Thiadiazole: a new family of intercalative photonuclease with electron transfer and radical mechanisms.

abstract：:2-Propargylthiobenzimidazole 1, 4-bromomethyl coumarins/1-aza-coumarins 2/3 and sodium azide have been reacted in one pot under Click chemistry conditions to give exclusively 1,4-disubstituted triazoles 5a-n. Anti-tubercular assays against M. tuberculosis (H37Rv) coupled with in silico molecular docking studies indica...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anand A,Kulkarni MV,Joshi SD,Dixit SR

更新日期：2016-10-01 00:00:00

abstract：:Viral infectivity factor (Vif) is one of the accessory protein of human immunodeficiency virus type I (HIV-1) that inhibits host defense factor, APOBEC3G (A3G), mediated viral cDNA hypermutations. Previous work developed a novel Vif inhibitor 2-amino-N-(2-methoxyphenyl)-6-((4-nitrophenyl)thio)benzamide (1) with strong...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang RH,Wang S,Luo RH,Zhou M,Zhang H,Xu GB,Zhao YL,Li YJ,Wang YL,Yan G,Liao SG,Zheng YT,Li R

更新日期：2019-12-15 00:00:00

abstract：:A series of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential telomerase inhibitors were synthesized. The bioassay tests show that compound 3d exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC(50) value of 2.69 ± 0.60 μg/mL. All title compounds were assa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu XH,Liu HF,Chen J,Yang Y,Song BA,Bai LS,Liu JX,Zhu HL,Qi XB

更新日期：2010-10-01 00:00:00

abstract：:A series of cyclopropyl hydroxamic acids were prepared. Many of the compounds displayed picomolar affinity for the TACE enzyme while maintaining good to excellent selectivity profiles versus MMP-1, -2, -3, -7, -14, and ADAM-10. X-ray analysis of an inhibitor in the TACE active site indicated that the molecules bound t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mazzola RD Jr,Zhu Z,Sinning L,McKittrick B,Lavey B,Spitler J,Kozlowski J,Neng-Yang S,Zhou G,Guo Z,Orth P,Madison V,Sun J,Lundell D,Niu X

更新日期：2008-11-01 00:00:00

abstract：:Current antibiotics for treating Clostridium difficile infections (CDI), that is, metronidazole, vancomycin and more recently fidaxomicin, are mostly effective but treatment failure and disease relapse remain as significant clinical problems. The shortcomings of these agents are attributed to their low selectivity for...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen C,Doll NK,Casadei G,Bremner JB,Lewis K,Kelso MJ

更新日期：2014-01-15 00:00:00

abstract：:The search for novel, potent Kv1.5 blockers based on an anthranilic amide scaffold employing a pharmacophore-based virtual screening approach is described. The synthesis and structure-activity relationships (SAR) with respect to inhibition of the Kv1.5 channel are discussed. The most potent compounds display sub-micro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peukert S,Brendel J,Pirard B,Strübing C,Kleemann HW,Böhme T,Hemmerle H

更新日期：2004-06-07 00:00:00

abstract：:A series of novel ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives were designed and synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds exhibited acrosin inhibitory activities. Among them, three compounds (5l, 5n, and 5v) were more potent than that of the co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qi J,Zhu J,Liu X,Ding L,Zheng C,Han G,Lv J,Zhou Y

更新日期：2011-10-01 00:00:00

abstract：:A series of inhibitors of the soluble epoxide hydrolase (sEH) containing two urea groups has been developed. Inhibition potency of the described compounds ranges from 2.0 μM to 0.4 nM. 1,6-(Hexamethylene)bis[(adamant-1-yl)urea] (3b) was found to be a potent slow tight binding inhibitor (IC50=0.5 nM) with a strong bind...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burmistrov V,Morisseau C,Lee KS,Shihadih DS,Harris TR,Butov GM,Hammock BD

更新日期：2014-05-01 00:00:00

abstract：:Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jung HA,Paudel P,Seong SH,Min BS,Choi JS

更新日期：2017-06-01 00:00:00

abstract：:A series of orthoalkylaminophenol derivatives was synthesized and tested in vitro with respect to their neuroprotective effect. Some of these compounds exhibited a potent antioxidant activity close to that of standard alpha-tocopherol. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Larget R,Lockhart B,Pfeiffer B,Neudorffer A,Fleury MB,Largeron M

更新日期：1999-10-18 00:00:00

abstract：:We have developed a series of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors. Preliminary biological evaluation indicated that most compounds possessed inhibitory potencies comparable to, or higher than AZD-2281. Among these compounds, 18q appeared to be the most notable one, whic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang LX,Zhou XB,Xiao ML,Jiang N,Liu F,Zhou WX,Wang XK,Zheng ZB,Li S

更新日期：2014-08-15 00:00:00

abstract：:We synthesized calothrixin B using our developed biomimetic method and derived N-alkyl-calothrixins A and B. The in vitro antimalarial activity of the calothrixin derivatives, including calothrixins A and B, against the Plasmodium falciparum FCR-3 strain was evaluated. All test compounds exhibited antimalarial activit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matsumoto K,Choshi T,Hourai M,Zamami Y,Sasaki K,Abe T,Ishikura M,Hatae N,Iwamura T,Tohyama S,Nobuhiro J,Hibino S

更新日期：2012-07-15 00:00:00

abstract：:4-(Substituted-benzylidine)-2-substituted-5,6-dihydrobenzo[h]quinazoline (5a-p) and 4-(substituted-benzylidine)-2-substituted-3, 4, 5, 6-tetrahydrobenzo[h]quinazoline (6a-p) have been synthesized from 2-(substituted-benzylidine)tetralone-1(3a-d) and several substituted guanidine sulfates(4a-d).These compounds were tes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Agarwal KC,Sharma V,Shakya N,Gupta S

更新日期：2009-09-15 00:00:00

abstract：:A novel cosalane analog having an extended polyanionic pharmacophore was synthesized in order to target specific cationic residues on the surface of CD4. The design rationale is based on a hypothetical binding model of cosalane to the surface of the protein. The new analog displayed an EC50 of 0.55 microM as an inhibi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cushman M,Insaf S,Ruell JA,Schaeffer CA,Rice WG

更新日期：1998-04-07 00:00:00

abstract：:(R)-Glycerol-monolinoleate 4 and (R)-glycerol-monostearate 5 were isolated from the ethyl acetate extracts of Saururus chinensis roots and (R)- or (S)-fatty acid glycerols 4 and 5 were synthesized for confirming their structures and evaluating their inhibitory activities against Lp-PLA(2). The (R)-4 and (S)-4 exhibite...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee WS,Kim MJ,Beck YI,Park YD,Jeong TS

更新日期：2005-08-01 00:00:00

abstract：:This work describes the application of thermophilic microorganisms for obtaining 6-halogenated purine nucleosides. Biosynthesis of 6-chloropurine-2'-deoxyriboside and 6-chloropurine riboside was achieved by Geobacillus stearothermophilus CECT 43 with a conversion of 90% and 68%, respectively. Furthermore, the selected...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rivero CW,De Benedetti EC,Sambeth JE,Lozano ME,Trelles JA

更新日期：2012-10-01 00:00:00

abstract：:The synthesis and pharmacological activity of novel nociceptin/orphanin FQ (N/OFQ) analogues modified in the Phe(1)-Gly(2) peptide bond are reported. The aim of the present work was to elucidate the importance of this peptide bond for the N/OFQ receptor (NOP) interaction. Our study indicates that the first peptide bon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guerrini R,Rizzi D,Zucchini M,Tomatis R,Regoli D,Calo' G,Salvadori S

更新日期：2003-02-10 00:00:00

abstract：:A series of phosphate and ester-based prodrugs of anilinopyrazinone 1 (BMS-665053) containing either a methylene or an (acyloxy)alkoxy linker was prepared and evaluated in rat pharmacokinetic studies with the goal of improving the oral bioavailability of the parent (1). The prodrugs, in general, had improved aqueous s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hartz RA,Vrudhula VM,Ahuja VT,Grace JE,Lodge NJ,Bronson JJ,Macor JE

更新日期：2017-03-15 00:00:00

abstract：:Kynurenine monooxygenase (KMO) is a potential drug target for treatment of neurodegenerative disorders such as Huntington's and Alzheimer's diseases. We have evaluated substituted kynurenines as substrates or inhibitors of KMO from Cytophaga hutchinsonii. Kynurenines substituted with a halogen at the 5-position are ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Phillips RS,Anderson AD,Gentry HG,Güner OF,Bowen JP

更新日期：2017-04-15 00:00:00

abstract：:Despite the excellent in vitro potency of a series of benzamide glycoprotein IIb/IIIa antagonists, which have been reported previously, poor in vivo potency in the inhibition of platelet aggregation was observed when the most potent inhibitor XU057 was dosed intravenously to dogs. In this communication, we report that...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xue CB,Roderick J,Mousa S,Olson RE,DeGrado WF

更新日期：1998-12-15 00:00:00

abstract：:Albocycline (ALB) is a unique macrolactone natural product with potent, narrow-spectrum activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate (VISA), and vancomycin-resistant S. aureus (VRSA) strains (MIC = 0.5-1.0 μg/mL). Described herein is the synthesis and evaluation of a nov...

journal_title：Bioorganic & medicinal chemistry letters

authors： Daher SS,Franklin KP,Scherzi T,Dunman PM,Andrade RB

更新日期：2020-11-01 00:00:00

abstract：:Water is an essential part of protein binding sites and mediates interactions to ligands. Its displacement by ligand parts affects the free binding energy of resulting protein-ligand complexes. Therefore the characterization of solvation properties is important for design. Of particular interest is the propensity of l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matter H,Güssregen S

更新日期：2018-08-01 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：:Natural or synthetic coumarins showed gastroprotective and antiulcer activity in animal models. In this study, we have synthetized twenty coumarins using classic methods to evaluate their gastroprotective effects on the ethanol/HCl-induced gastric lesion model in mice at 20mg/kg. Among the coumarins synthetized, compo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sepulveda B,Quispe C,Simirgiotis M,Torres-Benítez A,Reyes-Ortíz J,Areche C,García-Beltrán O

更新日期：2016-12-01 00:00:00

abstract：:Pradimicins are a group of antiviral and antifungal natural products from Actinomadura hibisca. Two putative O-methyltransferase genes, pdmF and pdmT, are present in the pradimicin biosynthetic gene cluster. However, there is only one methoxy group (11-OCH3) in pradimicins. Through heterologous expression and in vitro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu F,Napan K,Zhang S,Gladwin T,Takemoto J,Zhan J

更新日期：2017-08-01 00:00:00

abstract：:Analogues of BIBP 3226, (R)-N(alpha)-diphenylacetyl-N-(4-hydroxybenzyl)argininamide, were synthesized and investigated for Y1 antagonism (Ca2+-assay, HEL cells) and binding on Y1, Y2 and Y5 receptors. Replacing the benzylamino by a tetrahydrobenzazepinyl group preserves most of the Y1 activity. Combination with a N(G)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aiglstorfer I,Hendrich I,Moser C,Bernhardt G,Dove S,Buschauer A

更新日期：2000-07-17 00:00:00

abstract：:(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (1b) has been identified as a potent CCR5 antagonist having an IC50=10 nM. Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the disco...

journal_title：Bioorganic & medicinal chemistry letters

authors： Finke PE,Oates B,Mills SG,MacCoss M,Malkowitz L,Springer MS,Gould SL,DeMartino JA,Carella A,Carver G,Holmes K,Danzeisen R,Hazuda D,Kessler J,Lineberger J,Miller M,Schleif WA,Emini EA

更新日期：2001-09-17 00:00:00

abstract：:Ascorbic acid 2-glucoside (AA-2G) has been widely used in cream and lotion types of cosmetic products. Thus, the degradation of AA-2G caused by the temperature change and pH variation was very critical for determining the bio-functionality of cosmetics. Response surface methodology (RSM) was introduced to study the in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang WY,Lee PC,Huang LK,Lu LP,Liao WC

更新日期：2013-03-15 00:00:00

abstract：:In the study, we demonstrated that freezing was able to facilitate the short DNA strand T(4)G(4) to self-assemble into a tetramolecular G-quadruplex with a low DNA concentration in the absence of any ligand, providing a fast approach to configure intermolecular G-quadruplexes. The fast formation of intermolecular G-qu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhai Q,Deng M,Xu L,Zhang X,Zhou X

更新日期：2012-01-15 00:00:00

abstract：:Synthesis, pharmacology, and pharmacokinetic profiles of (1R, 2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile are reported. This compound demonstrated remarkable potency for stimulating hair growth in a male C3H mouse model as well as reducing sebum production in the male Syrian hamster ear model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hu LY,Du D,Hoffman J,Smith Y,Fedij V,Kostlan C,Johnson TR,Huang Y,Kesten S,Harter W,Yue WS,Li JJ,Barvian N,Mitchell L,Lei HJ,Lefker B,Carroll M,Dettling D,Krieger-Burke T,Samas B,Yalamanchili R,Lapham K,Pocaly

更新日期：2007-11-01 00:00:00