Synthesis and antimycobacterial activity of 5-formylaminopyrimidines; analogs of antibacterial purines.

abstract：:A group of tri and tetrasubstituted urea derivatives have been found to be hH(3)-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lau JF,Jeppesen CB,Rimvall K,Hohlweg R

更新日期：2006-10-15 00:00:00

abstract：:A new series of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridine compounds have been discovered as potent anaplastic lymphoma kinase (ALK) inhibitors. The 4-hydroxyphenyl in the 6-position of 1H-pyrazolo[3,4-b]pyridine were crucial and a fluorine atom substitution could give promising inhibitory activity. The IC50 of compound 9v...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen C,Pan P,Deng Z,Wang D,Wu Q,Xu L,Hou T,Cui S

更新日期：2019-04-01 00:00:00

abstract：:Pinostrobin (5-hydroxy-7-methoxyflavanone) obtained in relatively large amounts from fingerroot (Boesenbergia pandurata) was converted to its C-6 and C-8 prenylated derivatives. The Mitsunobu reaction, europium(III)-catalyzed Claisen-Cope rearrangement, and Claisen reaction coupled with cross-metathesis were used as t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Poerwono H,Sasaki S,Hattori Y,Higashiyama K

更新日期：2010-04-01 00:00:00

abstract：:The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Compounds from this set had binding and functional activities at MC4R less than 30 nM. The most selective compound in this series was >25,000-fold more pote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fotsch C,Han N,Arasasingham P,Bo Y,Carmouche M,Chen N,Davis J,Goldberg MH,Hale C,Hsieh FY,Kelly MG,Liu Q,Norman MH,Smith DM,Stec M,Tamayo N,Xi N,Xu S,Bannon AW,Baumgartner JW

更新日期：2005-03-15 00:00:00

abstract：:A series of thiazolo[4,5-d]pyrimidine thiones and -ones was prepared and discovered to have good binding affinity to the CRH-R1 receptor, thus showing promise as a new class of potential anxiolytics and/or antidepressants. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beck JP,Curry MA,Chorvat RJ,Fitzgerald LW,Gilligan PJ,Zaczek R,Trainor GL

更新日期：1999-04-19 00:00:00

abstract：:A series of novel hybrid molecules 4a-y containing thiazole and benzotriazole templates were designed and synthesized. The structures of the synthesized compounds were elucidated by IR, (1)H NMR, (13)C NMR and mass spectral data. All the synthesized compounds were tested for their antimicrobial activity (zone of inhib...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gaikwad ND,Patil SV,Bobade VD

更新日期：2012-05-15 00:00:00

abstract：:2'-O-[N-(4-Aminobutylcarbamoyl)]uridine (U(abcm)) was synthesized and incorporated into oligonucleotides. The oligonucleotides incorporating U(abcm) formed more stable duplexes with their complementary and mismatched RNAs than those containing 2'-O-carbamoyluridine (U(cm)). The stability of duplex with a U(abcm)-rG ba...

journal_title：Bioorganic & medicinal chemistry letters

authors： Seio K,Tokugawa M,Kanamori T,Tsunoda H,Ohkubo A,Sekine M

更新日期：2012-04-01 00:00:00

abstract：:A series of yohimbine dimers was prepared and evaluated at the human alpha2a- and alpha2b-adrenergic receptors (ARs) expressed in Chinese hamster ovary (CHO) cells. All dimers display higher binding selectivities for alpha2a versus alpha2b subtype than yohimbine, and four compounds (3d, 3e, 3g and 3i) represent the mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng W,Lei L,Lalchandani S,Sun G,Feller DR,Miller DD

更新日期：2000-04-03 00:00:00

abstract：:(+)-proto-Quercitol (1) and (-)-vibo-quercitol (2), both of which could be readily prepared by the bioconversion of myo-inositol, were successfully converted into the corresponding 4-methylenecyclohex-5-ene-1,2,3-triol derivatives. These compounds were demonstrated to be suitable precursors, preserving their configura...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kuno S,Takahashi A,Ogawa S

更新日期：2011-12-01 00:00:00

abstract：:A series of conformationally constrained 3-(N-alkylamino)propylphosphonic acids were systematically synthesized and their activities as S1P receptor agonists were evaluated. Several pyrrolidine and cyclohexane analogs had S1P receptor profiles comparable to the acyclic lead compound, 3-(N-tetradecylamino)propylphospho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan L,Hale JJ,Lynch CL,Budhu R,Gentry A,Mills SG,Hajdu R,Keohane CA,Rosenbach MJ,Milligan JA,Shei GJ,Chrebet G,Bergstrom J,Card D,Rosen H,Mandala SM

更新日期：2004-10-04 00:00:00

abstract：:A series of novel 1-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives 21-24 containing an oxime-functionalized pyrrolidine moiety were designed, synthesized and evaluated for their biological activity. Our results reveal that compounds 21a, 21e and 21j show considerable activity against MTB H37Rv ATCC 27294 (MICs...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang J,Liu H,Liu M,Zhang R,Li L,Wang B,Wang M,Wang C,Lu Y

更新日期：2015-11-15 00:00:00

abstract：:A series of heterobiaryl amides was designed and synthesized as novel mGluR5 antagonists. The synthesis using palladium catalyzed Suzuki-Miyaura cross-coupling reactions provided an array of compounds with a range of in vitro activities. In particular, compound 9e, 4(3,5-difluorophenyl)-N-(6-methylpyridin-1-yl)picolin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kulkarni SS,Newman AH

更新日期：2007-04-01 00:00:00

abstract：:We constructed a label-free and detector-free aptazyme-based riboswitch sensor for detecting the cofactor of the aptazyme. This riboswitch, which usually suppresses the gene expression with its anti-RBS sequence bound to the RBS of its own mRNA (OFF), activates the translation only when a cofactor is added to release ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogawa A,Maeda M

更新日期：2007-06-01 00:00:00

abstract：:In our efforts to develop CGRP receptor antagonists as backups to MK-3207, 2, we employed a scaffold hopping approach to identify a series of novel oxazolidinone-based compounds. The development of a structurally diverse, potent (20, cAMP+HS IC50=0.67 nM), and selective compound (hERG IC50=19 μM) with favorable rodent...

journal_title：Bioorganic & medicinal chemistry letters

authors： Crowley BM,Stump CA,Nguyen DN,Potteiger CM,McWherter MA,Paone DV,Quigley AG,Bruno JG,Cui D,Culberson JC,Danziger A,Fandozzi C,Gauvreau D,Kemmerer AL,Menzel K,Moore EL,Mosser SD,Reddy V,White RB,Salvatore CA,Kane S

更新日期：2015-11-01 00:00:00

abstract：:A group of novel quinoxalinone derivatives (4a-h) were prepared and investigated for their inhibitory activity against ALR2 and antioxidant activity. Most of them were found to be potent aldose reductase inhibitors with IC50 values ranging from 0.019 to 0.982 μM. The most active compound 2-(3-(4-hydroxyphenoxy)-6-fluo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zou Y,Qin X,Hao X,Zhang W,Yang S,Yang Y,Han Z,Ma B,Zhu C

更新日期：2015-09-15 00:00:00

abstract：:A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 microM) inhibitor that did not bear a zinc chelator. Structure-based drug design strategies were employed to append a Zn-chelating group to one end of the molecule and functionality to enhance selectivity to the other. A compound from th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wu J,Rush TS 3rd,Hotchandani R,Du X,Geck M,Collins E,Xu ZB,Skotnicki J,Levin JI,Lovering FE

更新日期：2005-09-15 00:00:00

abstract：:The steroidogenic enzyme 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) is a therapeutic target in the management of androgen-sensitive diseases such as prostate cancer and benign prostate hyperplasia. In this Letter, we designed and synthesized the first fluorescent inhibitor of this enzyme by combining a fluorog...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kenmogne LC,Maltais R,Poirier D

更新日期：2016-05-01 00:00:00

abstract：:We have developed two novel series of tetrasubstituted pyrazoles, embodying 1,3-diaryl-4,5-dialkyl or 3,5-diaryl-1,4-dialkyl substitution patterns. The scope of a regioselective method, developed by us earlier, was expanded to allow the synthesis of the first series of these tetrasubstituted pyrazoles directly from al...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nishiguchi GA,Rodriguez AL,Katzenellenbogen JA

更新日期：2002-03-25 00:00:00

abstract：:Matrix metalloproteinase-13 (MMP-13) has been implicated as the protease responsible for collagen degradation in cartilage during osteoarthritis (OA). Compounds that inhibit the metalloproteinase at the Zn binding site typically lack specificity among MMP family members. Analogs of the low-micromolar lead MMP-13 inhib...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roth J,Minond D,Darout E,Liu Q,Lauer J,Hodder P,Fields GB,Roush WR

更新日期：2011-12-01 00:00:00

abstract：:Sixteen new and one known unsymmetrical open-chain diacylamines were synthesized by sodium methoxide catalyzed acylation of amides with carboxylic esters and acylamino-carboxylic esters, or acylureas with acylamino-carboxylic esters and alpha-amino acid esters. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Weisz I,Roboz J,Wolf I,Szabo J,Bekesi JG

更新日期：1998-11-17 00:00:00

abstract：:Enedione derivatives of thieno[2,3-d]oxazinones are nanomolar inhibitors of CMV protease which act through a novel dual acylation of the catalytic serine and alkylation of the protease cysteine 161 via a Michael addition to the enedione moiety of the inhibitor. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pinto IL,Jarvest RL,Clarke B,Dabrowski CE,Fenwick A,Gorczyca MM,Jennings LJ,Lavery P,Sternberg EJ,Tew DG,West A

更新日期：1999-02-08 00:00:00

abstract：:We report SAR studies on a novel non-peptidic somatostatin receptor 3 (SSTR3) agonist lead series derived from (4-phenyl-1H-imidazol-2-yl)methanamine. This effort led to the discovery of a highly potent low molecular weight SSTR3 agonist 5c (EC50=5.2 nM, MW=359). The results from molecular overlays of 5c onto the L-12...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lai Z,He S,Sherer EC,Wu Z,Yu Y,Ball R,Hong Q,Yang DX,Guo L,Li D,Tuang Q,Chicchi GG,Trusca D,Tsao KL,Zhou YP,Howard AD,Nargund RP,Hagmann WK

更新日期：2015-09-01 00:00:00

abstract：:The addition of exogenous ent-cholesterol suppressed the antifungal activity of the amphotericin B when added to cultures of Candida albicans, but to a lesser extent than natural cholesterol. There were no detectable differences between added 2a or 2b on the antifungal activities of jaspamide or bengazole A, two unrel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Richter RK,Mickus DE,Rychnovsky SD,Molinski TF

更新日期：2004-01-05 00:00:00

abstract：:The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park CH,Choe H,Jang IY,Kwon SY,Latif M,Lee HK,Lee HJ,Yang EH,Yun JI,Chae CH,Cho SY,Choi SU,Ha JD,Jung H,Kim HR,Kim P,Lee CO,Yun CS,Lee K

更新日期：2013-11-15 00:00:00

abstract：:Currently, there is an ongoing interest in the synthesis of nucleoside diphosphate analogs as important regulators in catabolism/anabolism, and their potential applications as mechanistic probes and chemical tools for bioassays. However, the pyrophosphate bond formation step remains as the bottleneck. In this Digest, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu Z

更新日期：2015-09-15 00:00:00

abstract：:The use of doxorubicin (DOX) in the treatment of solid tumors is limited by cardiotoxicity essentially due to oxidative stress generation. The aim of this study was to identify coumarin derivatives displaying a protective antioxidant activity without affecting DOX antitumoral efficiency. A set of eighteen coumarinic d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beillerot A,Domínguez JC,Kirsch G,Bagrel D

更新日期：2008-02-01 00:00:00

abstract：:Antagonists of the TRPV4 receptor were identified using a focused screen, followed by a limited optimization program. The leading compounds obtained from this exercise, RN-1665 23 and RN-9893 26, showed moderate oral bioavailability when dosed to rats. The lead molecule, RN-9893 26, inhibited human, rat and murine var...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wei ZL,Nguyen MT,O'Mahony DJ,Acevedo A,Zipfel S,Zhang Q,Liu L,Dourado M,Chi C,Yip V,DeFalco J,Gustafson A,Emerling DE,Kelly MG,Kincaid J,Vincent F,Duncton MA

更新日期：2015-09-15 00:00:00

abstract：:The diastereoselective synthesis and structure activity relationship (SAR) of a series of fused cyclopropyl-3-amino-2,4-oxazine (2-oxa-4-azabicyclo[4.1.0]hept-3-en-3-amine)-containing BACE inhibitors is described. Through these efforts compound 2 was identified as a potent (cell IC50 = 15 nM) BACE inhibitor with accep...

journal_title：Bioorganic & medicinal chemistry letters

authors： Low JD,Bartberger MD,Cheng Y,Whittington D,Xue Q,Wood S,Allen JR,Minatti AE

更新日期：2018-04-01 00:00:00

abstract：:Preclinical studies suggest that compounds with dual norepinephrine reuptake inhibitor (NRI) and 5-HT(1A) partial agonist properties may provide an important new therapeutic approach to ADHD, depression, and anxiety. Reported herein is the discovery of a novel chemical series with a favorable NRI and 5-HT(1A) partial ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dounay AB,Barta NS,Campbell BM,Coleman C,Collantes EM,Denny L,Dutta S,Gray DL,Hou D,Iyer R,Maiti SN,Ortwine DF,Probert A,Stratman NC,Subedi R,Whisman T,Xu W,Zoski K

更新日期：2010-02-01 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