Novel cytokine release inhibitors. Part II: Steroids.

abstract：:New inhibitors have been designed for cdc2 kinase based on a multiple pseudosubstrate structure. The new inhibitors have three different structural components: 3,4-bis(indol-3-yl)maleimide, Ac-Cys-(Ser)-Pro-Lys-Lys-NHMe, and ethyloxy group between the two components. Inhibitory activities toward cdc2 and other protein...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sasaki S,Hashimoto T,Obana N,Yasuda H,Uehara Y,Maeda M

更新日期：1998-05-05 00:00:00

abstract：:Dihydroquinolines have been synthesized and have been shown to be potent n-NOS inhibitors. Selectivity versus e-NOS was increased to approximately 100-fold through appropriate substitution at the benzene ring. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jaroch S,Hölscher P,Rehwinkel H,Sülzle D,Burton G,Hillmann M,McDonald FM

更新日期：2002-09-16 00:00:00

abstract：:Bromofluoroacetophenone derivatives which produce fluorine substituted phenyl radicals that cleave DNA upon excitation were investigated as a novel photonuclease. Pyrrolecarboxamide-conjugated bromofluoroacetophenones; 4'-bromo-2'-fluoroacetophenone and 2'-bromo-4'-fluoroacetophenone were synthesized and their DNA cle...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wender PA,Jeon R

更新日期：2003-05-19 00:00:00

abstract：:Analogues of the benzazepine dopamine D1 receptor antagonist SCH-23390 incorporating the cyclo-pentadienyltricarbonyl-rhenium (CPTR) moiety were synthesized and evaluated pharmacologically. The CPTR derivatives retained affinity (0.3-2.9 nM) and D1 selectivity of the parent compound, supporting their use as neuropharm...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamagnan G,Baldwin RM,Kula NS,Baldessarini RJ,Innis RB

更新日期：2000-05-15 00:00:00

abstract：:A novel method to generate RNA binding D-peptide has been developed. To achieve the screening method, phage display was applied to "Mirrored" RNA (L-enantiomer of RNA). We have selected pre-miR21 as an initial screening target to demonstrate the method. The mirrored pre-miR-21 binding peptide sequences were successful...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sakamoto K,Otake K,Umemoto T

更新日期：2017-02-15 00:00:00

abstract：:Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists. Benzimidazole and indazolone derivatives prepared retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fletcher SR,McIver E,Lewis S,Burkamp F,Leech C,Mason G,Boyce S,Morrison D,Richards G,Sutton K,Jones AB

更新日期：2006-06-01 00:00:00

abstract：:Incorporation of a 4-hydroxy-N-acetylprolinol nucleotide analogue at the 3'-terminus of DNA or 2-5A-DNA sequences resulted in a significantly enhanced 3'-exonuclease resistance while the affinity for complementary RNA was only slightly decreased. Furthermore, the binding to and activation of human RNase L by thus modi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Verheijen JC,van Roon AM,Meeuwenoord NJ,Stuivenberg HR,Bayly SF,Chen L,van der Marel GA,Torrence PF,van Boom JH

更新日期：2000-04-17 00:00:00

abstract：:The Gram-negative bacterium Acinetobacter baumannii is an opportunistic pathogen in humans and infections are poorly treated by current therapy. Recent emergence of multi-drug resistant strains and the lack of new antibiotics demand an immediate action for development of new anti-Acinetobacter agents. To this end, oxi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rubin H,Selwood T,Yano T,Weaver DG,Loughran HM,Costanzo MJ,Scott RW,Wrobel JE,Freeman KB,Reitz AB

更新日期：2015-01-15 00:00:00

abstract：:A three-step protocol for SAR development was introduced and applied to the SAR studies of the MK2 inhibitor program. Following this protocol, key conformational features and functional groups for improving MK2 inhibitor activity were quickly identified. Through this effort, the initial gap observed between in vitro b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang X,Zhu X,Chen X,Zhou W,Xiao D,Degrado S,Aslanian R,Fossetta J,Lundell D,Tian F,Trivedi P,Palani A

更新日期：2012-01-01 00:00:00

abstract：:A new 'naked-eye' quinoline-based 'reactive' ratiometric fluorescent probe was prepared. The reactive stoichiometry of the probe with Hg²⁺ ion was 2:1. The probe exhibited high selectivity towards Hg²⁺ ion to other metal ions with a 410-fold increase in absorbance intensity ratio (A₄₀₂/A₃₄₀) in aqueous solution over a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Y,Yan Y,Chen S,Gao Z,Xu H

更新日期：2014-12-01 00:00:00

abstract：:A series of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones were synthesized and evaluated for their in vitro anti-filarial activity. To pre-assess the anti-filarial behavior of synthesized compounds (V(a-f)) on a structural basis, automated docking studies were carried out with Molecular Design Sui...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chhajed SS,Manisha P,Bastikar VA,Animeshchandra H,Ingle VN,Upasani CD,Wazalwar SS

更新日期：2010-06-15 00:00:00

abstract：:In the present communication we prepared a series of six 4-hydroxycoumarin derivatives, isosters of quercetin, recognized as an antioxidant natural compound, with the aim of evaluating the antitrypanosomal activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, and the antioxidant properties. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pérez-Cruz F,Serra S,Delogu G,Lapier M,Maya JD,Olea-Azar C,Santana L,Uriarte E

更新日期：2012-09-01 00:00:00

abstract：:Extensive SAR studies and optimization of ADME properties of benzimidazol-2-one derivatives led to the identification of BMS-433771 (3) as an orally active RSV fusion inhibitor. In order to extend the structure-activity relationships for this compound series, substitution of the benzimidazole ring was examined with a ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang XA,Cianci CW,Yu KL,Combrink KD,Thuring JW,Zhang Y,Civiello RL,Kadow KF,Roach J,Li Z,Langley DR,Krystal M,Meanwell NA

更新日期：2007-08-15 00:00:00

abstract：:During the course of our efforts toward the discovery of human histamine H4 antagonists from a series of 2-aminiopyrimidines, it was noted that a 6-trifluoromethyl group dramatically reduced affinity of the series toward the histamine H4 receptor. This observation was further investigated by synthesizing a series of l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Savall BM,Meduna SP,Venable J,Wei J,Smith RC,Hack MD,Thurmond RL,McGovern P,Edwards JP

更新日期：2014-12-01 00:00:00

abstract：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), also known as Apo2L, has been investigated in the past decade for its promising anticancer activity due to its ability to selectively induce apoptosis in tumoral cells by binding to TRAIL receptors (TRAIL-R). Macromolecules such as agonistic monoclonal a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ion GND,Nitulescu GM,Popescu CI

更新日期：2019-09-15 00:00:00

abstract：:Stable nitroxides are potential antioxidant drugs. In this study, we have linked nitroxide to natural amino acids with the aim to improve therapeutic activity. The radical scavenging activities of two nitronyl nitroxide-amino acid conjugates (NNR and NNK) were evaluated in PC 12 cell survival assays. The NO scavenging...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bi W,Cai J,Xue P,Zhang Y,Liu S,Gao X,Li M,Wang Z,Baudy-Floc'h M,Green SA,Bi L

更新日期：2008-03-15 00:00:00

abstract：:Cannabinoid CB2 PET tracers are considered as a promising alternative to PBR/TSPO tracers for the in-vivo imaging of neuroinflammation. We describe here the synthesis and characterization of compound 3, a new potent and brain penetrating CB2 ligand based on an original triazine template. The PET tracer [(18)F]-dideute...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hortala L,Arnaud J,Roux P,Oustric D,Boulu L,Oury-Donat F,Avenet P,Rooney T,Alagille D,Barret O,Tamagnan G,Barth F

更新日期：2014-01-01 00:00:00

abstract：:A single-step sensing system was developed to visually detect ligands of a cleavase-like RNA aptazyme at room temperature using aptazyme-tethered gold nanoparticles, the electrosteric stability of which was adjusted by increasing their diameter. In this system, the ligand induces self-cleavage of the aptazyme on gold ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogawa A

更新日期：2011-01-01 00:00:00

abstract：:Ceramides are the major lipid components of the stratum corneum, the major permeability barrier of the skin. Here we report a chemical synthesis of ceramide analogs covalently bonded on the silica particles, that can be used to predict the skin permeability of chemicals via HPLC methods. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yin J,Liu H,Pidgeon C

更新日期：1998-01-20 00:00:00

abstract：:Sulfonamide linker-based inhibitors with extended linear structure were designed and synthesized with the aim of producing multifunctional agents against several processes involved in the pathology of Alzheimer's disease (AD). The potency of the compounds were assessed in the inhibition of Aβ self-assembly (fibril and...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bag S,Tulsan R,Sood A,Cho H,Redjeb H,Zhou W,LeVine H 3rd,Török B,Török M

更新日期：2015-02-01 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 inhibition of the newly discovered cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme XIII of murine origin (mCA XIII) has been investigated with a series of anions, such as the physiological ones (bicarbonate, chloride), or the metal complexing anions (cyanate, cyanide, azide, hydrogen sulfide, etc), nitrate, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Innocenti A,Lehtonen JM,Parkkila S,Scozzafava A,Supuran CT

更新日期：2004-11-01 00:00:00

abstract：:We report the first biological evaluation the 1,2,3-thiaselenazole class of compound and utilising a concise synthetic approach of sulfur extrusion, selenium insertion of the 1,2,3-dithiazoles. We created a small diverse library of compounds to contrast the two ring systems. This approach has highlighted new structure...

journal_title：Bioorganic & medicinal chemistry letters

authors： Asquith CRM,Meili T,Laitinen T,Baranovsky IV,Konstantinova LS,Poso A,Rakitin OA,Hofmann-Lehmann R

更新日期：2019-07-15 00:00:00

abstract：:The synthesis and biological activity of novel glycoprotein IIb-IlIa anatagonists containing 3-azaspiro[5.5]undec-9-yl nucleus are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of the monoazaspirocyclic structure as central template for nonpeptide RGD mim...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pandey A,Seroogy J,Volkots D,Smyth MS,Rose J,Mehrotra MM,Heath J,Ruhter G,Schotten T,Scarborough RM

更新日期：2001-05-21 00:00:00

abstract：:Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight (M(W): 335-391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ries UJ,Priepke HW,Hauel NH,Haaksma EE,Stassen JM,Wienen W,Nar H

更新日期：2003-07-21 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：:A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC(50) values in the range of 10-150 nM and selectivity over the L-type channels up to nearly...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pajouhesh H,Feng ZP,Ding Y,Zhang L,Pajouhesh H,Morrison JL,Belardetti F,Tringham E,Simonson E,Vanderah TW,Porreca F,Zamponi GW,Mitscher LA,Snutch TP

更新日期：2010-02-15 00:00:00

abstract：:High throughput screening identified a phenoxyacetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a compound with functional potency for inhibition of human eosinophil shape change and oral bioavailability in the rat. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sandham DA,Aldcroft C,Baettig U,Barker L,Beer D,Bhalay G,Brown Z,Dubois G,Budd D,Bidlake L,Campbell E,Cox B,Everatt B,Harrison D,Leblanc CJ,Manini J,Profit R,Stringer R,Thompson KS,Turner KL,Tweed MF,Walker C,

更新日期：2007-08-01 00:00:00

abstract：:A set of 31 DNA minor groove binders (MGBs) with diverse structural features relating to both physical chemical properties and DNA binding sequence preference has been evaluated as potential drugs to treat Plasmodium falciparum infections using a chloroquine sensitive strain (3D7) and a chloroquine resistant strain (D...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scott FJ,Khalaf AI,Duffy S,Avery VM,Suckling CJ

更新日期：2016-07-15 00:00:00

abstract：:Using iron(III)porphyrins in combination with (diacetoxyiodo)benzene allows for the conversion of 2,9-bis(bromomethyl)-4,7-diphenyl-1,10-phenanthroline into 4,7-diphenyl-1,10-phenanthroline-2,9-dicarboxylic acid. This method provides a cost-effective and environmentally-friendly oxidation procedure using less toxic Ph...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhong QD,Xue YZ,Yan H,Song XQ,Zhong RG

更新日期：2010-09-15 00:00:00