2,4-Disubstituted oxazoles and thiazoles as latent pharmacophores for diacylhydrazine of SC-51089, a potent PGE2 antagonist.

abstract：:It looks that a new era of antimicrobial peptides (AMPs) started with the discovery of teixobactin, which is a "head to side-chain" cyclodepsipeptide. It was isolated from a soil gram-negative b-proteobacteria by means of a revolutionary technique. Since there, several groups have developed synthetic strategies for ef...

journal_title：Bioorganic & medicinal chemistry

authors： Abdel Monaim SAH,Jad YE,El-Faham A,de la Torre BG,Albericio F

更新日期：2018-06-01 00:00:00

abstract：:Gangjee et al. recently reported a novel series of 2-amino-4-methyl-5-phenylethyl substituted-7-benzyl-pyrrolo[2,3-d]pyrimidines, some of which exhibited two digit nanomolar antitumor and antimitotic activity and were not subject to P-glycoprotein (Pgp) or multidrug resistance protein 1 (MRP1) mediated tumor resistanc...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Namjoshi OA,Keller SN,Smith CD

更新日期：2011-07-15 00:00:00

abstract：:Geranylgeranyl diphosphate synthase (GGDPS) inhibitors are of potential therapeutic interest as a consequence of their activity against the bone marrow cancer multiple myeloma. A series of bisphosphonates linked to an isoprenoid tail through an amide linkage has been prepared and tested for the ability to inhibit GGDP...

journal_title：Bioorganic & medicinal chemistry

authors： Goetz DB,Varney ML,Wiemer DF,Holstein SA

更新日期：2020-08-15 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：:The binding specificities of the closely related lectins from Canavalia ensiformis and Dioclea grandiflora were examined using specifically O-alkylated mono- and disaccharides. Both lectins accept any substitution at the monosaccharide C2 hydroxyl group. The binding energy of C2-alkylated ligands-concanavalin A comple...

journal_title：Bioorganic & medicinal chemistry

authors： Chervenak MC,Toone EJ

更新日期：1996-11-01 00:00:00

abstract：:A novel series of substituted imidazol-5-ones were designed, synthesized and evaluated for in vitro reverse transcriptase (RT) inhibition activity using reverse transcriptase assay kit (Roche, Colorimetric). It has been observed from in vitro screening that newly synthesized compounds possess RT inhibitory activity. D...

journal_title：Bioorganic & medicinal chemistry

authors： Mokale SN,Lokwani D,Shinde DB

更新日期：2012-05-01 00:00:00

abstract：:Hypoxia is a common characteristic of many types of solid tumors and is associated with tumor propagation, malignant progression, and resistance to anti-cancer therapy. HIF-1 pathway is one of the survival pathways activated in tumor in response to hypoxia. In hypoxic condition, hypoxia-inducible factor-1α (HIF-1α) is...

journal_title：Bioorganic & medicinal chemistry

authors： Li J,Xi W,Li X,Sun H,Li Y

更新日期：2019-04-01 00:00:00

abstract：:Further structure-activity relationship (SAR) studies with the 1,2,3,4-tetrahydroisoquinoline (THIQ) class of 5-HT(1A) ligands led to the synthesis of new 1-adamantoyloaminoalkyl derivatives. The impact of substituent variations in the aromatic part of THIQ moiety on 5-HT(1A) and 5-HT(2A) receptor affinities, as well ...

journal_title：Bioorganic & medicinal chemistry

authors： Bojarski AJ,Mokrosz MJ,Minol SC,Kozioł A,Wesołowska A,Tatarczyńska E,Kłodzińska A,Chojnacka-Wójcik E

更新日期：2002-01-01 00:00:00

abstract：:A branched peptide containing multiple boronic acids was found to bind RRE IIB selectively and inhibit HIV-1 p24 capsid production in a dose-dependent manner. Structure-activity relationship studies revealed that branching in the peptide is crucial for the low micromolar binding towards RRE IIB, and the peptide demons...

journal_title：Bioorganic & medicinal chemistry

authors： Wynn JE,Zhang W,Tebit DM,Gray LR,Hammarskjold ML,Rekosh D,Santos WL

更新日期：2016-09-01 00:00:00

abstract：:A series of novel 6-methylene-bridged uracil derivatives have been optimized for clinical use as the inhibitors of human thymidine phosphorylase (TP). We describe their synthesis and evaluation. Introduction of a guanidino or an amidino group enhanced the in vitro inhibitory activity of TP comparing with formerly repo...

journal_title：Bioorganic & medicinal chemistry

authors： Yano S,Kazuno H,Sato T,Suzuki N,Emura T,Wierzba K,Yamashita J,Tada Y,Yamada Y,Fukushima M,Asao T

更新日期：2004-07-01 00:00:00

abstract：:Ethyl 3-aryl-3-oxopropanoates (aryl: phenyl, 2-fluorophenyl, 3-nitrophenyl, and 4-nitrophenyl) were reduced enantioselectively to the corresponding (S)-alcohols by the fungus Rhizopus arrhizus and other Rhizopus sp. The best results were generally obtained with Rhizopus arrhizus (wild type) and Rhizopus nivius NCIM 95...

journal_title：Bioorganic & medicinal chemistry

authors： Salvi NA,Chattopadhyay S

更新日期：2006-07-15 00:00:00

abstract：:5-HT(7) receptor antagonists generated antidepressant-like effects in animal model and the involvement of the 5-HT(7) receptor in other pathophysiological mechanisms such as thermoregulation, learning and memory, and sleep has been highlighted by various studies. As one of our efforts to discover a new type of 5-HT(7)...

journal_title：Bioorganic & medicinal chemistry

authors： Na YH,Hong SH,Lee JH,Park WK,Baek DJ,Koh HY,Cho YS,Choo H,Pae AN

更新日期：2008-03-01 00:00:00

abstract：:(1S,2E,4S,6R,7E,11E)-2,7,11-Cembratriene-4,6-diol (1) and its 4-epi-analog (2) are the cembranoid precursors to several key flavor ingredients in most Nicotiana (tobacco) species. Nearly 40-60% of 1 and 2 are purposely degraded during the commercial tobacco fermentation. However, 1 and 2 display promising bioactivitie...

journal_title：Bioorganic & medicinal chemistry

authors： Ebrahim HY,Mohyeldin MM,Hailat MM,El Sayed KA

更新日期：2016-11-15 00:00:00

abstract：:A set of phosphonic acid derivatives (1-4) of pyridoxal 5'-phosphate (PLP) was synthesized and characterized biochemically using purified murine pyridoxal phosphatase (PDXP), also known as chronophin. The most promising compound 1 displayed primarily competitive PDXP inhibitory activity with an IC50 value of 79μM, whi...

journal_title：Bioorganic & medicinal chemistry

authors： Knobloch G,Jabari N,Stadlbauer S,Schindelin H,Köhn M,Gohla A

更新日期：2015-06-15 00:00:00

abstract：:Bexarotene (1), a retinoid X receptor (RXR) agonist approved for the treatment of cutaneous T cell lymphoma (CTCL), was reported to migrate into baboon brain based on findings obtained by positron emission tomography (PET) with a 11C-labeled tracer. However, co-administration of non-radioactive 1 had no effect on the ...

journal_title：Bioorganic & medicinal chemistry

authors： Takamura Y,Shibahara O,Watanabe M,Fujihara M,Yamada S,Akehi M,Sasaki T,Hirano H,Kakuta H

更新日期：2019-07-15 00:00:00

abstract：:We report structure-activity investigations in a series of tripeptide amide inhibitors of thrombin, and the development of a series of highly potent active site directed alpha-keto carbonyl inhibitors having the side chain of lysine at P1. Compounds of this class are unstable by virtue of reactivity at the electrophil...

journal_title：Bioorganic & medicinal chemistry

authors： Brady SF,Sisko JT,Stauffer KJ,Colton CD,Qiu H,Lewis SD,Ng AS,Shafer JA,Bogusky MJ,Veber DF

更新日期：1995-08-01 00:00:00

abstract：:In this study a new set of thiazolo[5,4-d]pyrimidine derivatives was synthesized. These derivatives bear different substituents at positions 2 and 5 of the thiazolopyrimidine core while maintaining a free amino group at position-7. The new compounds were tested for their affinity and potency at human (h) A1, A2A, A2B ...

journal_title：Bioorganic & medicinal chemistry

authors： Varano F,Catarzi D,Falsini M,Vincenzi F,Pasquini S,Varani K,Colotta V

更新日期：2018-07-23 00:00:00

abstract：:Serotonin (5-hydroxytryptamine, 5-HT) is an important signaling molecule in the central nervous system (CNS) and in non-neuronal tissues and organs. Serotonin mediates a positive chronotropic and inotropic response through 5-HT4 receptors in the atrium and ventricle of the heart. Recent investigations have revealed in...

journal_title：Bioorganic & medicinal chemistry

authors： Brudeli B,Andressen KW,Moltzau LR,Nilsen NO,Levy FO,Klaveness J

更新日期：2013-11-15 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：:Three peptide amides, HPRK(Py)(4)HPRK-NH(2) (PyH-12), HPRK(Py)(3)HPRK-NH(2) (PyH-11) and HPRK(Py)(2)HPRK-NH(2) (PyH-10), incorporating two HPRK motifs and various 4-amino-1-methylpyrrole-2-carboxylic acid residues (Py) were synthesized by solid-phase peptide methodology. The binding of these three peptides to a 5'-32P...

journal_title：Bioorganic & medicinal chemistry

authors： Chang JC,Yang CH,Chou PY,Yang WH,Chou IC,Lu CT,Lin PH,Hou RC,Jeng KC,Cheng CC,Sheh L

更新日期：2004-01-02 00:00:00

abstract：:Cytosolic (TrxR1) and mitochondrial (TrxR2) thioredoxin reductases experience pronounced concentration- and time-dependent inhibition when incubated with the two naphthodianthrones hypericin and pseudohypericin. Pseudohypericin turned out to be a quite strong inhibitor of TrxR1 (IC(50)=4.40μM) being far more effective...

journal_title：Bioorganic & medicinal chemistry

authors： Sorrentino F,Karioti A,Gratteri P,Rigobello MP,Scutari G,Messori L,Bindoli A,Chioccioli M,Gabbiani C,Bergonzi MC,Bilia AR

更新日期：2011-01-01 00:00:00

abstract：:As part of an investigation to generate optimized drug leads from marine natural pharmacophores for the treatment of neoplastic and infectious diseases, a series of novel isoaaptamine analogs were prepared by coupling acyl halides to the C9 position of isoaaptamine (2) isolated from the Aaptos sponge. This library of ...

journal_title：Bioorganic & medicinal chemistry

authors： Gul W,Hammond NL,Yousaf M,Bowling JJ,Schinazi RF,Wirtz SS,de Castro Andrews G,Cuevas C,Hamann MT

更新日期：2006-12-15 00:00:00

abstract：:We have prepared a series of potent antihypertensive 1-benzazepin-2-one calcium channel blockers (CCBs) 1 that are structurally related to diltiazem 2. Structural studies and the preparation of conformationally constrained analogs of 1-benzazepin-2-ones have led us to postulate a receptor-bound conformation for both 1...

journal_title：Bioorganic & medicinal chemistry

authors： Kimball SD,Hunt JT,Barrish JC,Das J,Floyd DM,Lago MW,Lee VG,Spergel SH,Moreland S,Hedberg SA

更新日期：1993-10-01 00:00:00

abstract：:To assist in the development of technetium-based radiopharmaceuticals that are useful for the diagnostic imaging of steroid receptor-positive breast tumors, we have synthesized a series of small-sized metal chelates according to 'n + 1' mixed-ligand, thioether-carbonyl and organometallic designs. In these preliminary ...

journal_title：Bioorganic & medicinal chemistry

authors： Wüst F,Skaddan MB,Leibnitz P,Spies H,Katzenellenbogen JA,Johannsen B

更新日期：1999-09-01 00:00:00

abstract：:The outcomes of breast cancer patients are still poor although new compounds have recently been introduced into the clinic. Therefore, novel chemical approaches are required. In the present study, palladium(II) and corresponding platinum(II) complexes containing bis(2-pyridylmethyl)amine (bpma) and saccharine were syn...

journal_title：Bioorganic & medicinal chemistry

authors： Ari F,Ulukaya E,Sarimahmut M,Yilmaz VT

更新日期：2013-06-01 00:00:00

abstract：:CNS diseases such as Parkinson, schizophrenia, and attention deficit hyperactivity disorder (ADHD) are characterized by a significant alteration of dopamine transporter (DAT) density. Thus, the development of compounds that are able to selectively interact with DAT is of great interest. Herein we describe the design a...

journal_title：Bioorganic & medicinal chemistry

authors： Cini N,Danieli E,Menchi G,Trabocchi A,Bottoncetti A,Raspanti S,Pupi A,Guarna A

更新日期：2006-08-01 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：:Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. We generated two series of esters by multi-step synthesis with substituted 6-aminohexanoic acid as potential transdermal penetration enhancers by multi-step synthesis. Th...

journal_title：Bioorganic & medicinal chemistry

authors： Brychtova K,Opatrilova R,Raich I,Kalinowski DS,Dvorakova L,Placek L,Csollei J,Richardson DR,Jampilek J

更新日期：2010-12-15 00:00:00

abstract：:The amyloid-like fibril is considered to be a macromolecular self-assemblage with a highly-ordered quaternary structure, in which numerous beta-stranded polypeptide chains align regularly. Therefore, this kind of fibril has the potential to be engineered into proteinaceous materials, although conformational alteration...

journal_title：Bioorganic & medicinal chemistry

authors： Takahashi Y,Mihara H

更新日期：2004-02-15 00:00:00

abstract：:Here we report on a novel fluorescent analog of phenytoin as a potential inhibitor of neuropathic pain with potential use as an imaging agent. Compound 2 incorporated a heptyl side chain and dansyl moiety onto the parent compound phenytoin and produced greater displacement of BTX from sodium channels and greater funct...

journal_title：Bioorganic & medicinal chemistry

authors： Walls TH,Grindrod SC,Beraud D,Zhang L,Baheti AR,Dakshanamurthy S,Patel MK,Brown ML,MacArthur LH

更新日期：2012-09-01 00:00:00