Synthesis and antimicrobial activity of squalamine analogue.

abstract：:Carbonic anhydrase (CA; EC 4.2.1.1) was purified from the gill of the teleost fish Dicentrarchus labrax (European seabass). The purification procedure consisted of a single step affinity chromatography on Sepharose 4B-tyrosine-sulfanilamide. The enzyme was purified 84.9-fold with a yield of 58%, and a specific activit...

journal_title：Bioorganic & medicinal chemistry

authors： Ekinci D,Ceyhun SB,Sentürk M,Erdem D,Küfrevioğlu Oİ,Supuran CT

更新日期：2011-01-15 00:00:00

abstract：:This work investigated the in vitro and in vivo anti-angiogenic activity of some pyrroloazaflavones, exactly 2-phenyl-1H-pyrrolo[2,3-h]quinolin-4(7H)ones, with vinblastine as reference compound. Growth inhibitory activity, migration, and capillary-like structures formation were determined in human umbilical vein endot...

journal_title：Bioorganic & medicinal chemistry

authors： Ferlin MG,Conconi MT,Urbani L,Oselladore B,Guidolin D,Di Liddo R,Parnigotto PP

更新日期：2011-01-01 00:00:00

abstract：:A series of secondary face modified cyclodextrins (CDs) were synthesised with the aim of constructing host molecules capable of forming host-guest complexes with neuromuscular blockers, especially with rocuronium bromide. Perfacial 2-O-substitution of gamma-CD with 4-carboxybenzyl resulted in a CD host molecule 1 that...

journal_title：Bioorganic & medicinal chemistry

authors： Tarver GJ,Grove SJ,Buchanan K,Bom A,Cooke A,Rutherford SJ,Zhang MQ

更新日期：2002-06-01 00:00:00

abstract：:Poly(ADP-ribose) glycohydrolase (PARG) plays an essential role in poly(ADP-ribose) (PAR) turnover, and thereby regulating DNA transactions, such as DNA repair, replication, transcription and recombination. Here, we examined the inhibitory activities of 6-hydroxy-3H-xanthene-3-one (HXO) derivatives and analyzed their b...

journal_title：Bioorganic & medicinal chemistry

authors： Shibui Y,Oyama T,Okazawa M,Yoshimori A,Abe H,Uchiumi F,Tanuma SI

更新日期：2020-02-01 00:00:00

abstract：:Thirteen (Z)-4-(substituted benzylidene)-3-phenylisoxazol-5(4H)-ones were designed to confirm the geometric effect of the double bond of the β-phenyl-α, β-unsaturated carbonyl scaffold on tyrosinase inhibitory activity. Compounds 1a-1m, which all possessed the (Z)-β-phenyl-α, β-unsaturated carbonyl scaffold, were synt...

journal_title：Bioorganic & medicinal chemistry

authors： Kim SJ,Yang J,Lee S,Park C,Kang D,Akter J,Ullah S,Kim YJ,Chun P,Moon HR

更新日期：2018-08-07 00:00:00

abstract：:Various 4-(anilino)pyrrole-2-carboxamides were designed and synthesized as novel androgen receptor (AR) antagonists without steroidal or anilide structure, based on our strategy for developing full antagonists of nuclear receptors. Introduction of a bulky N-alkyl group, such as a cyclohexylmethyl or benzyl group, incr...

journal_title：Bioorganic & medicinal chemistry

authors： Wakabayashi K,Imai K,Miyachi H,Hashimoto Y,Tanatani A

更新日期：2008-07-15 00:00:00

abstract：:Novel 2-phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones (PQs) endowed with high affinity for central benzodiazepine receptor (BzR) were synthesized. In particular, 9-fluoro-2-(2-fluorophenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one (2(2)) showed binding affinity in the subnanomolar concentration range and p...

journal_title：Bioorganic & medicinal chemistry

authors： Carotti A,Altomare C,Savini L,Chiasserini L,Pellerano C,Mascia MP,Maciocco E,Busonero F,Mameli M,Biggio G,Sanna E

更新日期：2003-11-17 00:00:00

abstract：:We report the synthesis and the functional studies of multiple crown alpha-helical peptides designed to form artificial ion channels. The approach combines the versatility of solid phase peptide synthesis, the conformational predictability of peptidic molecules, and the solution synthesis of crown ethers with engineer...

journal_title：Bioorganic & medicinal chemistry

authors： Biron E,Otis F,Meillon JC,Robitaille M,Lamothe J,Van Hove P,Cormier ME,Voyer N

更新日期：2004-03-15 00:00:00

abstract：:Human enterovirus (EV) belongs to the picornavirus family, which consists of over 200 medically relevant viruses. A peptidomimetic inhibitor AG7088 was developed to inhibit the 3C protease of rhinovirus (a member of the family), a chymotrypsin-like protease required for viral replication, by forming a covalent bond wi...

journal_title：Bioorganic & medicinal chemistry

authors： Kuo CJ,Shie JJ,Fang JM,Yen GR,Hsu JT,Liu HG,Tseng SN,Chang SC,Lee CY,Shih SR,Liang PH

更新日期：2008-08-01 00:00:00

abstract：:In this work, we further investigated a previously introduced class of cholinesterase inhibitors. The removal of the carbamic function from the lead compound xanthostigmine led to a reversible cholinesterase inhibitors 3. Some new 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-one analogs were designed, synthesized, and...

journal_title：Bioorganic & medicinal chemistry

authors： Piazzi L,Belluti F,Bisi A,Gobbi S,Rizzo S,Bartolini M,Andrisano V,Recanatini M,Rampa A

更新日期：2007-01-01 00:00:00

abstract：:Cyclic D- and L-4-aminothreose were synthesised from ethyl D- and L-tartrate, respectively. D-aminothreose was a potent inhibitor of alpha-glucosidase and of alpha-mannosidase. From the glycosidase inhibition potencies of the four 4-amino-4-deoxy-tetroses, the contribution of binding of each functionality of the 5 and...

journal_title：Bioorganic & medicinal chemistry

authors： Chevrier C,Defoin A,Tarnus C

更新日期：2007-06-15 00:00:00

abstract：:A series of new N-substituted aminohydroxypyridines have been synthesized, pharmacologically evaluated and compared with their N-substituted oxazolopyridone analogs. The compound with the maximal combination of safety and analgesic efficacy was 3-[2-[4-(4-fluorophenyl)-1-piperazinyl]ethyl]amino-2-hydroxypyridine (comp...

journal_title：Bioorganic & medicinal chemistry

authors： Viaud MC,Jamoneau P,Bizot-Espiard JG,Pfeiffer B,Renard P,Caignard DH,Adam G,Guillaumet G

更新日期：1995-07-01 00:00:00

abstract：:The binding stoichiometry, binding constants, and inclusion mode of some water-soluble negatively charged cyclodextrin derivatives, i.e. heptakis-[6-deoxy-6-(3-sulfanylpropanoic acid)]-β-cyclodextrin(H1), heptakis-[6-deoxy-6-(2-sulfanylacetic acid)]-β-cyclodextrin(H2), mono-[6-deoxy-6-(3-sulfanylpropanoic acid)]-β-cyc...

journal_title：Bioorganic & medicinal chemistry

authors： Cheng JG,Yu HJ,Chen Y,Liu Y

更新日期：2018-05-15 00:00:00

abstract：:Since NSAIDs are commonly used anti-inflammatory agents that produce adverse effects, there have been ongoing efforts to develop more effective and less toxic compounds. Based on the structure of the anti-inflammatory pyrrolizines licofelone and ketorolac, a series of 1-arylpyrrolizin-3-ones was synthesized. Also prep...

journal_title：Bioorganic & medicinal chemistry

authors： Madrigal DA,Escalante CH,Gutiérrez-Rebolledo GA,Cristobal-Luna JM,Gómez-García O,Hernández-Benitez RI,Esquivel-Campos AL,Pérez-Gutiérrez S,Chamorro-Cevallos GA,Delgado F,Tamariz J

更新日期：2019-10-15 00:00:00

abstract：:The ribose moiety of adenine nucleotide 3',5'-bisphosphate antagonists of the P2Y(1) receptor has been successfully substituted with a rigid methanocarba ring system, leading to the conclusion that the North (N) ring conformation is preferred in receptor binding. Similarly, at P2Y(2) and P2Y(4) receptors, nucleotides ...

journal_title：Bioorganic & medicinal chemistry

authors： Ohno M,Costanzi S,Kim HS,Kempeneers V,Vastmans K,Herdewijn P,Maddileti S,Gao ZG,Harden TK,Jacobson KA

更新日期：2004-11-01 00:00:00

abstract：:Five series of novel 3,4,5-trisubstituted aminothiophene derivatives and analogs were designed and synthesized based on our previous studies. All target compounds were evaluated for their p53-MDM2 binding inhibitory activities and anti-proliferation activities against A549 and PC3 tumor cell lines. Twelve compounds di...

journal_title：Bioorganic & medicinal chemistry

authors： Wang W,Lv D,Qiu N,Zhang L,Hu C,Hu Y

更新日期：2013-06-01 00:00:00

abstract：:Sonodynamic therapy (SDT) involves the activation of a non-toxic sensitiser drug using low-intensity ultrasound to produce cytotoxic reactive oxygen species (ROS). Given the low tissue attenuation of ultrasound, SDT provides a significant benefit over the more established photodynamic therapy (PDT) as it enables activ...

journal_title：Bioorganic & medicinal chemistry

authors： McEwan C,Nesbitt H,Nicholas D,Kavanagh ON,McKenna K,Loan P,Jack IG,McHale AP,Callan JF

更新日期：2016-07-01 00:00:00

abstract：:A set of new muscarinic antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine (1), was synthesized and tested to evaluate their affinity and selectivity for M(1), M(2), M(3) and M(4) receptor subtypes. The conformational constraint of 1 in a bicyclic structure, and the varia...

journal_title：Bioorganic & medicinal chemistry

authors： Piergentili A,Gentili F,Ghelfi F,Marucci G,Pigini M,Quaglia W,Giannella M

更新日期：2003-09-01 00:00:00

abstract：:There is considerable interest in developing dopamine transporter (DAT) inhibitors as potential therapies for the treatment of cocaine abuse. We report herein our pharmacophore-based discovery and molecular modeling-assisted rational design of 2,3-disubstituted quinuclidines as potent DAT inhibitors with a novel chemi...

journal_title：Bioorganic & medicinal chemistry

authors： Sakamuri S,Enyedy IJ,Zaman WA,Tella SR,Kozikowski AP,Flippen-Anderson JL,Farkas T,Johnson KM,Wang S

更新日期：2003-03-20 00:00:00

abstract：:Inhibitors of transglycosylases may serve as potent antibiotics that are less prone to resistance development in bacterial pathogens. To facilitate the search of such compounds, a transglycosylase (TGase) domain of the membrane integral multidomain Streptococcus pneumoniae PBP1b was cloned and expressed. This TGase do...

journal_title：Bioorganic & medicinal chemistry

authors： Liu H,Wong CH

更新日期：2006-11-01 00:00:00

abstract：:Structurally modified phthalimide derivatives were prepared through condensation of phthalic and tetrafluorophthalic anhydride with selected sulfonamides with variable yields. All compounds were screened for their antimycobacterium activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) using a micro broth dilu...

journal_title：Bioorganic & medicinal chemistry

authors： Akgün H,Karamelekoğlu I,Berk B,Kurnaz I,Sarıbıyık G,Oktem S,Kocagöz T

更新日期：2012-07-01 00:00:00

abstract：:Protein geranylgeranylation reactions are dependent on the availability of geranylgeranyl diphosphate (GGDP), which serves as the isoprenoid donor. Inhibition of GGDP synthase (GGDPS) is of interest from a drug development perspective as GGDPS inhibition results in impaired protein geranylgeranylation, which in multip...

journal_title：Bioorganic & medicinal chemistry

authors： Wills VS,Metzger JI,Allen C,Varney ML,Wiemer DF,Holstein SA

更新日期：2017-04-15 00:00:00

abstract：:Even number fatty acid residues-docosanoyl (behenoyl) and stearoyl were selected for introduction to the N(4)-position of (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine) (HPMPC, cidofovir), and its 5-azacytosine counterpart, (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine) (HPMP-5-azaC) with the aim to prep...

journal_title：Bioorganic & medicinal chemistry

authors： Krečmerová M,Pohl R,Masojídková M,Balzarini J,Snoeck R,Andrei G

更新日期：2014-05-15 00:00:00

abstract：:A series of 18 cycloalkyl arylpyrimidines (CAPYs) were designed from lead compounds diarylpyrimidines (DAPYs), synthesized and evaluated for in vitro anti-HIV activity. Among them, the compound 1p displayed potent anti-HIV-1 activity against WT HIV-1 with an EC(50) value of 0.055 μM and a selectivity index (SI) >7290....

journal_title：Bioorganic & medicinal chemistry

authors： Gu SX,Yang SQ,He QQ,Ma XD,Chen FE,Dai HF,Clercq ED,Balzarini J,Pannecouque C

更新日期：2011-12-01 00:00:00

abstract：:Canavan disease is a fatal neurological disorder caused by defects in the metabolism of N-acetyl-l-aspartate (NAA). Recent work has shown that the devastating symptoms of this disorder are correlated with the elevated levels of NAA observed in these patients, caused as a consequence of the inability of mutated forms o...

journal_title：Bioorganic & medicinal chemistry

authors： Thangavelu B,Mutthamsetty V,Wang Q,Viola RE

更新日期：2017-02-01 00:00:00

abstract：:We report a series of tubulin targeting agents, some of which demonstrate potent antiproliferative activities. These analogs were designed to optimize the antiproliferative activity of 1 by varying the heteroatom substituent at the 4'-position, the basicity of the 4-position amino moiety, and conformational restrictio...

journal_title：Bioorganic & medicinal chemistry

authors： Xiang W,Choudhary S,Hamel E,Mooberry SL,Gangjee A

更新日期：2018-05-15 00:00:00

abstract：:In vitro evaluation of the halogenated pyrrolo[3,2-d]pyrimidines identified antiproliferative activities in compounds 1 and 2 against four different cancer cell lines. Upon screening of a series of pyrrolo[3,2-d]pyrimidines, the 2,4-Cl compound 1 was found to exhibit antiproliferative activity at low micromolar concen...

journal_title：Bioorganic & medicinal chemistry

authors： Temburnikar KW,Ross CR,Wilson GM,Balzarini J,Cawrse BM,Seley-Radtke KL

更新日期：2015-08-01 00:00:00

abstract：:The present study describes the chemical synthesis and pharmacological evaluation of a new series of eleven compounds stereoisomers of imidobenzenesulfonylaziridines in the forced-swimming test (FST) in mice. The pharmacological results of these compounds show that six of them, given intraperitoneally, reduced the imm...

journal_title：Bioorganic & medicinal chemistry

authors： Duarte FS,Andrade Eda S,Vieira RA,Uieara M,Nunes RJ,de Lima TC

更新日期：2006-08-01 00:00:00

abstract：:Antagonists of type 1 cannabinoid receptors (CB1) may be useful in treating diabetes, hepatic disorders, and fibrosis. Otenabant (1) is a potent and selective CB1 inverse agonist that was under investigation as an anti-obesity agent, but its development was halted once adverse effects associated with another marketed ...

journal_title：Bioorganic & medicinal chemistry

authors： Amato G,Wiethe R,Manke A,Vasukuttan V,Snyder R,Runyon S,Maitra R

更新日期：2019-08-15 00:00:00

abstract：:In this study, we disclose the design and synthesis of novel 4-susbtituted nipecotic acid derivatives as inhibitors of the GABA transporter mGAT1. Based on molecular modeling studies the compounds are assumed to adopt a binding pose similar to that of the potent mGAT1 inhibitor nipecotic acid. As substitution in 4-pos...

journal_title：Bioorganic & medicinal chemistry

authors： Hellenbrand T,Höfner G,Wein T,Wanner KT

更新日期：2016-05-01 00:00:00