Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.

abstract：:A series of 5-aminomethylquinoxaline-2,3-diones have been identified as potent and selective AMPA antagonists. Some of these compounds are also active at the glycine-binding site of the NMDA receptors. A number of these novel, water-soluble quinoxaline-2,3-dione derivatives display protective effects in the electrosho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Auberson YP,Bischoff S,Moretti R,Schmutz M,Veenstra SJ

更新日期：1998-01-06 00:00:00

abstract：:In previous study, a series of benzamides was identified as potent antipsychotic agents. As a continuation of the program to discover novel antipsychotics, herein we reported the evaluation of a series of pyridinecarboxamide derivatives. The most promising compound 7h not only held good activities on dopamine D2, sero...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu M,Wang Y,Yang F,Wu C,Wang Z,Ye B,Jiang X,Zhao Q,Li J,Liu Y,Zhang J,Tian G,He Y,Shen J,Jiang H

更新日期：2018-02-15 00:00:00

abstract：:Cytotoxicity and inhibition on human DNA topoisomerase I (TOP1) and II (TOP2) of 74 plant-originated triterpenoids and triterpenoid glycosides were investigated. The cytotoxic compounds are primarily polyhydroxylated oleananes (GI(50) of A549: 1.0-10.19 microM). Sixteen cytotoxic aesculiosides isolated from Aesculus p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang P,Ownby S,Zhang Z,Yuan W,Li S

更新日期：2010-05-01 00:00:00

abstract：:Novel Leu-enkephalin (Leu-Enk) (1) analogs possessing various types of alpha-substituted serine instead of its glycine residue in the position 2 were synthesized via an efficient O,N-migration method. The binding characteristics of the synthetic analogs using Chinese hamster ovary (CHO) cells expressed cloned rat mu-,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Horikawa M,Shigeri Y,Yumoto N,Yoshikawa S,Nakajima T,Ohfune Y

更新日期：1998-08-04 00:00:00

abstract：:Silybin is the major flavonolignan of silymarin and it displays a plethora of biological effects, generally ascribed to its antioxidant properties. Herein we shall describe an efficient synthetic strategy to obtain a variety of new and more water-soluble silybin and 2,3-dehydrosilybin (DHS) derivatives in which the 23...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zarrelli A,Sgambato A,Petito V,De Napoli L,Previtera L,Di Fabio G

更新日期：2011-08-01 00:00:00

abstract：:The syntheses and biological profiles of sulfoximine-based Vioxx analogs 2 are described. Interesting data have been obtained for 2a, which shows a selective COX-2 inhibition (albeit not as strong as Vioxx itself) exhibiting reduced hERG activity compare to the parent sulfone Vioxx (1). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park SJ,Buschmann H,Bolm C

更新日期：2011-08-15 00:00:00

abstract：:A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic phenylimidazole compounds. Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang C,Corte JR,Rossi KA,Bozarth JM,Wu Y,Sheriff S,Myers JE Jr,Luettgen JM,Seiffert DA,Wexler RR,Quan ML

更新日期：2017-09-01 00:00:00

abstract：:N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound 27, which subsequently impacted KG-1 tumor growth in a mouse model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barberis C,Erdman P,Czekaj M,Fire L,Pribish J,Tserlin E,Maniar S,Batchelor JD,Liu J,Patel VF,Hebert A,Levit M,Wang A,Sun F,Huang SA

更新日期：2020-12-01 00:00:00

abstract：:Certain gamma-aryloxymethyl-alpha-methylene-gamma-phenyl- gamma-butyrolactones were synthesized and evaluated for their anticancer activity. These compounds demonstrated a strong growth inhibitory activity against leukemia cell lines but are relatively inactive against non-small cell lung cancers and CNS cancers. The ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang TC,Lee KH,Chen YL,Liou SS,Tzeng CC

更新日期：1998-10-06 00:00:00

abstract：:We report a rapid method for profiling of kinases using a strategy that couples the merits of combinatorics (in rapid diversity generation) with the throughput attainable using microarrays (in parallel screening). Alanine-scanning, deletion and positional-scanning peptide libraries of a kinase substrate were synthesiz...

journal_title：Bioorganic & medicinal chemistry letters

authors： Uttamchandani M,Chan EW,Chen GY,Yao SQ

更新日期：2003-09-15 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 deficiency in pancreatic beta-cells. Since their discovery, three subtypes of peroxisome proliferator activated receptors have been identified, namely PPARalpha, PPARgamma and P...

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：2009-05-15 00:00:00

abstract：:Mannose-6-phosphate (M6P)-containing N-linked glycans are essential signaling molecules for sorting hydrolases in eukaryotic cells. Their receptors, especially the cation-independent M6P receptors (CI-MPRs), have emerged as promising protein targets for targeted drug delivery for the treatment of lysosomal storage dis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu Y,Marshall J,Li Q,Edwards N,Chen G

更新日期：2013-04-15 00:00:00

abstract：:The syntheses and anti-tuberculosis activity of quinolone-cephalosporin conjugates (1 and 2) are described. Both showed broad-spectrum antibacterial activity and significant anti-TB activity. The carbamate-linked quinolone-cephem 2 showed better antimycobacterial activity, including anti-TB activity, than the direct a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao G,Miller MJ,Franzblau S,Wan B,Möllmann U

更新日期：2006-11-01 00:00:00

abstract：:The use of chitosan as the wall of microcapsule designed for delivery of encapsulated celecoxib is reported. Microcapsules were characterised with respect to size and encapsulation efficiency of celecoxib. In vivo animals demonstrated that both free celecoxib administration and chitosan/celecoxib microcapsules adminis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cheng SY,Yuen MC,Lam PL,Gambari R,Wong RS,Cheng GY,Lai PB,Tong SW,Chan KW,Lau FY,Kok SH,Lam KH,Chui CH

更新日期：2010-07-15 00:00:00

abstract：:Two thermostable α-carbonic anhydrases (α-CAs) isolated from thermophilic Sulfurihydrogenibium spp., namely SspCA (from S. yellowstonensis) and SazCA (from S. azorense), were shown in a previous work to possess interesting complementary properties. SspCA was shown to have an exceptional thermal stability, whereas SazC...

journal_title：Bioorganic & medicinal chemistry letters

authors： De Simone G,Monti SM,Alterio V,Buonanno M,De Luca V,Rossi M,Carginale V,Supuran CT,Capasso C,Di Fiore A

更新日期：2015-05-01 00:00:00

abstract：:Isodesmosine and desmosine are crosslinking amino acids that are present only in elastin. They are useful biomarkers for the degradation of elastin, which occurs during the progression of chronic obstructive pulmonary disease (COPD) and related diseases. This Letter describes the synthesis of [(13)C3,(15)N1]-labeled i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tanigawa T,Komatsu A,Usuki T

更新日期：2015-01-01 00:00:00

abstract：:A series of N-(1-methyl-1H-indol-3-yl)methyleneamines and eight new 3,3-diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized and screened for their antileishmanial activity against Leishmania major. 3,3-Diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized by the Staudinger's ketene-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh GS,Al-Kahraman YM,Mpadi D,Yasinzai M

更新日期：2012-09-01 00:00:00

abstract：:With an insight that ligands possessing a N2S2 tetradentate array of donor atoms serve as ideal bifunctional chelating agents (BFCA) in the radiolabeling of target-specific agents, 5-hydroxy-3,7-diazanonan-1,9-dithiol (DAHPES) with a derivatizable substituent in the form of a hydroxyl group in the backbone was synthes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Das T,Banerjee S,Samuel G,Bapat K,Subramanian S,Pillai MR,Venkatesh M

更新日期：2006-11-15 00:00:00

abstract：:Novel quinolone-macrocycle conjugates displayed submicromolar antibacterial activity against Escherichia coli and Staphylococcus aureus bacterial strains. An analogous open-chain structure was not active at 100 microM against the same pathogenic strains. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jefferson EA,Swayze EE,Osgood SA,Miyaji A,Risen LM,Blyn LB

更新日期：2003-05-19 00:00:00

abstract：:Piperazinyl benzamidines were prepared and found to bind to the rat delta (delta) opioid receptor. The most active compounds had a N,N-diethylcarboxamido group and a N-benzyl piperazine. The most potent among these was N,N-diethyl-4-[4-(phenylmethyl)-1-piperazinyl][2-(trifluoromethyl)phenyl]iminomethyl]benzamide (27) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nortey SO,Baxter EW,Codd EE,Zhang SP,Reitz AB

更新日期：2001-07-09 00:00:00

abstract：:Myelin is a lipid multilayer involved in the rate of nerve transmission, and its loss is a pathological feature of multiple sclerosis in brains. Since in vivo imaging of myelin may be useful for drug development, early diagnosis, and monitoring the disease stage, we designed, synthesized, and evaluated eight novel rad...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watanabe H,Sakai S,Iikuni S,Shimizu Y,Shirakawa H,Kaneko S,Ono M

更新日期：2020-12-15 00:00:00

abstract：:Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2' p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cumming JN,Le TX,Babu S,Carroll C,Chen X,Favreau L,Gaspari P,Guo T,Hobbs DW,Huang Y,Iserloh U,Kennedy ME,Kuvelkar R,Li G,Lowrie J,McHugh NA,Ozgur L,Pan J,Parker EM,Saionz K,Stamford AW,Strickland C,Tadesse D,

更新日期：2008-06-01 00:00:00

abstract：:Pyrimido-oxazepine based sub-micromolar inhibitors (2-4) for Aurora and FLT-3 were designed and synthesized. These preliminary results supported the potential use of pyrimido-oxazepines as a versatile template for developing specific kinase inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pan W,Liu H,Xu YJ,Chen X,Kim KH,Milligan DL,Columbus J,Hadari YR,Kussie P,Wong WC,Labelle M

更新日期：2005-12-15 00:00:00

abstract：:A novel class of benzocinnolinones analogs of irdabisant were designed and synthesized as histamine H3R antagonists/inverse agonists. Modifications to the pyridazinone portion of the core and linker led to the identification of molecules with excellent target potency and selectivity with improved rat pharmacokinetic p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Josef KA,Aimone LD,Lyons J,Raddatz R,Hudkins RL

更新日期：2012-06-15 00:00:00

abstract：:Coibamide A is a highly potent antiproliferative cyclic depsipeptide, which was originally isolated from a Panamanian marine cyanobacterium. In this study, the synthesis of coibamide A has been investigated using Fmoc-based solid-phase peptide synthesis followed by the cleavage of the resulting linear peptide from the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nabika R,Suyama TL,Hau AM,Misu R,Ohno H,Ishmael JE,McPhail KL,Oishi S,Fujii N

更新日期：2015-01-15 00:00:00

abstract：:Gram positive (Bacillus cereus, B. subtilis), Gram negative (Pseudomonas aeruginosa, Escherichia coli) bacteria, and Candida albicans as a representative of fungi were used for screening the in vitro antimicrobial activity of diarylamines in the 2,3,5-trimethylbenzo[b]thiophene series bearing different substituents, s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ferreira IC,Calhelha RC,Estevinho LM,Queiroz MJ

更新日期：2004-12-06 00:00:00

abstract：:To improve the DNA hydrolytic activity of the zinc finger nuclease, we have created a new artificial zinc finger nuclease (ZWH4) by connecting two distinct zinc finger domains possessing different types of Zn(II) binding sites (Cys(2)His(2)- and His(4)-types). The overall fold of ZWH4 is similar to that of the wild-ty...

journal_title：Bioorganic & medicinal chemistry letters

authors： Negi S,Umeda Y,Masuyama S,Kano K,Sugiura Y

更新日期：2009-05-15 00:00:00

abstract：:We synthesized pyrrolomorphinan derivatives 6, 7, and 9 to examine whether the pyrrole ring would be an accessory site in the kappa opioid receptor selective antagonist, nor-binaltorphimine. Derivative 6 had an alpha,beta-unsaturated ketone substituent that strongly bound to the kappa receptor. The compound with the h...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujii H,Ida Y,Hanamura S,Osa Y,Nemoto T,Nakajima M,Hasebe K,Nakao K,Mochizuki H,Nagase H

更新日期：2010-09-01 00:00:00

abstract：:In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinities aimed at producing compounds with good pharmacokinetics proper...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pippel M,Boyce K,Venkatesan H,Phuong VK,Yan W,Barrett TD,Lagaud G,Li L,Morton MF,Prendergast C,Wu X,Shankley NP,Rabinowitz MH

更新日期：2009-11-15 00:00:00

abstract：:The synthesis of a lead anti-viral cyclopropyl carboxy acyl hydrazone 4F17 (5) and three sequential arrays of structural analogues along with the initial assessment and optimization of the antiviral pharmacophore against the herpes simplex virus type 1 (HSV-1) are reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： McNulty J,Babu Dokuburra C,D'Aiuto L,Demers M,McClain L,Piazza P,Williamson K,Zheng W,Nimgaonkar VL

更新日期：2020-12-15 00:00:00