Silanediol-based inhibitor of thermolysin.

abstract：:We have designed, synthesized, and evaluated the factor Xa inhibitory activities of p-amidinophenyl-sulfones, amines, and alcohols intended to take advantage of the polarity and hydrogen-bonding potential of the oxyanion hole region of the S1 specificity pocket. We demonstrate that placement of an anionic group within...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rumthao S,Lee O,Sheng Q,Fu W,Mulhearn DC,Crich D,Mesecar AD,Johnson ME

更新日期：2004-10-18 00:00:00

abstract：:Macromolecular chelators have potential applications in the medical area, for instance, in treatment of iron overload-related disorders and in the treatment of external infections. In this investigation, several novel iron(III)-selective hydroxypyridinone hexadentate-terminated first and second generation dendrimeric ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou T,Chen K,Kong LM,Liu MS,Ma YM,Xie YY,Hider RC

更新日期：2018-08-01 00:00:00

abstract：:Novel, metabolically stable and centrally acting TRH analogues with substituted pyridinium moieties replacing the [His(2)] residue of the endogenous peptide were prepared by solid-phase Zincke reaction. The 1,4-dihydropyridine prodrugs of these analogues obtained after reducing the pyridinium moiety were able to reach...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prokai-Tatrai K,Perjési P,Zharikova AD,Li X,Prokai L

更新日期：2002-08-19 00:00:00

abstract：:NCSi-gb is a neocarzinostatin chromophore (NCS-chrom) metabolite which binds strongly to certain two-base DNA bulges. Compared with previously reported NCSi-gb analogues, a new analogue with a different aminoglycoside position was synthesized, and it showed strong fluorescence and improved binding and sequence selecti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao Z,Kappen LS,Goldberg IH

更新日期：2006-06-01 00:00:00

abstract：:Some ergostane triterpenoids from Taiwanofungus camphoratus have been shown to exhibit anti-inflammatory activity in vitro. However, the effect of ergostane triterpenoids on the immune response remains unknown. In this study, we elucidated that ergostane triterpenoids significantly decreased the cytokines and chemokin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lin MK,Lee MS,Chang WT,Chen HY,Chen JF,Li YR,Lin CC,Wu TS

更新日期：2015-10-15 00:00:00

abstract：:The reaction mechanisms of hypochlorous acid (HOCl) with several tryptophan and tryptamine derivatives, previously reported to scavenge this powerful oxidant, was investigated to determine whether ionic or radical pathways were involved. For this purpose, the reaction of tryptamine and tryptophan derivatives with HOCl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carvalho LC,Estevão MS,Ferreira LM,Fernandes E,Marques MM

更新日期：2010-11-15 00:00:00

abstract：:Dopamine-mediated neurotransmission plays an important role in relevant psychiatric and neurological disorders. Nowadays, there is an enormous interest in the development of new drugs acting at the dopamine receptors (DR) as potential new targets for the treatment of schizophrenia or Parkinson's disease. Previous stud...

journal_title：Bioorganic & medicinal chemistry letters

authors： Moreno L,Cabedo N,Ivorra MD,Sanz MJ,Castel AL,Carmen Álvarez M,Cortes D

更新日期：2013-09-01 00:00:00

abstract：:A novel type of caspase inhibitor prodrug that improves systemic exposure after oral administration in rats has been designed. Such a prodrug, based on a 6,6a-dihydrofuro[3,2-d]oxazol-5(3aH)-one motif, has the advantage of rapidly liberating the active inhibitor without producing any cleavage by-product. Prodrugs 6-8,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Charrier JD,Durrant SJ,Studley J,Lawes L,Weber P

更新日期：2012-01-01 00:00:00

abstract：:Oligodeoxynucleotides containing 2'-O-beta-D-ribofuranosyladenosine were prepared and used as modified primers in RNA-templated DNA synthesis catalyzed by HIV reverse transcriptase. It was shown that the additional 2'-ribofuranose residue in specific position of primer prevents its elongation. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Andreeva OI,Golubeva AS,Kochetkov SN,Van Aerschot A,Herdewijn P,Efimtseva EV,Ermolinsky BS,Mikhailov SN

更新日期：2002-02-25 00:00:00

abstract：:Recent studies have found that phthalonitrile derivatives are remarkably potent inhibitors of human monoamine oxidase (MAO) A and B. In an attempt to further determine the structure-activity relationships (SARs) for MAO inhibition by this class of compounds and to discover novel potent MAO inhibitors, the present stud...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chirkova ZV,Kabanova MV,Filimonov SI,Abramov IG,Petzer A,Petzer JP,Firgang SI,Suponitsky KY

更新日期：2015-03-15 00:00:00

abstract：:Cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase (TS) possess a chiral centre at the 6-position of the molecule. The effect of this chirality on the inhibition of TS was investigated by synthesising compounds 6S-1a-c, 6R-1a-c. It was shown, in particular with the diastereoisomers 6S-1c, 6R-1c, that th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bavetsias V,Marriott JH,Theti DS,Melin JC,Wilson SC,Jackman AL

更新日期：2001-12-03 00:00:00

abstract：:Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Duncia JV,Santella JB 3rd,Higley CA,VanAtten MK,Weber PC,Alexander RS,Kettner CA,Pruitt JR,Liauw AY,Quan ML,Knabb RM,Wexler RR

更新日期：1998-04-07 00:00:00

abstract：:The pRBM4 cosmid, which harbors a putative cluster of genes spanning a 31.8-kb chromosomal region of the ribostamycin producer Streptomyces ribosidificus ATCC 21294, was heterologously expressed in Streptomyces lividans TK24. ESI-MS/MS, HPLC, and LC-ESI MS analyses showed that the transformation gave rise to ribostamy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Subba B,Kurumbang NP,Jung YS,Yoon YJ,Lee HC,Liou K,Sohng JK

更新日期：2007-04-01 00:00:00

abstract：:Recently, a disulfide-based cyclic RGD peptide called iRGD, that is, c(CRGDKGPDC), has been reported to interact with both integrin and neuropilin-1 receptors for cellular and deep tissue penetration to improve the imaging sensitivity and therapeutic efficacy. In this study, two new near-infrared fluorescent iRGD conj...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ye Y,Zhu L,Ma Y,Niu G,Chen X

更新日期：2011-02-15 00:00:00

abstract：:The methylendioxyphenyl group, present in a number of potent endothelin receptor antagonists, could have undesirable metabolic interactions with cytochrome P450 in vivo. Using a self-organizing neural network we analysed the features of molecular electrostatic potentials of several endothelin receptor ligands. A libra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anzali S,Mederski WW,Osswald M,Dorsch D

更新日期：1998-01-06 00:00:00

abstract：:A series of dehydroabietic acid (DHAA, 2) derivatives was synthesized and evaluated as BK channel openers in an assay system of CHO-K1 cells expressing hBKalpha channels. Systematic modifications of the peripheral functionality of ring C of DHAA showed that the introduction of a nitro or (thio)urea group in ring C gre...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cui YM,Yasutomi E,Otani Y,Yoshinaga T,Ido K,Sawada K,Ohwada T

更新日期：2008-10-01 00:00:00

abstract：:The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in 1 can be replaced by a simple, substituted aromatic ring such as a toluene in 2. The resulting compounds exhibit subnanomolar ren...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lacombe P,Aspiotis R,Bayly C,Chen A,Dubé D,Fortin R,Gallant M,Juteau H,Liu S,McKay D,Roy P,Wu T

更新日期：2010-10-01 00:00:00

abstract：:New inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) were discovered using an N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamide scaffold. The series was found to be potent in a porcine TACE (pTACE) assay with IC(50)s typically below 5 nM. For most compounds, selectivity for pTACE relative to MMP-1,-2, and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Duan JJ,Lu Z,Xue CB,He X,Seng JL,Roderick JJ,Wasserman ZR,Liu RQ,Covington MB,Magolda RL,Newton RC,Trzaskos JM,Decicco CP

更新日期：2003-06-16 00:00:00

abstract：:The new binuclear platinum(II) complexes, (1,3-benzenedimethanethiolate-S)di(2,2',2"-terpyridine)diplatinum(II) chloride tetrahydrate, 5, and (1,4-benzenedimethanethiolate-S)di(2,2',2"-terpyridine)diplatinum(II) chloride tetrahydrate, 6, were synthesized in order to investigate the binding of platinum(II) complex with...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kurosaki H,Yamakawa N,Sumimoto M,Kimura K,Goto M

更新日期：2003-03-10 00:00:00

abstract：:We have previously reported the essential structure of the opioid κ receptor agonist nalfurafine hydrochloride (TRK-820) for binding to the κ receptor. In the course of this study, we focused on the effect of the substituent at 17-N in nalfurafine on the binding affinity for the κ receptor. The exchange of the 17-N su...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nemoto T,Yamamoto N,Wada N,Harada Y,Tomatsu M,Ishihara M,Hirayama S,Iwai T,Fujii H,Nagase H

更新日期：2013-01-01 00:00:00

abstract：:Aiming to develop a new (99m)Tc-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free α-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with (99m)Tc using tricine and TPPTS as co-ligan...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guo H,Xie F,Zhu M,Li Y,Yang Z,Wang X,Lu J

更新日期：2011-04-01 00:00:00

abstract：:In continuation of our earlier work on benzothiadiazines, we have prepared a series of nitrofuran, nitrothiophene and arylfuran coupled benzothiadiazines and evaluated them for antimycobacterial and antibacterial activities. One of the compounds 2f has shown good in vitro antimycobacterial activity. All the synthesize...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Ahmed SK,Reddy KS,Khan MN,Shetty RV,Siddhardha B,Murthy US,Khan IA,Kumar M,Sharma S,Ram AB

更新日期：2007-10-01 00:00:00

abstract：:An inibition study of the β-carbonic anhydrase (CA, EC 4.2.1.1) DmBCA from the insect Drosophila melanogaster with sulfonamides and sulfamates is reported. Among the panel of 40 investigated compounds, the best DmBCA inhibitors were the sulfonylated benzenesulfonamides and ethoxzolamide, which showed inhibition consta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Syrjänen L,Parkkila S,Scozzafava A,Supuran CT

更新日期：2014-07-01 00:00:00

abstract：:Thienylpyrimidines substituted at position 2 of the pyrimidine with a chiral aminoalkoxy group were synthesized. Upon interaction with duplex DNA, the unfused heteroaromatic system of these compounds intercalates with DNA base pairs and the protonated side chain is located in the major groove. The S-enantiomers bind m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Strekowski L,Cegla MT,Honkan V,Buczak H,Winkeljohn WR,Baumstark AL,Wilson WD

更新日期：2005-06-02 00:00:00

abstract：:A new glucuronylated prodrug of nornitrogen mustard, incorporating the same spacer group as the doxorubicin prodrug HMR 1826, has been prepared. Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Papot S,Combaud D,Bosslet K,Gerken M,Czech J,Gesson JP

更新日期：2000-08-21 00:00:00

abstract：:A facile 1,3-dipolar cycloaddition of azomethine ylide generated in situ from the reaction of 1,3-thiazolane-4-carboxylic acid and isatin to 2-arylidene-1,3-indanediones furnished novel dispiro-oxindolylpyrrolothiazoles regio- and stereo-selectively in moderate to good yields (60-92%). In vitro antitubercular screenin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Maheswari SU,Balamurugan K,Perumal S,Yogeeswari P,Sriram D

更新日期：2010-12-15 00:00:00

abstract：:A rational fluorine scan based on co-crystal structures was explored to increase the potency of a series of selective BTK inhibitors. While fluorine substitution on a saturated bicyclic ring system yields no apparent benefit, the same operation on an unsaturated bicyclic ring can increase HWB activity by up to 40-fold...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lou Y,Sweeney ZK,Kuglstatter A,Davis D,Goldstein DM,Han X,Hong J,Kocer B,Kondru RK,Litman R,McIntosh J,Sarma K,Suh J,Taygerly J,Owens TD

更新日期：2015-01-15 00:00:00

abstract：:Early studies led to the identification of 11β-aryl-4',5'-dihydrospiro[estra-4,9-diene-17β,4'-oxazole] analogs with potent and more selective antiprogestational activity compared to antiglucocorticoid activity than mifepristone. In the present study, we replaced the 4'-dimethylaminophenyl group of mifepristone with th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin C,Fix SE,Kepler JA,Cook CE

更新日期：2012-02-15 00:00:00

abstract：:A series of novel 9-O-arylalkyloxime analogs based on three different 16-membered macrolide scaffolds-5-O-mycaminosyltylonolide (OMT), tilmicosin, and 20-deoxy-20-(3,5-dimethyl-1-piperidin-1-yl)-OMT-was synthesized. In vitro antibiotic activities were assayed against Gram-positive Streptococcus pneumoniae and Staphylo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fu H,Marquez S,Gu X,Katz L,Myles DC

更新日期：2006-03-01 00:00:00

abstract：:The synthesis and evaluation of antiplasmodial activity of benzothiazole, benzimidazole, benzoxazole and pyridine analogues of amodiaquine is hereby reported. Benzothiazole and benzoxazole analogues with a protonatable tertiary nitrogen atom possessed excellent activity against the W2 and K1 chloroquine resistant stra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ongarora DS,Gut J,Rosenthal PJ,Masimirembwa CM,Chibale K

更新日期：2012-08-01 00:00:00