Structural requirement(s) of N-phenylthioureas and benzaldehyde thiosemicarbazones as inhibitors of melanogenesis in melanoma B 16 cells.

abstract：:We report the discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by using a structure-based drug design (SBDD) based on a docking model. The work leads to the representative compound 4a with high CSF-1R inhibitory activity (IC50 = 9.1 nM). The obtained crystal ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ikegashira K,Ikenogami T,Yamasaki T,Hase Y,Yamaguchi T,Inagaki K,Doi S,Adachi T,Koga Y,Hashimoto H

更新日期：2019-01-01 00:00:00

abstract：:The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacteriumtuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug cand...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alegaon SG,Alagawadi KR,Sonkusare PV,Chaudhary SM,Dadwe DH,Shah AS

更新日期：2012-03-01 00:00:00

abstract：:An α-carbonic anhydrase (CA, EC 4.2.1.1) isolated from the living fossil sponge Astrosclera willeyana, Astrosclerin, was investigated for its inhibition profile with simple inorganic anions, complex anions and other small molecules known to interact with these zinc enzymes. Astrosclerin is a catalytically highly effic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohradanova A,Vullo D,Pastorekova S,Pastorek J,Jackson DJ,Wörheide G,Supuran CT

更新日期：2012-02-01 00:00:00

abstract：:A 2-pyrrolidinone ring containing a single hydroxymethyl side chain effectively replaces the N-acetylamino group of 4-(N-acetylamino)-3-guanidinobenzoic acid, a low micromolar inhibitor of influenza neuraminidase. This novel structural template affords new opportunities to evolve more potent benzoic acid inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brouillette WJ,Atigadda VR,Luo M,Air GM,Babu YS,Bantia S

更新日期：1999-07-19 00:00:00

abstract：:The design and synthesis of new 1alpha,25-dihydroxy-19-norvitamin D(3) analogues 3a-c, which have an amide bond in the molecule instead of the diene, are described. The A-ring moiety was constructed by a (3S,5S)-3,5-dihydroxypiperidine derivative (9, 11, or 13) prepared from D-mannose, and a CD-ring carboxylic acid 16...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suhara Y,Kittaka A,Ono K,Kurihara M,Fujishima T,Yoshida A,Takayama H

更新日期：2002-12-16 00:00:00

abstract：:Two series of novel tricyclic oxazine and oxazepine fused quinazolines have been designed and synthesized. The in vitro antitumor effect of the title compounds was screened on N87, A431, H1975, BT474 and Calu-3 cell lines. Compared to gefitinib and erlotinib, compounds 1a-1h were found to demonstrate more potent antit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun M,Zhao J,Chen X,Zong Z,Han J,Du Y,Sun H,Wang F

更新日期：2016-10-01 00:00:00

abstract：:Analogues of the benzazepine dopamine D1 receptor antagonist SCH-23390 incorporating the cyclo-pentadienyltricarbonyl-rhenium (CPTR) moiety were synthesized and evaluated pharmacologically. The CPTR derivatives retained affinity (0.3-2.9 nM) and D1 selectivity of the parent compound, supporting their use as neuropharm...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamagnan G,Baldwin RM,Kula NS,Baldessarini RJ,Innis RB

更新日期：2000-05-15 00:00:00

abstract：:Vancomycin resistance is currently a major healthcare problem. The development of a catalytic monoclonal antibody (mAb) that hydrolyzes the D-Ala-D-Lac depsipeptide provides a potentially novel antibiotic strategy. A phosphonate hapten design was used to program antibody catalysis. The characteristics of the hapten we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Isomura S,Ashley JA,Wirsching P,Janda KD

更新日期：2002-03-25 00:00:00

abstract：:The mechanism of edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one) to scavenge DPPH radical is clarified by density functional theory (DFT) calculations. It is revealed that H-atom-abstraction rather than electron-transfer reaction is involved in the radical-scavenging process of edaravone, and H-atom at position 4 is r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang LF,Zhang HY

更新日期：2003-11-03 00:00:00

abstract：:New cis-fused tetrahydrochromeno[4,3-b]quinolines have been synthesized by intramolecular [4+2] imino-Diels-Alder reactions of 2-azadienes derived in situ from aromatic amines and 7-O-prenyl derivatives of 8-formyl-2,3-disubstituted chromenones in the presence of 20mol% Yb(OTf)(3) in acetonitrile under reflux conditio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nagaiah K,Venkatesham A,Srinivasa Rao R,Saddanapu V,Yadav JS,Basha SJ,Sarma AV,Sridhar B,Addlagatta A

更新日期：2010-06-01 00:00:00

abstract：:Attachment of DOTA to a novel monofluoro-cyclooctyne facilitates bioconjugation to an azide-modified peptide via Cu-free click chemistry. The resulting conjugate was radiolabeled with (111)In to afford a potential targeted molecular imaging agent with high specific activity and an excellent radiochemical purity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Martin ME,Parameswarappa SG,O'Dorisio MS,Pigge FC,Schultz MK

更新日期：2010-08-15 00:00:00

abstract：:1,2,4-Oxadiazoles have been prepared in parallel using 1,1'-carbonyldiimidazole (CDI) as a reagent for both formation and cyclodehydration of O-acyl benzamidoximes. The use of CDI facilitates parallel purification of the oxadiazole products by simple liquid-liquid extraction and filtration. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deegan TL,Nitz TJ,Cebzanov D,Pufko DE,Porco JA Jr

更新日期：1999-01-18 00:00:00

abstract：:A novel series of acylated omega-aminoalkyl 2-amino-2-deoxy-4-phosphono-beta-D-glucopyranosides (aminoalkyl glucosaminide 4-phosphates) was synthesized and screened for immunostimulant activity. Several of these compounds enhance the production of tetanus toxoid-specific antibodies in mice and augment vaccine-induced ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Johnson DA,Sowell CG,Johnson CL,Livesay MT,Keegan DS,Rhodes MJ,Ulrich JT,Ward JR,Cantrell JL,Brookshire VG

更新日期：1999-08-02 00:00:00

abstract：:Urea-based inhibitors of human glutamate carboxypeptidase II (GCPII) have advanced into clinical trials for imaging metastatic prostate cancer. In parallel efforts, agents with increased lipophilicity have been designed and evaluated for targeting GCPII residing within the neuraxis. Here we report the structural and c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pavlicek J,Ptacek J,Cerny J,Byun Y,Skultetyova L,Pomper MG,Lubkowski J,Barinka C

更新日期：2014-05-15 00:00:00

abstract：:6-(4H-Selenolo[3,2-b]pyrrolyl)-L-alanine 1, 4-(6H-selenolo[2,3-b]pyrrolyl)-L-alanine 2, and 6-(4H-furo[3,2-b]pyrrolyl)-L-alanine 3 have been synthesized via reactions of selenolo[3,2-b]pyrrole, selenolo[2,3-b]pyrrole, and furo[3,2-b]pyrrole, respectively, with L-serine. The reactions are catalyzed by Salmonella typhim...

journal_title：Bioorganic & medicinal chemistry letters

authors： Welch M,Phillips RS

更新日期：1999-03-08 00:00:00

abstract：:Pulvinone and several 3-fluoro-4-morpholino substituted pulvinone derivatives were synthesized in five steps from a common precursor, phenyl acetic acid. Most of synthetic morpholine substituted pulvinones showed inhibitory activity against Esherichia coli. For the first time, the inhibition of pulvinone and its deriv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu HW,Xu C,Fan ZQ,Zhao LJ,Liu HM

更新日期：2013-02-01 00:00:00

abstract：:We synthesized novel vitamin K derivatives by converting the naphthoquinone group to benzene derivatives and benzoquinone. We evaluated their neuronal differentiation activities to investigate the effect of the quinone moiety on this process. We observed that the 1,4-quinone as well as the side chain part play importa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yoshimura H,Hirota Y,Soda S,Okazeri M,Takagi Y,Takeuchi A,Tode C,Kamao M,Osakabe N,Suhara Y

更新日期：2020-04-15 00:00:00

abstract：:Several efficient synthetic routes for 2-, 4-, and 6-aryl-1,2,4-triazine-3,5-diones were developed. Derivatives were synthesized and studied as gonadotropin-releasing hormone antagonists in an effort to understand structure-activity relationships of the monocyclic compounds. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pontillo J,Guo Z,Wu D,Struthers RS,Chen C

更新日期：2005-10-01 00:00:00

abstract：:A series of 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues were synthesized and evaluated for cytotoxic activity against eight human cancer cell lines. Compounds 18, 21, 28, 29, 30 and 31 showed cytotoxic activity with GI(50) values in the range of 2.1-8.1 microM concentration. Among these, compounds 21...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma VM,Adi Seshu KV,Vamsee Krishna C,Prasanna P,Chandra Sekhar V,Venkateswarlu A,Rajagopal S,Ajaykumar R,Deevi DS,Rao Mamidi NV,Rajagopalan R

更新日期：2003-05-19 00:00:00

abstract：:5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure-activity relationships led to the discovery of a potent antago...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ladouceur GH,Cook JH,Doherty EM,Schoen WR,MacDougall ML,Livingston JN

更新日期：2002-02-11 00:00:00

abstract：:We report structure-guided modifications of the benzyloxy substituent of the Insulin-like Growth Factor-1 Receptor (IGF-1R) inhibitor NVP-AEW541. This chemical group has been shown to confer selectivity against other protein kinases but at the expense of a metabolism liability. X-ray crystallography has revealed that ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Stauffer F,Cowan-Jacob SW,Scheufler C,Furet P

更新日期：2016-04-15 00:00:00

abstract：:A series of new triazole fused imidazo[2,1-b]thiazole hybrids (9a-u) were designed, synthesized and evaluated as antimicrobial agents. Compounds 9c, 9d, 9e, 9j and 9l showed promising broad spectrum antimicrobial activity. Further, compound 9c exhibited significant anti-biofilm activity with single and mixed biofilm d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shareef MA,Sirisha K,Sayeed IB,Khan I,Ganapathi T,Akbar S,Ganesh Kumar C,Kamal A,Nagendra Babu B

更新日期：2019-10-01 00:00:00

abstract：:We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazine series inhibitors such as 5b demonstrated acceptable metabolic stab...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu S,Liu Y,Wang H,Ding Y,Wu H,Dong J,Wong A,Chen SH,Li G,Chan M,Sawyer N,Gervais FG,Henault M,Kargman S,Bedard LL,Han Y,Friesen R,Lobell RB,Stout DM

更新日期：2009-10-01 00:00:00

abstract：:A series of novel 4-substituted benzoxazolone derivatives was synthesized, characterized and evaluated as human soluble epoxide hydrolase (sEH) inhibitors and anti-inflammatory agents. Some compounds showed moderate sEH inhibitory activities in vitro, and two novel compounds, 3g and 4j, exhibited the highest activitie...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tang L,Ma WH,Ma YL,Ban SR,Feng XE,Li QS

更新日期：2013-04-15 00:00:00

abstract：:Selective σ2 ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to determine the optimal substituents in the σ2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorop...

journal_title：Bioorganic & medicinal chemistry letters

authors： Motel WC,Healy JR,Viard E,Pouw B,Martin K,Matsumoto RR,Coop A

更新日期：2013-12-15 00:00:00

abstract：:Series of short amino terminal modified cationic peptides were designed and synthesized. All of the synthesized compounds were tested against gram-positive as well as gram-negative bacterial strain. Some of the compounds exhibit potent antibacterial activity and no hemolytic activity even at high dose level (1000 micr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bisht GS,Rawat DS,Kumar A,Kumar R,Pasha S

更新日期：2007-08-01 00:00:00

abstract：:Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic beta-secretase inhibitors incorporating hydroxyethylamine isosteres are described. We have identified inhibitor 24 which has shown exceedingly potent activity in memapsin 2 enzyme inhibitory (K(i) 1.8 nM) and cellular (IC(50)=1 ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ghosh AK,Kumaragurubaran N,Hong L,Kulkarni S,Xu X,Miller HB,Reddy DS,Weerasena V,Turner R,Chang W,Koelsch G,Tang J

更新日期：2008-02-01 00:00:00

abstract：:A new class of non-ionic amphiphilic molecules suitable for biological purposes, especially extraction of membrane proteins, is reported. Such surfactants were prepared in two steps: addition of alkyl or fluoroalkyl mercaptan on Tris(hydroxymethyl)acrylamidomethane (THAM) derivatives, followed by the oxydation of sulf...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barthélémy P,Maurizis JC,Lacombe JM,Pucci B

更新日期：1998-06-16 00:00:00

abstract：:A series of 2-phenylpyrimidine coumarin derivatives with potential telomerase-inhibiting activity was designed and synthesized. All of the compounds were screened for antiproliferative activity against CNE2, KB, and Cal27 cell lines in vitro. The results showed that most of the derivatives had a favorable effect on re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lv N,Sun M,Liu C,Li J

更新日期：2017-10-01 00:00:00

abstract：:Novel bendazac analogues and their salts have been designed and prepared. The resulting compounds (13c-d, 15c, 17c) showed very good aqueous solubility (>100 mg/mL). An in vitro assay showed that most of the resulting compounds had potent protective activity against the oxidative damage. Particularly, compound 13d was...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shen H,Gou S,Shen J,Zhu Y,Zhang Y,Chen X

更新日期：2010-04-01 00:00:00