Discovery of novel indazole-linked triazoles as antifungal agents.

abstract：:Multiple-targeted ligands can have certain advantages for the management of hypertension which has multiple controls. Molecules with dual bioactivities are available in literature for treating metabolic disorders like diabetes, hypertension and hypercholesterolemia. After scrutinizing the SAR of prazosin-type α1-block...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yadav MR,Naik PP,Gandhi HP,Chauhan BS,Giridhar R

更新日期：2013-07-01 00:00:00

abstract：:Chemical investigation of a marine-derived fungus Penicillium sp. SF-6013 resulted in the discovery of a new tanzawaic acid derivative, 2E,4Z-tanzawaic acid D (1), together with four known analogues, tanzawaic acids A (2) and D (3), a salt form of tanzawaic acid E (4), and tanzawaic acid B (5). Their structures were m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Quang TH,Ngan NTT,Ko W,Kim DC,Yoon CS,Sohn JH,Yim JH,Kim YC,Oh H

更新日期：2014-12-15 00:00:00

abstract：:Herein we report the synthesis of a series of bicyclo[3.2.1]octanes and their binding characteristics at the dopamine and serotonin transporters. The data confirm that a heteroatom at position 8 of the tropane nucleus is not a prerequisite for binding since the bicyclo[3.2.1]octanes prove potent inhibitors of both tra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Meltzer PC,Blundell P,Chen Z,Yong YF,Madras BK

更新日期：1999-03-22 00:00:00

abstract：:High throughput screening identified a phenoxyacetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a compound with functional potency for inhibition of human eosinophil shape change and oral bioavailability in the rat. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sandham DA,Aldcroft C,Baettig U,Barker L,Beer D,Bhalay G,Brown Z,Dubois G,Budd D,Bidlake L,Campbell E,Cox B,Everatt B,Harrison D,Leblanc CJ,Manini J,Profit R,Stringer R,Thompson KS,Turner KL,Tweed MF,Walker C,

更新日期：2007-08-01 00:00:00

abstract：:Makomotindoline (1) was isolated from Makomotake, Zizania latifolia infected with Ustilago esculenta. The structure was determined by the interpretation of spectroscopic data and synthesis. Makomotindoline (1), its l-Glc isomer (2) and its aglycon (3) were synthesized and their effects on rat glioma cells showed adver...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suzuki T,Choi JH,Kawaguchi T,Yamashita K,Morita A,Hirai H,Nagai K,Hirose T,Omura S,Sunazuka T,Kawagishi H

更新日期：2012-07-01 00:00:00

abstract：:Opuntia ficus-indica L. is known for its beneficial effects on human health, but still little is known on cladodes as a potent source of antioxidants. Here, a direct, economic and safe method was set up to obtain water extracts from Opuntia ficus-indica cladodes rich in antioxidant compounds. When human keratinocytes ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Petruk G,Di Lorenzo F,Imbimbo P,Silipo A,Bonina A,Rizza L,Piccoli R,Monti DM,Lanzetta R

更新日期：2017-12-15 00:00:00

abstract：:Bergenin is an isocoumarin natural product which aides in fat loss, healthy weight maintenance, enhancing the lipolytic effects of norepinephrine, inhibiting the formation of interleukin 1α and cyclooxygenases-2. Here we describe the anti-inflammatory activity of new bergenin derivatives 1-15 in the respiratory burst ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shah MR,Arfan M,Amin H,Hussain Z,Qadir MI,Choudhary MI,VanDerveer D,Mesaik MA,Soomro S,Jabeen A,Khan IU

更新日期：2012-04-15 00:00:00

abstract：:NaIO4 oxidation of allosamidin (1), a strong inhibitor of family 18 chitinases, followed by a coupling with Biotin Hydrazide afforded its mono- and dibiotinylated derivatives, 4 and 6. Reduction of 4 by NaBH4 afforded its reduced form 5. Each of these three biotinylated derivatives maintained strong chitinase inhibito...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sakuda S,Sakurada M

更新日期：1998-11-03 00:00:00

abstract：:Vitamin D receptor (VDR) ligands are therapeutic agents for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism. VDR ligands also show immense potential as therapeutic agents for autoimmune diseases and cancers of the skin, prostate, colon, and breast as well as leukemia. LG190178 is a novel no...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hakamata W,Sato Y,Okuda H,Honzawa S,Saito N,Kishimoto S,Yamashita A,Sugiura T,Kittaka A,Kurihara M

更新日期：2008-01-01 00:00:00

abstract：:Glucose transporters (GLUTs) facilitate glucose uptake and are overexpressed in most cancer cells. Inhibition of glucose transport has been shown to be an effective method to slow the growth of cancer cells both in vitro and in vivo. We have previously reported on the anticancer activity of an ester derived glucose up...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roberts DA,Wang L,Zhang W,Liu Y,Shriwas P,Qian Y,Chen X,Bergmeier SC

更新日期：2020-09-15 00:00:00

abstract：:The concurrent implementation of a proteome-wide serine hydrolase selectivity screen with traditional efforts to optimize fatty acid amide hydrolase (FAAH) inhibition potency led to the expedited discovery of a new class of exceptionally potent (Ki < 300 pM) and unusually selective (> 100-fold selective) inhibitors. T...

journal_title：Bioorganic & medicinal chemistry letters

authors： Leung D,Du W,Hardouin C,Cheng H,Hwang I,Cravatt BF,Boger DL

更新日期：2005-03-01 00:00:00

abstract：:In this letter, we describe the first synthesis of two recently isolated flavones 5-carbomethoxymethyl-7-hydroxy-2-pentylchromone (3a), 5-carboethoxymethyl-4',7-dihydroxyflavone (3b) and their derivatives (3c-t), evaluated for their antimicrobial, antioxidant and anticancer activities. Most of the synthesized compound...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Murty JN,Viswanath A,Sujitha P,Ganesh Kumar C

更新日期：2012-07-15 00:00:00

abstract：:Utilizing a combination of high-throughput and multi-step synthesis, SAR in a novel series of M(1) acetylcholine receptor antagonists was rapidly established. The efforts led to the discovery the highly potent M(1) antagonists 6 (VU0431263), and 8f (VU0433670). Functional Schild analysis and radioligand displacement e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Poslusney MS,Sevel C,Utley TJ,Bridges TM,Morrison RD,Kett NR,Sheffler DJ,Niswender CM,Daniels JS,Conn PJ,Lindsley CW,Wood MR

更新日期：2012-11-15 00:00:00

abstract：:Betulinic acid has been modified at C-3, C-20, and C-28 positions and the toxicity of the derivatives has been evaluated against cultured human melanoma (MEL-2) and human epidermoid carcinoma of the mouth (KB) cell lines. This preliminary investigation demonstrates that simple modifications of the parent structure of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim DS,Pezzuto JM,Pisha E

更新日期：1998-07-07 00:00:00

abstract：:The shift in apparent IC(50) that attends addition of serum proteins to in vitro cellular, enzymatic, and receptor binding assays can be used to determine the dissociation constant for compound-serum protein complexes. We show here that a simple linear relationship exists between the apparent IC(50) in the presence of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rusnak DW,Lai Z,Lansing TJ,Rhodes N,Gilmer TM,Copeland RA

更新日期：2004-05-03 00:00:00

abstract：:This paper describes the preliminary biological results that novel T-type calcium channel blockers inhibit the growth of human cancer cells by blocking calcium influx into the cell, based on unknown mechanism on the cell cycle responsible for cellular proliferation. Among the selected compounds from compound library, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JY,Park SJ,Park SJ,Lee MJ,Rhim H,Seo SH,Kim KS

更新日期：2006-10-01 00:00:00

abstract：:Germinal center kinase-like kinase (GLK, also known as MAP4K3) has been hypothesized to have an effect on key cellular activities, including inflammatory responses. GLK is required for activation of protein kinase C-θ (PKCθ) in T cells. Controlling the activity of T helper cell responses could be valuable for the trea...

journal_title：Bioorganic & medicinal chemistry letters

authors： May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K

更新日期：2018-06-01 00:00:00

abstract：:A novel synthetic method was developed for the synthesis of venlafaxine using inexpensive reagents. An improvement in the method, in the yield was achieved for the conversion of the venlafaxine. This is an improved version, simple and efficient method for the large-scale synthesis of venlafaxine. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Basappa,Kavitha CV,Rangappa KS

更新日期：2004-06-21 00:00:00

abstract：:Nineteen new 2-pyrazoline bearing benzenesulfonamide derivatives were synthesized by condensing chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride. Their chemical structures were proved by means of IR, (1)H NMR, (13)C NMR, mass spectroscopic and elemental analyses data. These compounds were tested at dose of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rathish IG,Javed K,Ahmad S,Bano S,Alam MS,Pillai KK,Singh S,Bagchi V

更新日期：2009-01-01 00:00:00

abstract：:Structure-activity relationships (SAR) of fused 1,2,4-triazolo[1,5-c ]pyrimidine were performed. Various substituents were introduced into the heterocyclic ring to improve the potency of adenosine A(3) receptor binding affinity and A(3)-selectivity against other subtypes. Potent and selective A(3) receptor antagonists...

journal_title：Bioorganic & medicinal chemistry letters

authors： Okamura T,Kurogi Y,Hashimoto K,Sato S,Nishikawa H,Kiryu K,Nagao Y

更新日期：2004-07-16 00:00:00

abstract：:Selective metabotropic glutamate receptor 2 (mGluR2) inhibitors have been demonstrated to show therapeutic effects by improving alleviating symptoms of schizophrenic patients in clinical studies. Herein we report the synthesis and preliminary evaluation of a 11C-labeled positron emission tomography (PET) tracer origin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumata K,Zhang Y,Ogawa M,Kurihara Y,Mori W,Hu K,Fujinaga M,Nengaki N,Zhang MR

更新日期：2020-12-01 00:00:00

abstract：:The development of novel non-phosphopeptide inhibitors for the Src family SH2 domain is described. Several commercially available hydroxyl aromatic acids have been appended off the N-terminus of pYEEIE and the potent phosphopeptide inhibitors of GST-Lck-SH2 were identified via ELISA. The most potent inhibitor, caffeic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park SH,Won J,Lee KH

更新日期：2002-10-07 00:00:00

abstract：:The transcription factor ΔFosB accumulates in response to chronic insults such as drugs of abuse, L-3,4-dihydroxyphenylalanine (l-DOPA) or stress in specific regions of the brain, triggering long lasting neural and behavioral changes that underlie aspects of drug addiction, dyskinesia, and depression. Thus, small mole...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Y,Liu Z,Aglyamova G,Chen J,Chen H,Bhandari M,White MA,Rudenko G,Zhou J

更新日期：2020-08-15 00:00:00

abstract：:A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A receptor antagonism and serotonin reuptake inhibition was discovered. 1-(1H-Indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high affinities at the 5-HT1A receptor and serotonin reuptake site in vitro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takeuchi K,Kohn TJ,Honigschmidt NA,Rocco VP,Spinazze PG,Hemrick-Luecke SK,Thompson LK,Evans DC,Rasmussen K,Koger D,Lodge D,Martin LJ,Shaw J,Threlkeld PG,Wong DT

更新日期：2006-05-01 00:00:00

abstract：:The synthesis and inhibitory activities of 10 potential inhibitors of Pfmrk, a Plasmodium falciparum cyclin-dependent protein kinase, are described. The most potent inhibitor is a 3-phenyl-quinolinone compound with an IC(50) value of 18 microM. It is the first compound reported to inhibit Pfmrk at the micro molar rang...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao Z,Waters NC,Woodard CL,Li Z,Li PK

更新日期：2001-11-05 00:00:00

abstract：:Mismatch binding protein MutS binding to bulge structure in DNA duplexes was controlled by UV irradiation. 4-O-(2-Nitrobenzyl)thymidine or 4-O-[2-(2-nitrophenyl)propyl]thymidine was incorporated into DNA duplexes a bulged position. The MutS did not bind to the caged DNA duplexes but bound after removing the 2-nitroben...

journal_title：Bioorganic & medicinal chemistry letters

authors： Seio K,Ohno Y,Ohno K,Takeshita L,Kanamori T,Masaki Y,Sekine M

更新日期：2016-10-01 00:00:00

abstract：:Novel analogues of the angiotensin I-converting enzyme (ACE) inhibitor keto-ACE were synthesized via a facile Horner-Emmons olefination of a phosphonoketone precursor with ethyl glyoxylate. Introduction of a bulky aromatic tryptophan at the P(2)(') position of keto-ACE resulted in a significant increase in C-domain-se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nchinda AT,Chibale K,Redelinghuys P,Sturrock ED

更新日期：2006-09-01 00:00:00

abstract：:We previously identified o-carborane bisphenol BE360 (4) as a selective estrogen receptor modulator (SERM), which ameliorated bone loss without inducing estrogenic action in uterus of OVX and ORX mice. Here, we synthesized a fluorinated derivative, B-fluorinated o-carborane bisphenol BE310 (5) by means of S(N)Ar react...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohta K,Ogawa T,Endo Y

更新日期：2012-07-15 00:00:00

abstract：:Based on the previously reported lead compound, a series of benzofuran derivatives were prepared to study their antagonistic activities to A(2A) receptor. The replacement of the phenyl group at the 4-position with a heterocyclic ring improved the PK profile and aqueous solubility. From these studies, we discovered a p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saku O,Saki M,Kurokawa M,Ikeda K,Uchida S,Takizawa T,Uesaka N

更新日期：2010-06-15 00:00:00

abstract：:Backbone-modified DNA analogs were synthesized in good yields by the boranophosphotriester method on a solid support. The oligodeoxyribonucleoside boranophosphates, protected with 2-(azidomethyl)benzoyl groups for nucleobases, were converted into DNA and its backbone-modified analogs via the corresponding H-phosphonat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kawanaka T,Shimizu M,Shintani N,Wada T

更新日期：2008-07-01 00:00:00