Showing papers in "Bioorganic & Medicinal Chemistry Letters in 2011"

TL;DR: Some synthesized coumarin triazoles displayed comparable or even better antibacterial and antifungal efficacy in comparison with reference drugs Enoxacin, Chloromycin and Fluconazole.

TL;DR: The inhibitory capacities of some phenolic compounds against three human CA isozymes and the gill carbonic anhydrase of the teleost fish Dicentrarchus labrax (European seabass) (dCA) are reported, which may lead to design novel CAIs with a diverse inhibition mechanism compared to sulfonamide/sulfamate inhibitors.

TL;DR: Among the title compounds, compound 4d showed pronounced activity against Mycobacterium tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis (INHR-TB) with minimum inhibitory concentrations (MICs) 0.78μM and 1.52 μM, respectively.

TL;DR: Starting from the oxindole 2a identified through a high-throughput screening campaign, a series of Na(V)1.7 blockers were developed, which demonstrated a 10-fold increase in target potency versus the original HTS hit and represents a promising structure for further optimization efforts.

TL;DR: Two series of five membered heterocyclic bis(1,3,4-oxadiazole) derivatives 2-a-h and 3,5-bis(substituted)pyrazoles, isoxazoles, 4(a-c) were synthesized via oxidative cyclization of some diaroylhydrazones using chloramine-T and cyclocondensation reaction with hydrazine hydrate and hydroxylamine hydrochloride.

TL;DR: A series of 3-phenylcoumarins synthesized and screened for potential antidepressant activity by tail suspension test (TST) in mice exhibited impressive antidepressant activity, measured in terms of percentage decrease in immobility duration.

TL;DR: A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design and lead optimization of this series led to the discovery of TAK-733.

TL;DR: A summary of the discovery and advancement of inhibitors of fatty acid amide hydrolase (FAAH) is presented.

TL;DR: Fourty-two thiazolyl-pyrazoline derivatives were synthesized to screen for their EGFR kinase inhibitory activity and molecular docking results indicated that compound 11 was nicely bound to the EGFR Kinase.

TL;DR: The preferential anti-tumor activity exhibited by compound 9 against PANC-1 under low oxygen and nutrient environment illustrates its great potential as a promising lead structure for the development of novel agents to combat pancreatic cancer.

TL;DR: The results of the present studying indicates 2,5-disubstituted 1,3,4-oxadiazole/thiadiazoles as promising surface recognition moiety for development of newer hydroxamic acid based histone deacetylase inhibitor.

TL;DR: Evidence of synergistic effect makes this inhibitor to have a potential possibility for control of pandemic infection by oseltamivir-resistant influenza virus.

TL;DR: The first application of a photoinduced 1,3-dipolar cycloaddition reaction to 'staple' a peptide dual inhibitor of the p53-Mdm2/Mdmx interactions showed enhanced cellular uptake along with modest in vivo activity.

TL;DR: Two compounds (2g and 2k) proved to have superior gastrointestinal safety profiles as compared to celecoxib, when tested for their ulcerogenic effects, and showed more potent anti-inflammatory activity than cele Coxib at 5h in carrageenan-induced rat paw edema bioassay.

TL;DR: The optimization of biochemical activity and other drug-like properties through substitutions to the pyrrole, piperidine, and heterocycle portions of the molecule resulted in pyrrolamides with improved cellular activity and in vivo efficacy.

TL;DR: The development of an extremely fast and efficient method for generating (18)F labeled probes based on the tetrazine-trans-cyclooctene ligation and the receptor specificity was confirmed by blocking experiments.

TL;DR: Results indicate strong associations among plasma urolithin A levels, the plasma ORAC scores, and anti-inflammatory effects and may help explain a mechanism by which ellagitannins confer protection against inflammatory diseases.

TL;DR: A series of novel covalent EGFR kinase inhibitors with selectivity for the clinically relevant T790M 'gatekeeper' resistance mutation relative to wild-type EGFR were discovered by library screening.

TL;DR: The structure-activity relationships of 5-phenoxy 3-methylfuran-2(5H)-one (3) derivatives, which possess a common substructure with SLs, are reported, which showed SL-like activity more potently than GR24, a typical SL derivative, in a rice assay.

TL;DR: Replacement of the enamine functionality of the hit series with either an imidazole or a pyrazole ring led to compounds that inhibited both capsid assembly and reverse transcriptase, leading to lead compound 48, a pure capsidAssembly inhibitor with improved antiviral activity.

TL;DR: Sodium bisulfite has been reported first time for the synthesis of 2,5-disubstituted 1,3,4-oxadiazole using microwave and conventional method in ethanol-water and some of the compounds were equipotent with miconazole against Candida albicans and Fusarium oxysporum.

TL;DR: It is revealed from the antioxidant screening results that the compounds 9c and f manifested profound antioxidant potential.

TL;DR: This is the first report assigning in vitro anti-mycobacterial, anticancer and structure-activity relationship for this new class of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates.

TL;DR: A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates synthesized using click chemistry approach exhibited inhibition of Src kinase and inhibited the cell proliferation of HT-29 and SK-Ov-3.

TL;DR: In this article, the authors describe the syntheses of various hydrazides of comarins, quinolones and pyrroles and screening against M. tuberculosis (Mtb) H37Rv by using rifampin as a standard drug.

TL;DR: A fluorescent sensor for Fe(3+) has been synthesized based on rhodamine-lactam, which shows excitation and emission wavelength, displays an excellent selectivity for Fe (3+) and can be used for imaging Fe( 3+) in living cells.

TL;DR: In vitro antitubercular activity of these triazoles was screened against Mycobacterium tuberculosis H(37)Rv strain and four of the compounds showed MIC in the range of 1.56-3.13 μg/mL proving their potential activity.

TL;DR: B Bis spiro-indoles exhibited stronger antibacterial and antifungal efficiency than their corresponding monospiro-bisindole intermediates.

TL;DR: ATQ3 may represent a broader class of unappreciated dietary-derived phytomolecular redox motifs that digitally encode biochemical data using redox state as a means to sense and transfer information essential for cellular function.

TL;DR: Results suggest that asperuloside in Eucommia leaves has important anti-obesity effects, similar to those of EGLE.