Novel fluoroquinolones: design, synthesis, and in vivo activity in mice against Mycobacterium tuberculosis H37Rv.

abstract：:Bis-(aryl)thioureas were found to be potent and selective inhibitors of cytomegalovirus (CMV) in cultured HFF cells. Of these, the thiazole analogue 38 was investigated as a potential development candidate. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bloom JD,DiGrandi MJ,Dushin RG,Curran KJ,Ross AA,Norton EB,Terefenko E,Jones TR,Feld B,Lang SA

更新日期：2003-09-01 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：:New cis-fused tetrahydrochromeno[4,3-b]quinolines have been synthesized by intramolecular [4+2] imino-Diels-Alder reactions of 2-azadienes derived in situ from aromatic amines and 7-O-prenyl derivatives of 8-formyl-2,3-disubstituted chromenones in the presence of 20mol% Yb(OTf)(3) in acetonitrile under reflux conditio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nagaiah K,Venkatesham A,Srinivasa Rao R,Saddanapu V,Yadav JS,Basha SJ,Sarma AV,Sridhar B,Addlagatta A

更新日期：2010-06-01 00:00:00

abstract：:We report the discovery of a novel series of ATP-competitive Janus kinase 3 (JAK3) inhibitors based on the 5H-pyrrolo[2,3-b]pyrazine scaffold. The initial leads in this series, compounds 1a and 1h, showed promising potencies, but a lack of selectivity against other isoforms in the JAK family. Computational and crystal...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jaime-Figueroa S,De Vicente J,Hermann J,Jahangir A,Jin S,Kuglstatter A,Lynch SM,Menke J,Niu L,Patel V,Shao A,Soth M,Vu MD,Yee C

更新日期：2013-05-01 00:00:00

abstract：:NAD(P)H-dependent oxidoreductases play important roles in biology. Recently, we reported that the luminescence lifetime of some Tb(3+) complexes is sensitive to NAD(P)H, and we used this phenomenon to detect activities of these enzymes. However, conventional time-resolved luminescence assays are susceptible to static ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Terai T,Ito H,Hanaoka K,Komatsu T,Ueno T,Nagano T,Urano Y

更新日期：2016-05-01 00:00:00

abstract：:The in vitro and in vivo activities of a series of (2R,3R)-2-(2,4-difluorophenyl)-3-(substituted indazol-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol as potential antifungal agents are described. In particular, the analog 12j having 5-bromo substitution on the indazole ring exhibited significant antifungal activity again...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park JS,Yu KA,Kang TH,Kim S,Suh YG

更新日期：2007-06-15 00:00:00

abstract：:Inhibitors of CYP1 enzymes may play vital roles in the prevention of cancer and overcoming chemo-resistance to anticancer drugs. In this letter, we report synthesis of twenty-three pyrrole based heterocyclic chalcones which were screened for inhibition of CYP1 isoforms. Compound 3n potently inhibited CYP1B1 with an IC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Williams IS,Joshi P,Gatchie L,Sharma M,Satti NK,Vishwakarma RA,Chaudhuri B,Bharate SB

更新日期：2017-08-15 00:00:00

abstract：:Three novel steroidal antiestrogen-geldanamycin conjugates were prepared using a convergent strategy. The antiestrogenic component utilized the 11β-(4-functionalized-oxyphenyl) estradiol scaffold, while the geldanamycin component was derived by replacement of the 17-methoxy group with an appropriately functionalized a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adam Hendricks J,Hanson RN,Amolins M,Mihelcic JM,Blagg BS

更新日期：2013-06-15 00:00:00

abstract：:We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses exceptional potency at MC4R and potent anti-obesity efficacy in a mouse model. However, the efficacy is not completely mediated through MC4R. Additional SAR studies le...

journal_title：Bioorganic & medicinal chemistry letters

authors： He S,Ye Z,Dobbelaar PH,Bakshi RK,Hong Q,Dellureficio JP,Sebhat IK,Guo L,Liu J,Jian T,Lai Y,Franklin CL,Reibarkh M,Holmes MA,Weinberg DH,MacNeil T,Tang R,Tamvakopoulos C,Peng Q,Miller RR,Stearns RA,Chen HY,Chen

更新日期：2010-11-15 00:00:00

abstract：:Human serum albumin (HSA) was shown to mediate oligoribonucleotide cleavage. Nonenzymatic glycation of HSA decreased the ribonuclease-like activity of the protein. According to (31)P NMR data, both native and glycated albumins induced hydrolysis of RNA molecule through 2',3'-cyclophosphate intermediates. A feasible me...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gerasimova YV,Erchenko IA,Shakirov MM,Godovikova TS

更新日期：2008-08-15 00:00:00

abstract：:Several imidazole-based cyclohexyl amides were identified as potent CB-1 antagonists, but they exhibited poor oral exposure in rodents. Incorporation of a hydroxyl moiety on the cyclohexyl ring provided a dramatic improvement in oral exposure, together with a ca. 10-fold decrease in potency. Further optimization provi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith RA,Fathi Z,Achebe F,Akuche C,Brown SE,Choi S,Fan J,Jenkins S,Kluender HC,Konkar A,Lavoie R,Mays R,Natoli J,O'Connor SJ,Ortiz AA,Su N,Taing C,Tomlinson S,Tritto T,Wang G,Wirtz SN,Wong W,Yang XF,Ying S,

更新日期：2007-05-15 00:00:00

abstract：:In continuation of our earlier work on benzothiadiazines, we have prepared a series of nitrofuran, nitrothiophene and arylfuran coupled benzothiadiazines and evaluated them for antimycobacterial and antibacterial activities. One of the compounds 2f has shown good in vitro antimycobacterial activity. All the synthesize...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Ahmed SK,Reddy KS,Khan MN,Shetty RV,Siddhardha B,Murthy US,Khan IA,Kumar M,Sharma S,Ram AB

更新日期：2007-10-01 00:00:00

abstract：:Two new oligostilbenes, caragasinins A (5) and B (10), and eight known compounds, kobophenol A (1), (+)-α-viniferin (2), (+)-ampelopsin F (3), pallidol (4), (+)-isoampelopsin F (6), miyabenol C (7), carasinaurone (8) and caraphenol B (9) were isolated from the ethylacetate-soluble extract of the roots of Caragana sini...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin Q,Han XH,Hong SS,Lee C,Choe S,Lee D,Kim Y,Hong JT,Lee MK,Hwang BY

更新日期：2012-01-15 00:00:00

abstract：:PTPases are considered to be involved in the etiology of diabetes mellitus and neural diseases, such as Alzheimer's disease and Parkinson's disease. Therefore, PTPase inhibitors should be useful tools to study the role of PTPases in these diseases and other biological phenomena, and which can be developed into chemoth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahmad G,Mishra PK,Gupta P,Yadav PP,Tiwari P,Tamrakar AK,Srivastava AK,Maurya R

更新日期：2006-04-15 00:00:00

abstract：:Proteases typically recognize their peptide substrates in extended conformations. General approaches for designing protease inhibitors often consist of peptidomimetics that feature this conformation. Herein we discuss a combination of computational and experimental studies to evaluate the potential of triazole-linked ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jochim AL,Miller SE,Angelo NG,Arora PS

更新日期：2009-11-01 00:00:00

abstract：:The synthesis and biological evaluation of novel antagonists of the rat H(3) receptor are described. These compounds differ from prototypical H(3) antagonists in that they do not contain an imidazole moiety, but rather a substituted aminopyrrolidine moiety. A systematic modification of the substituents on the aminopyr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vasudevan A,Conner SE,Gentles RG,Faghih R,Liu H,Dwight W,Ireland L,Kang CH,Esbenshade TA,Bennani YL,Hancock AA

更新日期：2002-11-04 00:00:00

abstract：:Structure-activity relationship studies directed toward improving the metabolic stability of compound 1 resulted in the identification of 3-[5-(3,5-difluorophenyl)-3-({[(1S,3R)-3-fluorocyclopentyl]amino}methyl)-4-methyl-1H-pyrazol-1-yl]propanenitrile 39 (MK-1925) as a selective, orally available and brain-penetrable o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kobayashi K,Tsujita T,Ito H,Ozaki S,Tani T,Ishii Y,Okuda S,Tadano K,Fukuroda T,Ohta H,Okamoto O

更新日期：2009-08-15 00:00:00

abstract：:A number of compounds bearing a quaternary ammonium moiety were found to be antagonists with nanomolar binding affinity for the chemokine receptor-2. The structure-activity relationships in the series are described herein along with some detailed characterization of the interesting compounds. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lagu B,Gerchak C,Pan M,Hou C,Singer M,Malaviya R,Matheis M,Olini G,Cavender D,Wachter M

更新日期：2007-08-01 00:00:00

abstract：:A number of analogues of the recently described compound nematophin were prepared and studied for antibacterial activity. The 2-phenyl derivative was found to exhibit exceptional activity against methicillin resistant Staphylococcus aureus (MRSA) whereas the isosteric benzimidazole analogue was much less active. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kennedy G,Viziano M,Winders JA,Cavallini P,Gevi M,Micheli F,Rodegher P,Seneci P,Zumerle A

更新日期：2000-08-07 00:00:00

abstract：:Substitution at the alpha center of the known human arginase inhibitor 2-amino-6-boronohexanoic acid (ABH) is acceptable in the active site pockets of both human arginase I and arginase II. In particular, substituents with a tertiary amine linked via a two carbon chain show improved inhibitory potency for both enzyme ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Golebiowski A,Paul Beckett R,Van Zandt M,Ji MK,Whitehouse D,Ryder TR,Jagdmann E,Andreoli M,Mazur A,Padmanilayam M,Cousido-Siah A,Mitschler A,Ruiz FX,Podjarny A,Schroeter H

更新日期：2013-04-01 00:00:00

abstract：:4,7-Dichloro-1-benzothien-2-yl sulfonylaminomethyl boronic acid (DSABA, Compound I) was discovered as the first boronic acid-based class D beta-lactamase inhibitor. It exhibited an IC(50) of 5.6 microM against OXA-40. The compound also inhibited class A and C beta-lactamases with sub to low microM IC(50), and synergiz...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tan Q,Ogawa AM,Painter RE,Park YW,Young K,DiNinno FP

更新日期：2010-04-15 00:00:00

abstract：:The X-ray crystallographic structure for the adduct of an activator with human carbonic anhydrase isozyme I (hCA I) is reported. L-Histidine binds deep within the enzyme active site, participating in a network of hydrogen bonds involving its carboxylate moiety and the zinc-bound water molecule, as well as the imidazol...

journal_title：Bioorganic & medicinal chemistry letters

authors： Temperini C,Scozzafava A,Supuran CT

更新日期：2006-10-01 00:00:00

abstract：:The halogenated and oxidized derivatives (1a-1e, 1a'-1c', 2a-2d, 2a'-2b', 3a-3e, 3' and 3a'-3b') of schizandrin (1), schizandrin B (2) and schisanhenol (3) were synthesized. The hepatoprotective effects of these dibenzocyclooctadiene lignan analogues against CCl4-induced injury were preliminarily evaluated. Most of th...

journal_title：Bioorganic & medicinal chemistry letters

authors： He T,Wang QY,Shi JZ,Fan TY,Yan C,Huang LJ,Liu S,Hao XJ,Mu SZ

更新日期：2014-04-01 00:00:00

abstract：:A series of novel tetracyclic core-containing HCV NS5A inhibitors has been discovered. Incorporation of tetrahydropyran-substituted amino acid moiety improved their potency and yielded HCV NS5A inhibitors with a minimum potency shift from the GT1a strain compared to other genotypes and mutants. Compounds 53 and 54 sho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yu W,Hu B,Zhong B,Hao J,Lei Z,Agrawal S,Rokosz L,Liu R,Chen S,Asante-Appiah E,Kozlowski JA

更新日期：2019-03-01 00:00:00

abstract：:A novel series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols, have been discovered by combining virtual and focused screening efforts with design techniques. Synthesis of the two diastereomeric isomers of the molecule followed by chiral resolution of each enantiomer revealed the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim CY,Mahaney PE,McConnell O,Zhang Y,Manas E,Ho DM,Deecher DC,Trybulski EJ

更新日期：2009-09-01 00:00:00

abstract：:Fibronectin contains the active sequence Arg-Gly-Asp (RGD), along with its synergic site Pro-His-Ser-Arg-Asn (PHSRN). However, the PHSRN peptide does not show synergic activity when it is mixed with the RGD peptide, indicating that a spatial array between RGD and PHSRN in fibronectin may be necessary for synergic acti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hojo K,Susuki Y,Maeda M,Okazaki I,Nomizu M,Kamada H,Yamamoto Y,Nakagawa S,Mayumi T,Kawasaki K

更新日期：2001-06-04 00:00:00

abstract：:Two new antiinflammatory macrolides, lobophorins A and B (1 and 2), have been isolated from fermentation broths of a marine bacterium isolated from the surface the Caribbean brown alga Lobophora variegata (Dictyotales). The new compounds, distantly related to antibiotics of the kijanimicin class, are potent inhibitors...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jiang ZD,Jensen PR,Fenical W

更新日期：1999-07-19 00:00:00

abstract：:Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha7 NNR...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li T,Bunnelle WH,Ryther KB,Anderson DJ,Malysz J,Helfrich R,Grønlien JH,Håkerud M,Peters D,Schrimpf MR,Gopalakrishnan M,Ji J

更新日期：2010-06-15 00:00:00

abstract：:A class of small molecules displaying comparable activities with peptide ligands BAM22 and corticostatin-14 at both the human and rhesus monkey MrgX1 and MrgX2 receptors, respectively, was discovered. A comparative study to compare solid-phase and solution-phase chemistries for the efficient synthesis of the active cl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Malik L,Kelly NM,Ma JN,Currier EA,Burstein ES,Olsson R

更新日期：2009-03-15 00:00:00

abstract：:Aminoglycosides have been shown to target A-form nucleic acids. Our work has previously shown that neomycin (and other aminoglycosides) bind and stabilize DNA/RNA triplexes and other A-form nucleic acids. We report herein the unexpected B-form duplex stabilization shown by aminoglycoside dimers (neomycin-neomycin and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arya DP,Coffee RL Jr,Xue L

更新日期：2004-09-20 00:00:00