Showing papers in "Bioorganic & Medicinal Chemistry in 2009"

TL;DR: The historical use of natural products in agricultural practices, the impact ofnatural products on the development of new pesticides, and the future prospects for natural products-based pest management are reviewed.

TL;DR: The evaluation of targeted nanoparticles in the treatment of cancers and diseases of the central nervous system, such as glioblastoma multiforme, neurovascular disorders, and neurodegenerative diseases, is discussed.

TL;DR: Diamide insecticides have emerged as one of the most promising new classes of insecticide chemistry owing to their excellent insecticidal efficacy and high margins of mammalian safety.

TL;DR: Recent advances in antimalarial drug discovery from natural sources are presented, including plant extracts, and compounds isolated from plants, bacteria, fungi and marine organisms, which offer new and novel scaffolds for development as antimalarials.

TL;DR: It could be suggested that phlorotaninns from this genus would be more potential candidates for the development of unique natural antioxidants for further industrial applications as functional foods, cosmetics and pharmaceuticals.

TL;DR: The results suggest that the five-carbon linker-containing analogues of curcumin may be favorable for theCurcumin-based drug development both pharmacokinetically and pharmacologically.

TL;DR: An attempt is made to understand Azadirachtin's failure to capture a larger market, 40 years after its discovery.

TL;DR: A chronicle of the important events that facilitated the rapid clinical development of this exciting molecule salinosporamide A (NPI-0052) into human clinical trials is offered.

TL;DR: An extensive structure-relationship study was performed and revealed that several chalcones and aurones possess an appealing pharmacological profile combining high antioxidant and lipid peroxidation activity with potent soybean LOX inhibition.

TL;DR: It is concluded that the isatin-linked benzothiazole analog can serve as a prototype molecule for further development of a new class of anti-breast cancer agents.

TL;DR: The structure-activity relationship (SAR) and in silico drug relevant properties (HBD, HBA, PSA, cLogP, molecular weight, E(HOMO) and E(LUMO)) further confirmed that the compounds are potential lead compounds for future drug discovery study.

TL;DR: Some antioxidant phenol derivatives investigated here showed effective hCA II inhibitory effects, in the same range as the clinically used sulfonamide acetazolamide, and might be used as leads for generating enzyme inhibitors possibly targeting other CA isoforms which have not been yet assayed for their interactions with such agents.

TL;DR: The synthesis of two groups of structure hybrids comprising basically the antipyrine moiety attached to either polysubstituted thiazole or 2,5-disubstituting-1,3,4-thiadiazole counterparts through various linkages is described, and compound 10 could be identified as the most biologically active member within this study with an interesting dual anti-inflammatory analgesic and antibacterial profile.

TL;DR: This work focuses on well established DNA sequences and determines the topologies and stabilities of the corresponding RNA sequences by CD spectroscopy and CD thermal melting experiments, finding that the RNA sequences exclusively fold into the all-parallel conformation in contrast to the diverse topologies adopted by DNA quadruplexes.

TL;DR: A highly atom economic one pot synthesis of tetrahydropyridines was achieved by L-proline/TFA catalysed multicomponent reaction of beta-keto-esters, aromatic aldehydes and anilines.

TL;DR: A review, outlining the origins and subsequent development of the triketone class of herbicidal 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitors.

TL;DR: The results obtained indicate that quercetin zinc(II) complex can intercalate into the stacked base pairs of DNA, and compete with the strong intercalator ethidium bromide for the intercalative binding sites with Stern-Volmer quenching constant.

TL;DR: The design, synthesis and pharmacological evaluation of novel 3-arylamine-imidazo[1,2-a]pyridine derivatives structurally designed as novel symbiotic prototypes presenting analgesic and anti-inflammatory properties are described.

TL;DR: Treatment of type 2 diabetes especially in the early stages of the disease via DPP-4 inhibition has been recognized as a validated principle and a large number of inhibitors are presently in various stage of pre-clinical/clinical development.

TL;DR: Several cases have also recently emerged where deglycosylation of an enzyme results in significantly increased catalytic activity, binding affinity and altered substrate specificity, highlighting the very unique and diverse roles that individual N-glycans play in regulating enzyme function.

TL;DR: The alpha-methyl chalcone SD400 is a potent inhibitor of tubulin assembly and possesses potent anticancer activity and remarkable cell shape changes were elicit in HUVEC cells, consistent with vasculature damaging activity.

TL;DR: Five flavonols were isolated from Rhodiola rosea, and compared with commercially available flavonoids to facilitate analysis of their structure-activity relationship (SAR), and gossypetin exhibited the most potent inhibitory activity, with IC(50) values of 0.8 to 56.9 microM.

TL;DR: The synthesis and characterization of new compounds derived from benzothiazoles and thiadiazoles showed an interesting antioxidant property and some of these compounds could be good radioprotectors.

TL;DR: The results indicate that the cytotoxic lupane-type glycosides 10 and 22 bearing an alpha-l-rhamnopyranose moiety at the C-3 position represent promising antitumour agents for further studies on tumour-bearing mice since they are devoid of toxicity associated with the haemolysis of red blood cells.

TL;DR: An inclusion complex of the antimalarial artemether (ATM) in hydroxypropyl-beta-cyclodextrin (HPbetaCD) showed an increase in water solubility and gave an apparent binding constant of 220 M(-1) according to the phase-solubility diagram.

TL;DR: 33 carboxylic acid derivatives were tested and caffeic acid derivatives such as chlorogenic acid and curcumin were found to be highly potent compared to sodium butyrate, which is a well-known HDAC inhibitor.

TL;DR: A series of 33 quinoline derivatives synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv exhibited a significant activity when compared with first line drugs such as ethambutol and could be a good starting point to develop new lead compounds in the fight against multi-drug resistant tuberculosis.

TL;DR: Those classes of compounds which inhibit Hsp90 by binding to the N-terminal ATP pocket are reviewed, including natural product inhibitors such as geldanamycin and radicicol and synthetic inhibitors comprised of purines, pyrazoles, isoxazoles and other scaffolds.

TL;DR: An efficient synthesis of 5,10-dihydroindeno[1,2-b]indoles (3a-t) containing substituents such as methoxy, hydroxyl, and halogen on indeno part showed effective antioxidant power.

TL;DR: Two series of novel rigid pyrazolone derivatives were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis and confirm the fundamental role of the p-chlorophenyl moiety at C4 in the antimycobacterial activity.