Slow generation of hydrogen sulfide from sulfane sulfurs and NADH models.

abstract：:The synthesis and inhibitory activities of 10 potential inhibitors of Pfmrk, a Plasmodium falciparum cyclin-dependent protein kinase, are described. The most potent inhibitor is a 3-phenyl-quinolinone compound with an IC(50) value of 18 microM. It is the first compound reported to inhibit Pfmrk at the micro molar rang...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao Z,Waters NC,Woodard CL,Li Z,Li PK

更新日期：2001-11-05 00:00:00

abstract：:The investigation of the Vietnamese marine sponge Spongia sp. led to the isolation of three new sesquiterpene phenols, langconols A-C (1-3), and one new sesquiterpene hydroxyquinone, langcoquinone C (4), together with two known meroterpenoids (5 and 6). Their structures were determined on the basis of spectroscopic an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen HM,Ito T,Kurimoto SI,Ogawa M,Win NN,Hung VQ,Nguyen HT,Kubota T,Kobayashi J,Morita H

更新日期：2017-07-15 00:00:00

abstract：:The development of novel non-phosphopeptide inhibitors for the Src family SH2 domain is described. Several commercially available hydroxyl aromatic acids have been appended off the N-terminus of pYEEIE and the potent phosphopeptide inhibitors of GST-Lck-SH2 were identified via ELISA. The most potent inhibitor, caffeic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park SH,Won J,Lee KH

更新日期：2002-10-07 00:00:00

abstract：:Bergenin is an isocoumarin natural product which aides in fat loss, healthy weight maintenance, enhancing the lipolytic effects of norepinephrine, inhibiting the formation of interleukin 1α and cyclooxygenases-2. Here we describe the anti-inflammatory activity of new bergenin derivatives 1-15 in the respiratory burst ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shah MR,Arfan M,Amin H,Hussain Z,Qadir MI,Choudhary MI,VanDerveer D,Mesaik MA,Soomro S,Jabeen A,Khan IU

更新日期：2012-04-15 00:00:00

abstract：:The reactivity of 4-[13C]- and 5-[13C]-5-chloro-2-methylisothiazol-3-one (MCI) and 2-methylisothiazol-3-one (MI) towards a model peptide and glutathione was followed by 13C and 1H[13C] NMR spectroscopy. Both molecules were found to react with GSH but in addition MCI was found to react with histidine and lysine to form...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alvarez-Sánchez R,Basketter D,Pease C,Lepoittevin JP

更新日期：2004-01-19 00:00:00

abstract：:A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various amide modifications and substitution on the left side phenyl ring were prepared and found to show significant inhibitory activities towards both CXCR2 and CXCR1 receptors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aki C,Chao J,Ferreira JA,Dwyer MP,Yu Y,Chao J,Merritt RJ,Lai G,Wu M,Hipkin RW,Fan X,Gonsiorek W,Fosseta J,Rindgen D,Fine J,Lundell D,Taveras AG,Biju P

更新日期：2009-08-01 00:00:00

abstract：:Four novel mononuclear complexes, [Cd(L)2·2H2O] (1), [Ni(L)2·2H2O] (2) [Cu(L)2·H2O] (3), and [Zn(L)2·2H2O] (4) (CCDC numbers: 1444630-1444633 for complexes 1-4) (HL=4-(2,3-dichlorophenyl)piperazine-1-carboxylic acid) were synthesized, and have been characterized by IR spectroscopy, elemental analysis, and X-ray crysta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang DD,Chen YN,Wu YS,Wang R,Chen ZJ,Qin J,Qian SS,Zhu HL

更新日期：2016-07-15 00:00:00

abstract：:Regiospecific synthesis of 2,3-disubstituted-L-histidines and 2,3-disubstituted histamines starting from L-histidine methyl ester and histamine is reported. The key step involves homolytic free radical alkylation via silver catalyzed oxidative decarboxylation of alkylcarboxylic acids with ammonium persulfate. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Narayanan S,Vangapandu S,Jain R

更新日期：2001-05-07 00:00:00

abstract：:High throughput screening for β-lactamase inhibitors afforded biphenyl hits such as 1. Hit confirmation and X-ray soaking experiments with Pseudomonas Aeruginosa AmpC enzyme led to the identification of an aryl boronic acid-serine complex 4, which was formed from phenyl boronic acid 8 (an impurity in compound 1) and e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang SW,Pan J,Root Y,Scapin G,Xiao L,Su J

更新日期：2020-01-15 00:00:00

abstract：:The effect of methanesulfonamide (MeSO(2)NH) group on COX-2 inhibitory activity of 1,5-diarylpyrazole is described. While this group being at position-4 of the N(1)-phenyl ring was found to be ineffective, its installation at position-4 of the C-5 phenyl ring offered several potent and selective inhibitors of COX-2 wi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh SK,Vobbalareddy S,Shivaramakrishna S,Krishnamraju A,Rajjak SA,Casturi SR,Akhila V,Rao YK

更新日期：2004-04-05 00:00:00

abstract：:Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P(1) benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deaton DN,Gao EN,Graham KP,Gross JW,Miller AB,Strelow JM

更新日期：2008-01-15 00:00:00

abstract：:A series of new class of 4-(hetero)aryl-2-piperazino quinazolines were synthesized and assessed for in vitro activity against extracellular promastigotes and intracellular amastigotes of Leishmania donovani. Among the compounds evaluated, compound 4bb and 4cb showed the selectivity index (SI) value>8.03 and 4.21, resp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumar S,Shakya N,Gupta S,Sarkar J,Sahu DP

更新日期：2009-05-01 00:00:00

abstract：:The Hedgehog (Hh-) signalling pathway is a key developmental pathway and there is a growing body of evidence showing that this pathway is aberrantly reactivated in a number of human tumors. Novel agents capable of inhibiting this pathway are sought, and an entirely novel series of smoothened (Smo) antagonists capable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ontoria JM,Bufi LL,Torrisi C,Bresciani A,Giomini C,Rowley M,Serafini S,Bin H,Hao W,Steinkühler C,Jones P

更新日期：2011-09-15 00:00:00

abstract：:This study aims to develop novel azatyrosinamide compounds structurally modified from ras-specific antioncogenic azatyrosine. Analogues 4-15 were prepared and their inhibition on the growth of wild-type and ras-transformed NIH 3T3 cell lines was compared. Compound 12 was found to be the most active with IC50 16.5+/-2....

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang HP,Hwang TL,Lee O,Tseng YJ,Shu CY,Lee SJ

更新日期：2005-10-01 00:00:00

abstract：:A series of pyrazole and triazole derivatives containing 5-phenyl-2-furan functionality were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. The bioassay results showed that title compounds exhibited considerable inhibitory activity against PDE4B and blockade of LPS-induced TNFα release. Meanwh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li YS,Tian H,Zhao DS,Hu DK,Liu XY,Jin HW,Song GP,Cui ZN

更新日期：2016-08-01 00:00:00

abstract：:Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to both the P2' and P3' side chains. Enzyme inhibition and antibacterial activity data revealed that a variety of substituents are tolerated at the P2' and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Davies SJ,Ayscough AP,Beckett RP,Clements JM,Doel S,Pratt LM,Spavold ZM,Thomas SW,Whittaker M

更新日期：2003-08-18 00:00:00

abstract：:Compounds belonging to a carbazole series have been identified as potent fungal plasma membrane proton adenosine triphophatase (H+-ATPase) inhibitors with a broad spectrum of antifungal activity. The carbazole compounds inhibit the adenosine triphosphate (ATP) hydrolysis activity of the essential fungal H+-ATPase, the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Clausen JD,Kjellerup L,Cohrt KO,Hansen JB,Dalby-Brown W,Winther AL

更新日期：2017-10-01 00:00:00

abstract：:A test series of 32 phenylpiperazines III with affinity for 5-HT1A and alpha1 receptors was subjected to QSAR analysis using artificial neural networks (ANNs), in order to get insight into the structural requirements that are responsible for 5-HT1A/alpha1 selectivity. Good models and predictive power were obtained for...

journal_title：Bioorganic & medicinal chemistry letters

authors： López-Rodríguez ML,Morcillo MJ,Fernández E,Rosado ML,Orensanz L,Beneytez ME,Manzanares J,Fuentes JA,Schaper KJ

更新日期：1999-06-21 00:00:00

abstract：:A series of 4-substituted (benzo[b]thiophene-2-carbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardioprotective efficacy both in vitro and in vivo. Several analogs exhibited a strong inhibition on NHE-1, and which was generally well correlated with their cardioprotective efficac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee S,Lee H,Yi KY,Lee BH,Yoo SE,Lee K,Cho NS

更新日期：2005-06-15 00:00:00

abstract：:The structure-activity relationships for semicarbazide-sensitive amine oxidase (SSAO) inhibitors based on arylpropynylamines was investigated using solution-phase combinatorial Sonogashira coupling. The results suggest that binding to the active site occurs by coordination of the amine to the proximal copper(II) and f...

journal_title：Bioorganic & medicinal chemistry letters

authors： Conn C,Shimmon R,Cordaro F,Hargraves TL,Ibrahim P

更新日期：2001-10-08 00:00:00

abstract：:Breast cancer is the most common malignancy among females, and cancer invasion and metastasis are the leading causes of cancer death in breast cancer patients. Pterostilbene, a naturally occurring dimethylether analogue of resveratrol, has been demonstrated to possess anti-cancer effects. However, inhibitory effects o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ko HS,Kim JS,Cho SM,Lee HJ,Ahn KS,Kim SH,Lee EO

更新日期：2014-02-15 00:00:00

abstract：:A novel series of hepatitis C virus (HCV) NS3/4A protease inhibitors bearing a P2-P4 macrocycle and a P1-P1' alpha-ketoamide serine trap is reported. The NS3 protease, which is essential for viral replication, is considered one of the most attractive targets for developing novel anti-HCV therapies. The optimization of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Avolio S,Robertson K,Hernando JI,DiMuzio J,Summa V

更新日期：2009-04-15 00:00:00

abstract：:An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent inhibitor endowed with poor drug properties, conformational constraint of the P(2)-P(3) linker and modifications to P(1') elements led to an enhancement in potency, s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barrett DG,Boncek VM,Catalano JG,Deaton DN,Hassell AM,Jurgensen CH,Long ST,McFadyen RB,Miller AB,Miller LR,Payne JA,Ray JA,Samano V,Shewchuk LM,Tavares FX,Wells-Knecht KJ,Willard DH Jr,Wright LL,Zhou HQ

更新日期：2005-08-01 00:00:00

abstract：:We aimed to discover a novel type of transient receptor potential vanilloid 1 (TRPV1) antagonist because such antagonists are possible drug candidates for treating various disorders. We modified the structure of hit compound 7 (human TRPV1 IC50=411 nM) and converted its pyrrolidino group to a (hydroxyethyl)methylamino...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takahashi E,Hirano N,Nagahara T,Yoshikawa S,Momen S,Yokokawa H,Hayashi R

更新日期：2013-06-01 00:00:00

abstract：:3,6-Ketals of 15-membered azalide pseudoaglycones are a novel series of macrolide antibiotics. The aromatic derivatives of the azalide 3,6-ketals demonstrated potent antibacterial activities against both Gram-positive and Gram-negative bacteria. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cheng H,Dirlam JP,Ziegler CB,Lundy KM,Hayashi SF,Kamicker BJ,Dutra JK,Daniel KL,Santoro SL,George DM,Bertsche CD,Sakya SM,Suarez-Contreras M

更新日期：2002-09-02 00:00:00

abstract：:Positive allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) is regarded as a potential novel treatment for schizophrenic patients. Herein we report the synthesis and SAR of 4-aryl piperazine and piperidine amides as potent mGluR5 positive allosteric modulators (PAMs). Several analogs have excellent ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiong H,Brugel TA,Balestra M,Brown DG,Brush KA,Hightower C,Hinkley L,Hoesch V,Kang J,Koether GM,McCauley JP Jr,McLaren FM,Panko LM,Simpson TR,Smith RW,Woods JM,Brockel B,Chhajlani V,Gadient RA,Spear N,Sygowski LA

更新日期：2010-12-15 00:00:00

abstract：:A new immobilization chemistry for covalent attachment of phosphorylated oligonucleotides on epoxy-activated glass surface via opening of oxirane ring is described. The proposed strategy results in excellent immobilization efficiency, spot homogeneity, and morphology. The constructed microarray was successfully demons...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mahajan S,Kumar P,Gupta KC

更新日期：2006-11-01 00:00:00

abstract：:The design and synthesis of macrocyclic inhibitors of human rhinovirus 3C protease is described. A macrocyclic linkage of the P1 and P3 residues, and the subsequent structure-based optimization of the macrocycle conformation and size led to the identification of a potent biochemical inhibitor 10 with sub-micromolar an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Namoto K,Sirockin F,Sellner H,Wiesmann C,Villard F,Moreau RJ,Valeur E,Paulding SC,Schleeger S,Schipp K,Loup J,Andrews L,Swale R,Robinson M,Farady CJ

更新日期：2018-03-01 00:00:00

abstract：:Novel approaches that do not rely upon developing microbicidal compounds are sorely needed to combat multidrug resistant (MDR) bacteria. The potential of marine secondary metabolites to serve as a source of non-traditional anti-bacterial agents is demonstrated by showing that pyrrole-imidazole alkaloids inhibit biofil...

journal_title：Bioorganic & medicinal chemistry letters

authors： Melander RJ,Liu HB,Stephens MD,Bewley CA,Melander C

更新日期：2016-12-15 00:00:00

abstract：:A novel series of prodrugs containing dabigatran and methyl (E)-3-(4-hydroxy-2-methoxyphenyl)propenoate (methyl ferulate) were synthesized. All of them reveal the effect of thrombin-induced anti-platelet aggregation in vitro. In addition, in vivo experiment shows that one of the target compounds, X-2 (ED50=3.7 ± 1.0 μ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang XZ,Diao XJ,Yang WH,Li F,He GW,Gong GQ,Xu YG

更新日期：2013-04-01 00:00:00