Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.

abstract：:Regioselective synthesis of a number of highly functionalized 3-benzylpyrimidino chromen-2-ones (4) were accomplished in a one pot three component reaction in acetic acid and determined their anti-microbial and anti-biofilm activities. Compounds 4o and 4p showed an excellent anti-microbial activity against Micrococcus...

journal_title：Bioorganic & medicinal chemistry letters

authors： Emmadi NR,Atmakur K,Bingi C,Godumagadda NR,Chityal GK,Nanubolu JB

更新日期：2014-01-15 00:00:00

abstract：:Pholasin is a bioluminescent photoprotein of Pholas dactylus. Pholasin is a commercially available photoprotein used to measure intracellular reactive oxygen species. Although extensive efforts have been carried out to determine the chemical structure of the prosthetic (chromophore) group, it still remains unclear to ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kuse M,Tanaka E,Nishikawa T

更新日期：2008-10-15 00:00:00

abstract：:Over the past 15years there have been extensive efforts to understand and reduce the high attrition rates of drug candidates with an increased focus on physicochemical properties. The fruits of this labor have been the generation of numerous efficiency indices, metric-based rules and visualization tools to help guide ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shultz MD

更新日期：2013-11-01 00:00:00

abstract：:4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production. One of the compounds (6e) was found to be efficacious in the rat iodoacetate (RIA) in vivo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Golebiowski A,Townes JA,Laufersweiler MJ,Brugel TA,Clark MP,Clark CM,Djung JF,Laughlin SK,Sabat MP,Bookland RG,VanRens JC,De B,Hsieh LC,Janusz MJ,Walter RL,Webster ME,Mekel MJ

更新日期：2005-05-02 00:00:00

abstract：:A new route to 17 beta-substituted-6-azaandrost-4-en-3-ones, potent dual inhibitors of type 1 and 2 steroidal 5 alpha-reductase, is described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharp MJ,Fang FG

更新日期：1998-12-01 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：:Developing efficient controlled release system of insecticide can facilitate the better use of insecticide. We described here a first example of photo-controlled release of an insecticide by linking fipronil with photoresponsive coumarin covalently. The generated coumarin-fipronil (CF) precursor could undergo cleavage...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gao Z,Yuan P,Wang D,Xu Z,Li Z,Shao X

更新日期：2017-06-01 00:00:00

abstract：:SAR exploration at C-6 and C-8 positions of the tricyclic sulfone series was carried out. Several functional groups were found to be well tolerated at C-6 and C-8 positions. Selective combination of C-6 and C-8 modification resulted in new tricyclic sulfone analogs with efficacy in in vivo mouse Aβ(40) lowering model....

journal_title：Bioorganic & medicinal chemistry letters

authors： Su J,Tang H,McKittrick BA,Xu R,Clader JW,Greenlee WJ,Hyde L,Zhang L

更新日期：2011-06-01 00:00:00

abstract：:The effect of 2,3 modifications on the antibacterial activity of ketolides was evaluated by introducing substituents in position 2 and converting the C-1, C-2, C-3 beta-keto-ester into stable 2,3 enol-ether or 2,3 anhydro derivatives. Introduction of a fluorine in C-2 is beneficial with regard to the overall antibacte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Denis A,Bretin F,Fromentin C,Bonnet A,Piltan G,Bonnefoy A,Agouridas C

更新日期：2000-09-04 00:00:00

abstract：:The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S,3R)-N-{[1-(3-chloropyridin-2-yl)-5-(5-fluoro-6-methylpyridin-3-yl)-4-methyl-1...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kobayashi K,Uchiyama M,Ito H,Takahashi H,Yoshizumi T,Sakoh H,Nagatomi Y,Asai M,Miyazoe H,Tsujita T,Hirayama M,Ozaki S,Tani T,Ishii Y,Ohta H,Okamoto O

更新日期：2009-07-01 00:00:00

abstract：:1-((Substituted)methyl)quinoxaline-2,3(1H,4H)-dione (2a-e) and 1-((substituted)acryloyl)quinoxaline-2,3(1H,4H)-dione (4a-c) were synthesized from quinoxaline-2,3(1H,4H)-dione 1 and evaluated for their antimicrobial activities. Results of the antitubercular screening against Mycobacterium tuberculosis H(37)Rv showed th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramalingam P,Ganapaty S,Rao ChB

更新日期：2010-01-01 00:00:00

abstract：:A series of acetylcholine carbamoyl analogues, cyclised at the carbamate moiety or at the cationic head or at both, were tested for binding affinity at muscarinic and neuronal nicotinic receptors (nAChRs). While no muscarinic affinity was found, submicromolar Ki values, similar to that of carbachol, were measured at α...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bolchi C,Valoti E,Binda M,Fasoli F,Ferrara R,Fumagalli L,Gotti C,Matucci R,Vistoli G,Pallavicini M

更新日期：2013-12-01 00:00:00

abstract：:In the search of molecules that can serve as leads in the design of a new drug for the treatment of Chagas' disease, we found that some brevifolin carboxylate derivatives isolated from Geranium bellum Rose, inactivate triosephosphate isomerase from Trypanosoma cruzi (TcTIM) in a species-specific manner. After spectros...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gayosso-De-Lucio J,Torres-Valencia M,Rojo-Domínguez A,Nájera-Peña H,Aguirre-López B,Salas-Pacheco J,Avitia-Domínguez C,Téllez-Valencia A

更新日期：2009-10-15 00:00:00

abstract：:A group of sixteen iridoids isolated from plants used as anti-inflammatory remedies in Mexican folk medicine were evaluated for their potential to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. From these assays, loganic acid (10) was identified as the most promising compound with both COX-1 (3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramírez-Cisneros MÁ,Rios MY,Aguilar-Guadarrama AB,Rao PP,Aburto-Amar R,Rodríguez-López V

更新日期：2015-10-15 00:00:00

abstract：:Optimisation of a series of 4-piperidinyltriazoles led to the identification of compound 28a which showed good whole cell antiviral activity, excellent selectivity over the hERG ion channel and complete oral absorption. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barber CG,Blakemore DC,Chiva JY,Eastwood RL,Middleton DS,Paradowski KA

更新日期：2009-03-01 00:00:00

abstract：:A developing therapy of cystic fibrosis caused by the DeltaF508 mutation in CFTR employs correction of defective CFTR chloride channel gating by a 'potentiator' and of defective CFTR protein folding by a 'corrector'. Based on SAR data for phenylglycine-type potentiators and bithiazole correctors, we designed a hybrid ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mills AD,Yoo C,Butler JD,Yang B,Verkman AS,Kurth MJ

更新日期：2010-01-01 00:00:00

abstract：:A short route to pyrimidine locked nucleosides has been developed for their incorporation in triplex forming oligonucleotides (TFO). Compared to oligonucleotides built with standard nucleosides, the modified TFOs containing 3'-endo blocked residues formed, with their corresponding DNA duplexes, more stable triple heli...

journal_title：Bioorganic & medicinal chemistry letters

authors： Savy P,Benhida R,Fourrey JL,Maurisse R,Sun JS

更新日期：2000-10-16 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：:In this Letter, we report the structure-activity relationship (SAR) studies on series of positional isomers of 5(6)-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles derivatives 7(a-j) and 8(a-j) synthesized in good yields and characterized by (1)H NMR, (13)C NMR and mass spectral analyses. The c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ranjith PK,Rajeesh P,Haridas KR,Susanta NK,Row TN,Rishikesan R,Kumari NS

更新日期：2013-09-15 00:00:00

abstract：:This study explores the possible use of reactive oxygen-activated DNA modifying agents against acute myeloid leukemia (AML). A key amine on the lead agent was investigated via cytotoxicity assays and was found necessary for potency. The two best compounds were screened via the NCI-60 cell panel. These two compounds ha...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bell-Horwath TR,Vadukoot AK,Thowfeik FS,Li G,Wunderlich M,Mulloy JC,Merino EJ

更新日期：2013-05-15 00:00:00

abstract：:Investigation of hydrophobic extract of Dichondra repens (Convolvulaceae) led to the isolation of three new resin glycosides dichondrins A-C (1-3), and three known resin glycosides cus-1, cus-2, and cuse 3. All the isolated resin glycosides with an acyclic core were evaluated for their multidrug resistance reversal ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Song WB,Wang WQ,Zhang SW,Xuan LJ

更新日期：2015-02-15 00:00:00

abstract：:Using structure-based optimization procedures on in silico hits, dibenzosuberyl- and benzoate substituted tropines were designed as ligands for acetylcholine-binding protein (AChBP). This protein is a homolog to the ligand binding domain of the nicotinic acetylcholine receptor (nAChR). Distinct SAR is observed between...

journal_title：Bioorganic & medicinal chemistry letters

authors： Edink E,Akdemir A,Jansen C,van Elk R,Zuiderveld O,de Kanter FJ,van Muijlwijk-Koezen JE,Smit AB,Leurs R,de Esch IJ

更新日期：2012-02-01 00:00:00

abstract：:The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are inter...

journal_title：Bioorganic & medicinal chemistry letters

authors： Douty B,Wayland B,Ala PJ,Bower MJ,Pruitt J,Bostrom L,Wei M,Klabe R,Gonneville L,Wynn R,Burn TC,Liu PC,Combs AP,Yue EW

更新日期：2008-01-01 00:00:00

abstract：:A novel application of distance-based topological indices : Wiener (W)-, Szeged (Sz)-, Padmakar-Ivan (PI)-, and Sadhana (Sd)-indices in modeling electronic absorption bands of arene absorption spectra has been described. It is demonstrated that all these indices correlate linearly with the logarithm of beta and para e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Khadikar PV,Singh S,Jaiswal M,Mandloi D

更新日期：2004-09-20 00:00:00

abstract：:Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive. We report here a novel series non-peptidic phenyl-based, highly potent, highly selective and orally bioavailable thrombin inhibi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tomczuk B,Lu T,Soll RM,Fedde C,Wang A,Murphy L,Crysler C,Dasgupta M,Eisennagel S,Spurlino J,Bone R

更新日期：2003-04-17 00:00:00

abstract：:Twenty three side chain analogs of the crambescidin alkaloids were prepared from the corresponding pentacyclic zwitterionic core acid. In the crambescidin 800 and 657 series, potency increased with increasing chain length. In addition, substantial variations in tumor selectivity with structure were seen. Crambescidin ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aron ZD,Pietraszkiewicz H,Overman LE,Valeriote F,Cuevas C

更新日期：2004-07-05 00:00:00

abstract：:Novel pyrroloimidazoles have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor subtypes. Pyrimidine 19 possessed attractive CNS drug-like properties with good membrane permeability and no evidence for P-gp mediate...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roberts LR,Fish PV,Ian Storer R,Whitlock GA

更新日期：2009-06-01 00:00:00

abstract：:This paper describes the preliminary biological results that novel T-type calcium channel blockers inhibit the growth of human cancer cells by blocking calcium influx into the cell, based on unknown mechanism on the cell cycle responsible for cellular proliferation. Among the selected compounds from compound library, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JY,Park SJ,Park SJ,Lee MJ,Rhim H,Seo SH,Kim KS

更新日期：2006-10-01 00:00:00

abstract：:Transglutaminase 2 (TG2) is a ubiquitously expressed, Ca(2+)-activated extracellular enzyme in mammals that is maintained in a catalytically dormant state by multiple mechanisms. Although its precise physiological role in the extracellular matrix remains unclear, aberrantly up-regulated TG2 activity is a hallmark of s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yi MC,Palanski BA,Quintero SA,Plugis NM,Khosla C

更新日期：2015-11-01 00:00:00

abstract：:Penicillium digitatum, as well as five other citrus pathogenic species, (Penicillium ulaiense Link, Geotrichum citri Link, Botrytis cinerea P. Micheli ex Pers., Lasiodiplodia theobromae (Pat.) Griffon & Maubl., and Phomopsis citri (teleomorph Diaporthe citri)) were observed to convert 6',7'-epoxybergamottin (1) into 6...

journal_title：Bioorganic & medicinal chemistry letters

authors： Myung K,Manthey JA,Narciso JA

更新日期：2012-03-15 00:00:00