Toxocara canis: Larvicidal activity of fatty acid amides.

abstract：:A combinatorial synthesis process involving sequential cycles of cutting a membrane support into pieces and combining these into groups and subjecting the groups to simultaneous solid-phase chemical reactions is demonstrated by the rapid assembly of four hundred N-terminally biotinylated, soluble, octameric peptide po...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dittrich F,Tegge W,Frank R

更新日期：1998-09-08 00:00:00

abstract：:Two new heterocycles, pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole, were prepared in three steps from 3-aminocarbazole and 3-aminoindole, respectively. The key Friedel-Crafts intramolecular cyclization was realized under microwave irradiation using montmorillonite K-10 clay as a catalyst. The pyrimido[4,5-c]carb...

journal_title：Bioorganic & medicinal chemistry letters

authors： Debray J,Zeghida W,Baldeyrou B,Mahieu C,Lansiaux A,Demeunynck M

更新日期：2010-07-15 00:00:00

abstract：:A series of acetylenic chalcones were evaluated for antimalarial and antitubercular activity. The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy group ortho to the acetylenic group. Most compounds were more ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hans RH,Guantai EM,Lategan C,Smith PJ,Wan B,Franzblau SG,Gut J,Rosenthal PJ,Chibale K

更新日期：2010-02-01 00:00:00

abstract：:Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic beta-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARalpha, PPARgamma and PPARbeta/(d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parmenon C,Guillard J,Caignard DH,Hennuyer N,Staels B,Audinot-Bouchez V,Boutin JA,Dacquet C,Ktorza A,Viaud-Massuard MC

更新日期：2008-03-01 00:00:00

abstract：:Bacterial resistance to β-lactam antibiotics caused by class B metallo-β-lactamases (MBL), especially for certain hospital-acquired, Gram-negative pathogens, poses a significant threat to public health. We report several 2-substituted 4,5-dihydrothiazole-4-carboxylic acids to be novel MBL inhibitors. Structure activit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen P,Horton LB,Mikulski RL,Deng L,Sundriyal S,Palzkill T,Song Y

更新日期：2012-10-01 00:00:00

abstract：:The eryA gene of the bacterial pathogen Brucella abortus has been functionally expressed in Escherichia coli. The resultant EryA was shown to catalyze the ATP-dependent conversion of erythritol to L-erythritol-4-phosphate (L-E4P). The steady state kinetic parameters of this reaction were determined and the enzyme was ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lillo AM,Tetzlaff CN,Sangari FJ,Cane DE

更新日期：2003-02-24 00:00:00

abstract：:A series of 5-substitutedbenzylideneamino-2-butylbenzofuran-3-yl-4-methoxyphenyl methanones is synthesized and evaluated for antileishmanial and antioxidant activities. Compounds 4f (IC50 = 52.0 ± 0.09 µg/ml), 4h (IC50 = 56.0 ± 0.71 µg/ml) and 4l (IC50 = 59.3 ± 0.55 µg/ml) were shown significant antileishmanial when c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patil SR,Bollikonda S,Patil RH,Sangshetti JN,Bobade AS,Asrondkar A,Reddy PP,Shinde DB

更新日期：2018-02-01 00:00:00

abstract：:A series of tetrahydro-β-carboline derivatives of a lead compound known to target the heat shock 90 protein of Plasmodium falciparum were synthesized and assayed for both potency against the parasite and toxicity against a human cell line. Using a rationalized structure based design strategy, a new lead compound with ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Eagon S,Hammill JT,Bach J,Everson N,Sisley TA,Walls MJ,Durham S,Pillai DR,Falade MO,Rice AL,Kimball JJ,Lazaro H,DiBernardo C,Kiplin Guy R

更新日期：2020-11-01 00:00:00

abstract：:Novel derivatives of the D-glucosidase inhibitor 2,5-dideoxy-2,5-imino-D-mannitol bearing lipophilic aliphatic or aromatic amides attached to C-1 have been found to inhibit beta-glucosidase from Agrobacterium sp. in the nanomolar range. One of them, a coumarin derivative, ranks amongst the most active compounds in the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wrodnigg TM,Withers SG,Stütz AE

更新日期：2001-04-23 00:00:00

abstract：:A dumbbell-shaped circular oligonucleotide containing topoisomerase I-binding sites and two mismatched base pairs in its sequence has been designed and synthesized. Our further studies demonstrate that this particularly designed oligonucleotide displays an IC(50) value of 9 nM in its inhibition on the activity of huma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Tao Ng MT,Wang Y,Liu X,Li T

更新日期：2007-09-01 00:00:00

abstract：:We have synthesized and tested novel quinuclidinone analogs to assay the effects on H1299 lung cancer cell lines alone or with gamma-radiation. We have found two series of quinuclidinone analogs that act as anti-cancer agents. Of these, four interesting analogs significantly decreased cell viability in H1299 lung canc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Malki A,Pulipaka AB,Evans SC,Bergmeier SC

更新日期：2006-03-01 00:00:00

abstract：:A novel series of acylated omega-aminoalkyl 2-amino-2-deoxy-4-phosphono-beta-D-glucopyranosides (aminoalkyl glucosaminide 4-phosphates) was synthesized and screened for immunostimulant activity. Several of these compounds enhance the production of tetanus toxoid-specific antibodies in mice and augment vaccine-induced ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Johnson DA,Sowell CG,Johnson CL,Livesay MT,Keegan DS,Rhodes MJ,Ulrich JT,Ward JR,Cantrell JL,Brookshire VG

更新日期：1999-08-02 00:00:00

abstract：:We have recently reported that the elaboration of the N-substituent in the δ opioid receptor (DOR) antagonist naltrindole (NTI) enabled the regulation of the DOR activities from full inverse agonists to weak partial agonists. The investigations of amide-type NTI derivatives revealed that N-phenylacetyl and N-dihydroci...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujii H,Uchida Y,Shibasaki M,Nishida M,Yoshioka T,Kobayashi R,Honjo A,Itoh K,Yamada D,Hirayama S,Saitoh A

更新日期：2020-06-15 00:00:00

abstract：:A series of β-boswellic acid derivatives were synthesized and evaluated for anticancer activity. One of the lead analog 4f displayed significant anticancer activity against a panel of cancer cells as well as substantially inhibited colony formation in HCT-116 cells. Furthermore, 4f was found to be a potent inducer of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumar A,Qayum A,Sharma PR,Singh SK,Shah BA

更新日期：2016-01-01 00:00:00

abstract：:A novel class of 4-aryl-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1- ones have been discovered and developed as potent and selective GlyT1 inhibitors. The molecules are devoid of activity at the GlyT2 isoform and display excellent selectivities against the mu-opioid receptor as well as the Nociceptin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alberati D,Hainzl D,Jolidon S,Krafft EA,Kurt A,Maier A,Pinard E,Thomas AW,Zimmerli D

更新日期：2006-08-15 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：:GPR91, a 7TM G-Protein-Coupled Receptor, has been recently deorphanized with succinic acid as its endogenous ligand. Current literature indicates that GPR91 plays role in various pathophysiology including renal hypertension, autoimmune disease and retinal angiogenesis. Starting from a small molecule high-throughput sc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhuniya D,Umrani D,Dave B,Salunke D,Kukreja G,Gundu J,Naykodi M,Shaikh NS,Shitole P,Kurhade S,De S,Majumdar S,Reddy SB,Tambe S,Shejul Y,Chugh A,Palle VP,Mookhtiar KA,Cully D,Vacca J,Chakravarty PK,Nargund RP,W

更新日期：2011-06-15 00:00:00

abstract：:A novel class of 2,3-diaminopyridine bradykinin B1 receptor antagonists is disclosed. Structure-activity relationship studies (SARs) that led to compounds with significantly improved potency and pharmacokinetic properties relative to the lead compound are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng DM,Wai JM,Kuduk SD,Ng C,Murphy KL,Ransom RW,Reiss D,Chang RS,Harrell CM,MacNeil T,Tang C,Prueksaritanont T,Freidinger RM,Pettibone DJ,Bock MG

更新日期：2005-05-02 00:00:00

abstract：:In this communication, human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11β-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent eff...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan X,Wang Z,Sudom A,Cardozo M,DeGraffenreid M,Di Y,Fan P,He X,Jaen JC,Labelle M,Liu J,Ma J,McMinn D,Miao S,Sun D,Tang L,Tu H,Ursu S,Walker N,Ye Q,Powers JP

更新日期：2010-12-01 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

abstract：:A labeled variant of MSH(4), a tetrapeptide that binds to the human melanocortin 4 receptor (hMC4R) with low microM affinity, was prepared by solid-phase synthesis methods, purified, and characterized. The labeled ligand, Eu-DTPA-PEGO-His-dPhe-Arg-Trp-NH(2), exhibited a K(d) for hMC4R of 9.1+/-1.4 microM, approximatel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu L,Vagner J,Alleti R,Rao V,Jagadish B,Morse DL,Hruby VJ,Gillies RJ,Mash EA

更新日期：2010-04-15 00:00:00

abstract：:The methylendioxyphenyl group, present in a number of potent endothelin receptor antagonists, could have undesirable metabolic interactions with cytochrome P450 in vivo. Using a self-organizing neural network we analysed the features of molecular electrostatic potentials of several endothelin receptor ligands. A libra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anzali S,Mederski WW,Osswald M,Dorsch D

更新日期：1998-01-06 00:00:00

abstract：:A β-carbonic anhydrases (CAs, EC 4.2.1.1) was recently cloned, purified and characterized kinetically in the pathogen Clostridium perfringens. We report here the first inhibition study of this enzyme (CpeCA). CpeCA was poorly inhibited by iodide and bromide, and was inhibited with KIs in the range of 1-10mM by a range...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vullo D,Sai Kumar RS,Scozzafava A,Capasso C,Ferry JG,Supuran CT

更新日期：2013-12-15 00:00:00

abstract：:(3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (1) was recently identified as a functionally selective, inverse agonist at the benzodiazepine site of GABA(A) alpha5 receptors and enhances performance in animal models of cognition. The routes of metabolis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jones P,Atack JR,Braun MP,Cato BP,Chambers MS,O'Connor D,Cook SM,Hobbs SC,Maxey R,Szekeres HJ,Szeto N,Wafford KA,MacLeod AM

更新日期：2006-02-15 00:00:00

abstract：:Novel CCR2 antagonists with a novel 2-aminooctahydrocyclopentalene-3a-carboxamide scaffold were designed. SAR studies led to a series of potent compounds. For example, compound 51 had a good PK profile in both dog and monkey, and exhibited excellent efficacy when dosed orally in an inflammation model in hCCR2 KI mice....

journal_title：Bioorganic & medicinal chemistry letters

authors： Cai C,Kang FA,Hou C,O'Neill JC,Opas E,McKenney S,Johnson D,Sui Z

更新日期：2013-01-01 00:00:00

abstract：:The concept of sequential cytotoxicity, which states that successive chemical attacks on cellular constituents can be more deleterious to neoplasms than normal cells, was evaluated using a series of 3,5-bis(benzylidene)-1-diethylphosphono-4-oxopiperidines 1 and related phosphonic acids 2, which were screened against a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Das S,Das U,Sakagami H,Hashimoto K,Kawase M,Gorecki DK,Dimmock JR

更新日期：2010-11-15 00:00:00

abstract：:The identification of a novel pyrazolidine-3,5-dione based scaffold hit compound as Farnesoid X receptor (FXR) partial or full agonist has been accomplished by means of virtual screening techniques. A series of pyrazolidine-3,5-dione derivatives (1a-u and 7) was designed, synthesized, and evaluated by a cell-based luc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deng G,Li W,Shen J,Jiang H,Chen K,Liu H

更新日期：2008-10-15 00:00:00

abstract：:Optically active tetrahydroisoquinoline alkaloids, (R)-(+)-higenamine (1R) and (S)-(-)-higenamine (1 S), and their optically active 1-naphthylmethyl analogues (2 and 3), were synthesized by enantioselective hydrogenation of the corresponding dihydroisoquinoline intermediates 7 as a key step. The evaluation of the plat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pyo MK,Lee DH,Kim DH,Lee JH,Moon JC,Chang KC,Yun-Choi HS

更新日期：2008-07-15 00:00:00

abstract：:A series of substituted sulfonamide bioisosteres of 8-hydroxyquinoline were evaluated for their antibacterial activity against the common mastitis causative pathogens Streptococcus uberis, Staphylococcus aureus and Escherichia coli, both in the presence and absence of supplementary zinc. Compounds 9a-e, 10a-c, 11a-e, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： McGowan JE,Harper AD,Davison EK,Jeong JY,Mros S,Harbison-Price N,Van Zuylen EM,Knottenbelt MK,Heikal A,Ferguson SA,McConnell MA,Cook GM,Krittaphol W,Walker GF,Brimble MA,Rennison D

更新日期：2020-06-01 00:00:00

abstract：:A series of novel, potent and selective pyrido[1,2-a]pyrazine dopamine D4 receptor antagonists are reported including CP-293,019 (D4 Ki = 3.4 nM, D2 Ki > 3,310 nM), which also inhibits apomorphine-induced hyperlocomotion in rats after oral dosing. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sanner MA,Chappie TA,Dunaiskis AR,Fliri AF,Desai KA,Zorn SH,Jackson ER,Johnson CG,Morrone JM,Seymour PA,Majchrzak MJ,Faraci WS,Collins JL,Duignan DB,Prete Di CC,Lee JS,Trozzi A

更新日期：1998-04-07 00:00:00