazole-4-carboxaldehyde with the corresponding amines, followed by reduction with sodium borohydride. The synthesized compounds have been screened for their in vitro antimicrobial activity against 11 bacteria and three...

journal_title：Bioorganic & medicinal chemistry letters

authors： Damljanović I,Vukićević M,Radulović N,Palić R,Ellmerer E,Ratković Z,Joksović MD,Vukićević RD

更新日期：2009-02-15 00:00:00

abstract：:In the search for new antibacterial agents, the enzyme FabI has been identified as an attractive target. Employing a structure guided approach, the previously reported ene-amide series of FabI inhibitors were expanded to include 2,3,4,5-tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines. These novel series incorporate a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramnauth J,Surman MD,Sampson PB,Forrest B,Wilson J,Freeman E,Manning DD,Martin F,Toro A,Domagala M,Awrey DE,Bardouniotis E,Kaplan N,Berman J,Pauls HW

更新日期：2009-09-15 00:00:00

abstract：:A series of substituted indoles were examined as selective inhibitors of tropomyosin-related kinase receptor A (TrkA), a therapeutic target for the treatment of pain. An SAR optimization campaign based on ALIS screening lead compound 1 is reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hurzy DM,Henze DA,Cabalu TD,Narayan K,Heller A,Cooke AJ

更新日期：2017-06-15 00:00:00

abstract：:An efficient synthesis of [D-lysine](8)cyclosporin A has been developed. Several analogs of [D-lysine](8)cyclosporin A have been synthesized and show promising anti-HCV activity, particularly compounds 39 and 43, which each exhibit an anti-HCV EC(50)<200 nM, and are each ≥50-fold less immunosuppressive than cyclospori...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scribner A,Houck D,Huang Z,Mosier S,Peel M,Scorneaux B

更新日期：2010-11-15 00:00:00

abstract：:Bromodomains (BRDs) recognize acetyl-lysine modified histone tails mediating epigenetic processes. BRD4, a protein containing two bromodomains, has emerged as an attractive therapeutic target for several types of cancer as well as inflammatory diseases. Using a fragment-based in silico screening approach, we identifie...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao H,Gartenmann L,Dong J,Spiliotopoulos D,Caflisch A

更新日期：2014-06-01 00:00:00

abstract：:In the course of our research aimed at the discovery of metabolic stable pleuromutilin derivatives with more potent antibacterial activity against Gram-positive pathogens than previous analogues, a series of compounds bearing a purine ring were prepared and evaluated. From SAR studies, we identified two promising comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hirokawa Y,Kinoshita H,Tanaka T,Nakamura T,Fujimoto K,Kashimoto S,Kojima T,Kato S

更新日期：2008-06-15 00:00:00

abstract：:Neutral fluorescent active di-pyrene modified gamma-cyclodextrin (1) was synthesized in order to discriminate with single and double strand DNA (ssDNA and dsDNA, respectively) with high selectivity. The binding and selectivity of 1 for dsDNA was indicated by increase of the fluorescent intensity in an addition of dsDN...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takeda A,Akimoto K,Kondo Y,Hamada F

更新日期：2010-06-01 00:00:00

abstract：:Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists. Benzimidazole and indazolone derivatives prepared retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fletcher SR,McIver E,Lewis S,Burkamp F,Leech C,Mason G,Boyce S,Morrison D,Richards G,Sutton K,Jones AB

更新日期：2006-06-01 00:00:00

abstract：:Novel 3-[4-(dimethylamino)phenyl]alkyl-2-oxindole analogs were synthesized by either of the following two pathways: (1) a sequence of Knoevenagel condensation of oxindole with (4-dimethylamino)cinnamaldehyde-hydrogenation, or (2) alkylation of oxindole dianion with [(4-dimethylamino)phenyl]alkyl halides. Subsequent al...

journal_title：Bioorganic & medicinal chemistry letters

authors： Furuta K,Kawai Y,Mizuno Y,Hattori Y,Koyama H,Hirata Y

更新日期：2017-09-15 00:00:00

abstract：:There is tremendous interest in developing activator artificial transcription factors that functionally mimic endogenous transcriptional activators for use as mechanistic probes, as components of synthetic cell circuitry, and in transcription-targeted therapies. Here, we demonstrate that a phage display selection agai...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majmudar CY,Labut AE,Mapp AK

更新日期：2009-07-15 00:00:00

abstract：:Two regioisomeric isoxazoline monoacetates 1 and 2 were synthesized from the corresponding diacetate 3 via PPL or PLE catalyzed hydrolysis. With both the enzymes, the initial regioselectivity (approximately 3-4:1) was offset by an intramolecular acyl transfer. In addition to a non-enzymatic catalysis for the acyl tran...

journal_title：Bioorganic & medicinal chemistry letters

authors： Basak A,Bisai S

更新日期：2005-05-16 00:00:00

abstract：:A series of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides were identified as small molecule PCSK9 mRNA translation inhibitors. Analogues from this new chemical series, such as 4d and 4g, exhibited improved PCSK9 potency, ADME properties, and in vitro safety profiles when compared to earlier l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Londregan AT,Aspnes G,Limberakis C,Loria PM,McClure KF,Petersen DN,Raymer B,Ruggeri RB,Wei L,Xiao J,Piotrowski DW

更新日期：2018-12-15 00:00:00

abstract：:Inhibition of 11beta-HSD1 has demonstrated potential in the treatment of various components of metabolic syndrome. We wish to report herein the discovery of novel azabicyclic sulfonamide based 11beta-HSD1 inhibitors. Highly potent compounds exhibiting inhibitory activities at both human and mouse 11beta-HSD1 were iden...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shah U,Boyle CD,Chackalamannil S,Baker H,Kowalski T,Lee J,Terracina G,Zhang L

更新日期：2010-03-01 00:00:00

abstract：:Glycogen synthase kinase-3 beta (GSK3β) kinase serves as a promising therapeutic target for the treatment of various human diseases, such as diabetes, obesity, and Alzheimer's disease. In this study, we report lead GSK3β inhibitors identified using a fragment-linking strategy. Through the systematic exploration, a six...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim J,Moon Y,Hong S

更新日期：2016-12-01 00:00:00

abstract：:High throughput cell-based screening led to the identification of 3-aryloxy lactams as potent androgen receptor (AR) antagonists. Refinement of these leads to improve the ADME profile and remove residual agonism led to the discovery of 12, a potent full antagonist with greater oral bioavailability. Improvements in the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guo C,Kephart S,Ornelas M,Gonzalez J,Linton A,Pairish M,Nagata A,Greasley S,Elleraas J,Hosea N,Engebretsen J,Fanjul AN

更新日期：2012-01-15 00:00:00

abstract：:The synthesis of a series of novel 1-[(benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles is described. The compounds were tested for human placental aromatase inhibition in vitro, using [1beta-3H]-androstenedione as the substrate for the aromatase enzyme, the percentage inhibition and IC50 data is included. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vinh TK,Ahmadi M,Delgado PO,Perez SF,Walters HM,Smith HJ,Nicholls PJ,Simons C

更新日期：1999-07-19 00:00:00

abstract：:Novel C-seco-taxoids were synthesized from 10-deacetylbaccatin III and their potencies evaluated against drug-sensitive and drug-resistant cancer cell lines. The drug-resistant cell lines include ovarian cancer cell lines resistant to cisplatin, topotecan, adriamycin and paclitaxel overexpressing class III beta-tubuli...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pepe A,Sun L,Zanardi I,Wu X,Ferlini C,Fontana G,Bombardelli E,Ojima I

更新日期：2009-06-15 00:00:00

abstract：:Distamycin and nitrogen mustard conjugates, in which the nitrogen mustard unit was coupled to the C-terminus of the pyrrole, were synthesized. The switching of the nitrogen mustard unit from the N-terminus to the C-terminus did not compromise the compound's cytotoxicity. Compound 3, bearing three pyrrole units, was hi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Y,Wright SC,Larrick JW

更新日期：2003-02-10 00:00:00

abstract：:To discover new natural-product-based insecticidal agents, a series of novel oxime derivatives of podophyllotoxin-based phenazines modified in the C, D and E rings of podophyllotoxin were prepared and tested as insecticidal agents against the pre-third-instar larvae of oriental armyworm, Mythimna separata (Walker) in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhi X,Yang C,Yu X,Xu H

更新日期：2014-12-15 00:00:00

abstract：:Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight (M(W): 335-391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ries UJ,Priepke HW,Hauel NH,Haaksma EE,Stassen JM,Wienen W,Nar H

更新日期：2003-07-21 00:00:00

abstract：:In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G. J. Med. Chem.2005, 48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by com...

journal_title：Bioorganic & medicinal chemistry letters

authors： McClure KJ,Huang L,Arienti KL,Axe FU,Brunmark A,Blevitt J,Breitenbucher JG

更新日期：2006-04-01 00:00:00