Investigating the activity of 2-substituted alkyl-6-(2,5-dioxopyrrolidin-1-yl)hexanoates as skin penetration enhancers.

abstract：:Condensation of substituted anthranilic acids with 4-isothiocyanatoethyl-benzenesulfonamide led to series of heterocyclic benzenesulfonamides incorporating 2-mercapto-quinazolin-4-one tails. These sulfonamides were investigated as inhibitors of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA I and II (cyto...

journal_title：Bioorganic & medicinal chemistry

authors： Bozdag M,Alafeefy AM,Carta F,Ceruso M,Al-Tamimi AS,Al-Kahtani AA,Alasmary FAS,Supuran CT

更新日期：2016-09-15 00:00:00

abstract：:Synthesis and antimicrobial activity of squalamine analogue 2 are reported. The synthesis of 2 was accomplished from bisnoralcohol 3. The spermidine moiety was introduced via reductive amination of an appropriately functionalized 3beta-aminosterol with spermidinyl aldehyde 17 utilizing sodium triacetoxyborohydride as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kim HS,Choi BS,Kwon KC,Lee SO,Kwak HJ,Lee CH

更新日期：2000-08-01 00:00:00

abstract：:Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC(50) of 16 compounds which have displayed MIC of 0.25 microg/mL were also recorded. One of the compounds (...

journal_title：Bioorganic & medicinal chemistry

authors： Madapa S,Tusi Z,Mishra A,Srivastava K,Pandey SK,Tripathi R,Puri SK,Batra S

更新日期：2009-01-01 00:00:00

abstract：:In our search for a novel class of non-TZD, non-carboxylic acid peroxisome proliferator-activated receptor (PPAR) γ agonists, we explored alternative lipophilic templates to replace benzylpyrazole core of the previously reported agonist 1. Introduction of a pentylsulfonamide group into arylpropionic acids derived from...

journal_title：Bioorganic & medicinal chemistry

authors： Rikimaru K,Wakabayashi T,Abe H,Tawaraishi T,Imoto H,Yonemori J,Hirose H,Murase K,Matsuo T,Matsumoto M,Nomura C,Tsuge H,Arimura N,Kawakami K,Sakamoto J,Funami M,Mol CD,Snell GP,Bragstad KA,Sang BC,Dougan DR,Tanak

更新日期：2012-05-15 00:00:00

abstract：:Cyclopentane derivatives, designated as BCX-1812, BCX-1827, BCX-1898, and BCX-1923, were tested in parallel with oseltamivir carboxylate and zanamivir for the in vivo activity in mice infected with A/Turkey/Mas/76 X A/Beijing/32/92 (H6N2) influenza virus. The compounds were tested orally and intranasally at different ...

journal_title：Bioorganic & medicinal chemistry

authors： Chand P,Bantia S,Kotian PL,El-Kattan Y,Lin TH,Babu YS

更新日期：2005-06-02 00:00:00

abstract：:An unusual class of 5,6,7-trioxygenated dihydroflavonols (3a-e and 4a-j) were designed and prepared. Their antioxidative properties were assessed by examining their capacities in several in vitro models, including superoxide anion and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, rat liver homogenate lipid ...

journal_title：Bioorganic & medicinal chemistry

authors： Gong J,Huang K,Wang F,Yang L,Feng Y,Li H,Li X,Zeng S,Wu X,Stöckigt J,Zhao Y,Qu J

更新日期：2009-05-01 00:00:00

abstract：:Colorectal cancer is the third and fourth leading cause of cancer in males and females, respectively. Flavonoids, including chalcones, are secondary metabolites in plants that exhibit diverse biological activities, including antibacterial, antimalarial, and antitumor activities. In order to find potent and novel chemo...

journal_title：Bioorganic & medicinal chemistry

authors： Shin SY,Yoon H,Hwang D,Ahn S,Kim DW,Koh D,Lee YH,Lim Y

更新日期：2013-11-15 00:00:00

abstract：:The three-dimensional structure of the endothelin B receptor (ETB) selective antagonist RES-701-1 has been determined by 1H NMR in deuterated dimethyl sulphoxide. RES-701-1 consists of 16 amino acid residues with a novel internal linkage between the beta-carboxyl group of Asp9 and the alpha-amino group of Gly1. The st...

journal_title：Bioorganic & medicinal chemistry

authors： Katahira R,Shibata K,Yamasaki M,Matsuda Y,Yoshida M

更新日期：1995-09-01 00:00:00

abstract：:A growing number of proteins are known to exert their regulatory or biological functions via RNA binding. In some cases genetic interactions allow us to infer candidate targets for RNA directed regulation, but in many other cases identification of potential regulatory targets is problematic. We have developed an in vi...

journal_title：Bioorganic & medicinal chemistry

authors： Brunel C,Ehresmann B,Ehresmann C,McKeown M

更新日期：2001-10-01 00:00:00

abstract：:Avermectin B1a (1) is a potent anthelmintic, insecticide, miticide and chloride channel activator on interaction with a specific nerve membrane site analyzed by binding assays with [3H]1. Candidate photoaffinity probes were prepared replacing the dioleandrosyl substituent with potential isosteric esters and ethers app...

journal_title：Bioorganic & medicinal chemistry

authors： Tsukamoto Y,Cole LM,Casida JE

更新日期：2000-01-01 00:00:00

abstract：:The cyclohexyl piperazine 1 (1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine) has been shown to be a potent and selective sigma-2 receptor ligand. In the present study, we prepared [(11)C]1 by O-alkylation of the phenolic precursor 2 with [(11)C]CH(3)I. [(11)C]1 was obtained in a 29...

journal_title：Bioorganic & medicinal chemistry

authors： Kassiou M,Dannals RF,Liu X,Wong DF,Ravert HT,Scheffel UA

更新日期：2005-06-01 00:00:00

abstract：:Two groups of benzimidazole derivatives were synthesized using as precursors 5(6)-substituted 2-mercapto-benzimidazol-thiols and their antioxidant activity was investigated using TBA-MDA test. In the group of 1,3-disubstituted-benzimidazol-2-imines the highest lipid peroxidation inhibition effect 74.04% (IC₅₀=141.89 μ...

journal_title：Bioorganic & medicinal chemistry

authors： Mavrova ATs,Yancheva D,Anastassova N,Anichina K,Zvezdanovic J,Djordjevic A,Markovic D,Smelcerovic A

更新日期：2015-10-01 00:00:00

abstract：:We describe the syntheses, physicochemical properties and biological evaluation of a novel series of complexones containing bis- or biazoles moieties and two iminodiacetic acid units as novel ligands for paramagnetic lanthanides. The complexones were prepared by reaction of the corresponding 1,1'-bishaloethylbi- or bi...

journal_title：Bioorganic & medicinal chemistry

authors： Mayoral EP,García-Amo M,López P,Soriano E,Cerdán S,Ballesteros P

更新日期：2003-12-01 00:00:00

abstract：:The boranophosphate ester nucleotides are a new class of nucleic acid analogues that are isoelectronic and isostructural to normal phosphodiester nucleic acids and that maintain the anionic charge of the nucleic acid backbone. The two P-diastereoisomers of dithymidine boranomonophosphates were separated using reverse ...

journal_title：Bioorganic & medicinal chemistry

authors： Li H,Huang F,Shaw BR

更新日期：1997-05-01 00:00:00

abstract：:Natural product inspired compound collections are prevalidated due to the evolutionary selection of the natural product scaffolds. Their synthesis requires the development of novel strategies amenable to formats suitable for library build-up. We describe a method for the synthesis of an oxepane library inspired by the...

journal_title：Bioorganic & medicinal chemistry

authors： Basu S,Waldmann H

更新日期：2014-08-15 00:00:00

abstract：:The nitronate and nitrovinyl methods to synthesize indole glucosinolates (GLs) have been investigated. The results were applied to generally the most prevalent natural indole glucosinolates to synthesize 4-methoxyglucobrassicin (MGB) and neo-glucobrassicin (NGB) in moderate overall yield for the first time. The anti-i...

journal_title：Bioorganic & medicinal chemistry

authors： Vo QV,Trenerry C,Rochfort S,Wadeson J,Leyton C,Hughes AB

更新日期：2014-01-15 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：:Seven new nitrogen heterocycle porphyrins, 5,10,15,20-tetra[4-(N-pyrrolidinyl)phenyl]porphine (TBPPH(2)), 5,10,15,20-tetra[4-(4'-ethylpiperazinyl)phenyl]porphine (TEPPH(2)), 5,10,15,20-tetra [4-(4'-butylpiperazinyl)phenyl]porphine (TUPPH(2)), 5,10,15,20-tetra[4-(4'-heptylpiperazinyl) phenyl]porphine (THPPH(2)), 5-[4-(...

journal_title：Bioorganic & medicinal chemistry

authors： Guo CC,Li HP,Zhang XB

更新日期：2003-04-17 00:00:00

abstract：:17β-Hydroxysteroid dehydrogenase type 3 (17β-HSD3) is a key enzyme involved in the biosynthesis of testosterone and dihydrotestosterone. These hormones are known to stimulate androgen-dependent prostate cancer. In order to generate effective inhibitors of androgen biosynthesis without androgenic effect, we synthesized...

journal_title：Bioorganic & medicinal chemistry

authors： Djigoué GB,Kenmogne LC,Roy J,Maltais R,Poirier D

更新日期：2015-09-01 00:00:00

abstract：:We have used fluorescence anisotropy to measure in situ the thermodynamics of binding of alanine-rich mutants of the GCN4 basic region/leucine zipper (bZIP) to short DNA duplexes, in which thymines were replaced with uracils, in order to quantify the contributions of the C5 methyl group on thymines with alanine methyl...

journal_title：Bioorganic & medicinal chemistry

authors： Kise KJ Jr,Shin JA

更新日期：2001-09-01 00:00:00

abstract：:The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small molecules. Acquired drug resistance against first-line EGFR inhibitors remains the major bottleneck in NSCLC and is currently addressed by the appl...

journal_title：Bioorganic & medicinal chemistry

authors： Basu D,Richters A,Rauh D

更新日期：2015-06-15 00:00:00

abstract：NAD(P)H:quinone oxidoreductase 1 (NQO1) is an obligate two-electron reductase and is highly expressed in many human solid cancers. Because NQO1 can be induced immediately after exposure to ionizing radiation, we aimed to develop an NQO1-targeted radiolabeled agent to establish a novel internal radiation therapy that am...

journal_title：Bioorganic & medicinal chemistry

authors： Sasaki J,Sano K,Hagimori M,Yoshikawa M,Maeda M,Mukai T

更新日期：2014-11-01 00:00:00

abstract：:A novel peptidyl chemosensor (PySO2-His-Gly-Gly-Lys(PySO2)-NH2, 1) was synthesized by incorporation of two pyrene (Py) fluorophores into the tetrapeptide using sulfonamide group. Compound 1 exhibited selective fluorescence response towards Hg(II) over the other metal ions in aqueous buffered solutions. Furthermore, 1 ...

journal_title：Bioorganic & medicinal chemistry

authors： Thirupathi P,Lee KH

更新日期：2013-12-15 00:00:00

abstract：:Fourteen beta-elemene derivatives containing a piperazine, a morpholine, a tetrahydropyrrole, a thiophenylethylamine, or a cyclohexamine group were synthesized. The structures of these beta-elemene derivatives were characterized with IR, 1H NMR, MS, and elemental analyses. All these derivatives had an increased anti-p...

journal_title：Bioorganic & medicinal chemistry

authors： Xu L,Tao S,Wang X,Yu Z,Wang M,Chen D,Jing Y,Dong J

更新日期：2006-08-01 00:00:00

abstract：:Twenty-one benzotriazoles (3-16 and 18-24) were synthesized and half of them (5, 8-16, 20, and 21) were reported for the first time. Their antiproliferative activities against three human cancer cells were assayed. It revealed that 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate (9) showed considerable activit...

journal_title：Bioorganic & medicinal chemistry

authors： Fu J,Yang Y,Zhang XW,Mao WJ,Zhang ZM,Zhu HL

更新日期：2010-12-15 00:00:00

abstract：:A series of pyrrolobenzodiazepine-naphthalimide conjugates tethered through a piperazine ring system have been designed, synthesized, and evaluated for their anticancer activity. These new conjugates exhibit very high DNA binding affinity and cytotoxic activity against a number of cell lines. ...

journal_title：Bioorganic & medicinal chemistry

authors： Kamal A,Ramu R,Tekumalla V,Khanna GB,Barkume MS,Juvekar AS,Zingde SM

更新日期：2008-08-01 00:00:00

abstract：:Peptides are limited in their use as drugs due to low cell permeability and vulnerability to proteases. In contrast, peptoids are immune to enzymatic degradation and some peptoids have been shown to be relatively cell permeable. In order to facilitate future design of peptoid libraries for screening experiments, it wo...

journal_title：Bioorganic & medicinal chemistry

authors： Tan NC,Yu P,Kwon YU,Kodadek T

更新日期：2008-06-01 00:00:00

abstract：:The histamine H(3) receptor (H(3)R) plays a role in cognition and memory processes and is implicated in different neurological disorders, including Alzheimer's disease, schizophrenia, and narcolepsy. In vivo studies of the H(3)R occupancy using a radiolabeled PET tracer would be very useful for CNS drug discovery and ...

journal_title：Bioorganic & medicinal chemistry

authors： Selivanova SV,Honer M,Combe F,Isensee K,Stark H,Krämer SD,Schubiger PA,Ametamey SM

更新日期：2012-05-01 00:00:00

abstract：:KPU-105 (4), a potent anti-microtubule agent that contains a benzophenone was derived from the diketopiperazine-type vascular disrupting agent (VDA) plinabulin 3, which displays colchicine-like tubulin depolymerization activity. To develop derivatives with more potent anti-microtubule and cytotoxic activities, we furt...

journal_title：Bioorganic & medicinal chemistry

authors： Yamazaki Y,Sumikura M,Masuda Y,Hayashi Y,Yasui H,Kiso Y,Chinen T,Usui T,Yakushiji F,Potts B,Neuteboom S,Palladino M,Lloyd GK,Hayashi Y

更新日期：2012-07-15 00:00:00

abstract：:Tuberculosis is today amongst the worldwide health threats. As resistant strains of Mycobacterium tuberculosis have slowly emerged, treatment failure is too often a fact, especially in countries lacking the necessary health care organisation to provide the long and costly treatment adapted to patients. Because of lack...

journal_title：Bioorganic & medicinal chemistry

authors： Janin YL

更新日期：2007-04-01 00:00:00