Five-coordinated oxovanadium(IV) complexes derived from amino acids and ciprofloxacin: synthesis, spectral, antimicrobial, and DNA interaction approach.


:Five-coordinated oxovanadium(IV) complexes with ciprofloxacin and various uninegative bidentate amino acids have been prepared. The structure of complexes has been investigated using spectral, physicochemical, mass spectroscopy, and elemental analyses. The antimicrobial activities (MIC) of the complexes, ligands, metal salt, and some standard drugs have been evaluated using the doubling dilution technique against Staphylococcus aureus, Bacillus subtilis, Serratia marcescens (gram-positive), and Pseudomonas aeruginosa, and Escherichia coli (gram-negative) bacteria. The result shows the significant increase in the antibacterial activity of the ligand, metal, and ciprofloxacin on complexation. The interaction of the complexes with pBR322 DNA has been investigated using spectroscopic, gel electrophoresis, and viscometric techniques. This shows that the complexes can bind to pBR322 DNA by the intercalative mode. The superoxide dismutase-like activity of the complexes has been determined.


Bioorg Med Chem Lett


Patel MN,Patel SH,Chhasatia MR,Parmar PA




Has Abstract


2008-12-15 00:00:00














  • Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists.

    abstract::Novel CCR2 antagonists with a novel 2-aminooctahydrocyclopentalene-3a-carboxamide scaffold were designed. SAR studies led to a series of potent compounds. For example, compound 51 had a good PK profile in both dog and monkey, and exhibited excellent efficacy when dosed orally in an inflammation model in hCCR2 KI mice....

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Cai C,Kang FA,Hou C,O'Neill JC,Opas E,McKenney S,Johnson D,Sui Z

    更新日期:2013-01-01 00:00:00

  • Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.

    abstract::Optimisation of affinity, chemical stability, metabolic stability and solubility led from a chemically labile HTS hit 1 to mGlu5 receptor antagonists (24-26) with high affinity for the allosteric MPEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel co...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Büttelmann B,Peters JU,Ceccarelli S,Kolczewski S,Vieira E,Prinssen EP,Spooren W,Schuler F,Huwyler J,Porter RH,Jaeschke G

    更新日期:2006-04-01 00:00:00

  • Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.

    abstract::The synthesis and structure-activity relationship (SAR) study of a novel series of N-type calcium channel blockers are described. L-Cysteine derivative 2a was found to be a potent and selective N-type calcium channel blocker with IC(50) 0.63 microM on IMR-32 assay. Compound 2a showed analgesic efficacy in the rat form...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Seko T,Kato M,Kohno H,Ono S,Hashimura K,Takimizu H,Nakai K,Maegawa H,Katsube N,Toda M

    更新日期:2001-08-20 00:00:00

  • Synthesis of H-bonding probes of alpha7 nAChR agonist selectivity.

    abstract::The alpha7 subtype of the nicotinic acetylcholine receptor (nAChR) is the target of studies aimed at identifying features that will lead to the development of selective therapeutics. Five arylidine anabaseines, three with pyridine rings and two with the pyrrole rings, were synthesized in 35-65% yield via aldol condens...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wang J,Papke RL,Horenstein NA

    更新日期:2009-01-15 00:00:00

  • Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.

    abstract::Highly selective orexin receptor antagonists (SORAs) of the orexin 2 receptor (OX2R) have become attractive targets both as potential therapeutics for insomnia as well as biological tools to help further elucidate the underlying pharmacology of the orexin signaling pathway. Herein, we describe the discovery of a novel...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Raheem IT,Breslin MJ,Bruno J,Cabalu TD,Cooke A,Cox CD,Cui D,Garson S,Gotter AL,Fox SV,Harrell CM,Kuduk SD,Lemaire W,Prueksaritanont T,Renger JJ,Stump C,Tannenbaum PL,Williams PD,Winrow CJ,Coleman PJ

    更新日期:2015-02-01 00:00:00

  • Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.

    abstract::Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X(7) receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X(7) receptor in both human and rodent. Compound (entry 31) exhibited oral efficacy...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Matasi JJ,Brumfield S,Tulshian D,Czarnecki M,Greenlee W,Garlisi CG,Qiu H,Devito K,Chen SC,Sun Y,Bertorelli R,Geiss W,Le VD,Martin GS,Vellekoop SA,Haber J,Allard ML

    更新日期:2011-06-15 00:00:00

  • A hit deconstruction approach for the discovery of fetal hemoglobin inducers.

    abstract::Beta-hemoglobinopathies such as sickle cell disease represent a major global unmet medical need. De-repression of fetal hemoglobin in erythrocytes is a clinically validated approach for the management of sickle cell disease, but the only FDA-approved medicine for this purpose has limitations to its use. We conducted a...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Benowitz AB,Eberl HC,Erickson-Miller CL,Gilmartin AG,Gore ER,Montoute MN,Wu Z

    更新日期:2018-12-15 00:00:00

  • Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors.

    abstract::The diacylglycerol acyltransferase enzyme, DGAT1, presents itself as a potential target for obesity as this enzyme is dedicated to the final committed step in triglyceride biosynthesis. Biphenyl ureas, exemplified by compound 4, have been reported to be potent hDGAT1 inhibitors. We have synthesized and evaluated 2-pyr...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Motiwala H,Kandre S,Birar V,Kadam KS,Rodge A,Jadhav RD,Mahesh Kumar Reddy M,Brahma MK,Deshmukh NJ,Dixit A,Doshi L,Gupte A,Gangopadhyay AK,Vishwakarma RA,Srinivasan S,Sharma M,Nemmani KV,Sharma R

    更新日期:2011-10-01 00:00:00

  • Synthesis and α-Glucosidase II inhibitory activity of valienamine pseudodisaccharides relevant to N-glycan biosynthesis.

    abstract::Valienol-derived allylic C-1 bromides have been used as carbaglycosyl donors for α-xylo configured valienamine pseudodisaccharide synthesis. We synthesised valienamine analogues of the Glc(α1→3)Glc and Glc(α1→3)Man disaccharides representing the linkages cleaved by α-Glucosidase II in N-glycan biosynthesis. These (N1→...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Cumpstey I,Ramstadius C,Eszter Borbas K,Alonzi DS,Butters TD

    更新日期:2011-09-15 00:00:00

  • New triple-helix DNA stabilizing agents.

    abstract::Several substituted quinolin-4-amines and heteroaromatic analogs were synthesized and evaluated for interaction with triplex polydA.2polydT and duplex polydA.polydT by using UV-thermal melting experiments. Excellent triple-helix DNA ligands with high affinity toward T.A.T triplets and triple/duplex selectivity were de...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Strekowski L,Hojjat M,Wolinska E,Parker AN,Paliakov E,Gorecki T,Tanious FA,Wilson WD

    更新日期:2005-02-15 00:00:00

  • Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.

    abstract::A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Skerlj R,Bridger G,Zhou Y,Bourque E,McEachern E,Langille J,Harwig C,Veale D,Yang W,Li T,Zhu Y,Bey M,Baird I,Sartori M,Metz M,Mosi R,Nelson K,Bodart V,Wong R,Fricker S,Mac Farland R,Huskens D,Schols D

    更新日期:2011-12-01 00:00:00

  • Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors.

    abstract::A co-crystal structure of amide-containing compound (4) in complex with the nicotinamide phosphoribosyltransferase (Nampt) protein and molecular modeling were utilized to design and discover a potent novel cyanoguanidine-containing inhibitor bearing a sulfone moiety (5, Nampt Biochemical IC50=2.5nM, A2780 cell prolife...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Zheng X,Baumeister T,Buckmelter AJ,Caligiuri M,Clodfelter KH,Han B,Ho YC,Kley N,Lin J,Reynolds DJ,Sharma G,Smith CC,Wang Z,Dragovich PS,Oh A,Wang W,Zak M,Wang Y,Yuen PW,Bair KW

    更新日期:2014-01-01 00:00:00

  • trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.

    abstract::Inhibition of the aspartyl protease renin is considered as an efficient approach for treating hypertension. Lately, we described the discovery of a novel class of direct renin inhibitors which comprised a pyrrolidine scaffold (e.g., 2). Based on the X-ray structure of the lead compound 2 bound to renin we predicted th...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Sellner H,Cottens S,Cumin F,Ehrhardt C,Kosaka T,Lorthiois E,Ostermann N,Webb RL,Rigel DF,Wagner T,Maibaum J

    更新日期:2015-04-15 00:00:00

  • Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL.

    abstract::The existence of drug resistance caused by mutations in the break-point cluster region-Abelson (BCR-ABL) tyrosine kinase domain remains a clinical challenge due to limited treatment options for effective CML therapies. Here, we report a series of flavone-based common inhibitors equipotent for the wild type and the mos...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Choe H,Kim J,Hong S

    更新日期:2013-08-01 00:00:00

  • Structure activity relationship and optimization of N-(3-(2-aminothiazol-4-yl)aryl)benzenesulfonamides as anti-cancer compounds against sensitive and resistant cells.

    abstract::We recently described a new family of bioactive molecules with interesting anti-cancer activities: the N-(4-(3-aminophenyl)thiazol-2-yl)acetamides. The lead compound of the series (1) displays significant anti-proliferative and cytotoxic activities against a panel of cancer cell lines, either sensitive or resistant to...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Ronco C,Millet A,Plaisant M,Abbe P,Hamouda-Tekaya N,Rocchi S,Benhida R

    更新日期:2017-05-15 00:00:00

  • Induction of apoptosis and differentiation by atractylenolide-1 isolated from Atractylodes macrocephala in human leukemia cells.

    abstract::Atractylodes macrocephula Koidz (A. macrocephula, also known as Baizhu) is an important ingredient in several traditional Chinese herb complexes for the treatment of abdominal pain and gastroenterology diseases for thousands of years. We previously demonstrated the induction of ROS-mediated apoptosis by methanol extra...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Huang HL,Lin TW,Huang YL,Huang RL

    更新日期:2016-04-15 00:00:00

  • The purine transferase from Trypanosoma cruzi as a potential target for bisphosphonate-based chemotherapeutic compounds.

    abstract::We identified and tested bisphosphonates as inhibitors of a protozoan molecular target. Computational modeling studies demonstrated that these compounds are mimics of the natural substrate of the enzyme. The most potent bisphosphonates in vitro are pamidronate and risedronate, which inhibit the purine transferase from...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Fernández D,Wenck MA,Craig SP 3rd,Delfino JM

    更新日期:2004-09-06 00:00:00

  • Novel, druglike 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine-based selective inhibitors of human neuronal nitric oxide synthase (nNOS).

    abstract::A novel class of 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine derivatives was designed, synthesized and evaluated as human nitric oxide synthase (NOS) inhibitors. Structure-activity relationship studies based on various basic amine side chains attached at the 1-position of the 2,3,4,5-tetrahydro-1H-benzo[b]...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Annedi SC,Ramnauth J,Cossette M,Maddaford SP,Dove P,Rakhit S,Andrews JS,Porreca F

    更新日期:2012-04-01 00:00:00

  • In vitro evolution of an HIV integrase binding protein from a library of C-terminal domain γS-crystallin variants.

    abstract::A protein without natural binding functions was engineered to bind HIV-1 integrase. Phage display selections applied a library of variants based on the C-terminal domain of the eye lens protein human γS-crystallin. Multiple loop regions were altered to encode libraries with ≈3.6 × 10(11) different variants. A crystall...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Moody IS,Verde SC,Overstreet CM,Edward Robinson W Jr,Weiss GA

    更新日期:2012-09-01 00:00:00

  • Synthesis and antitumor activity of leinamycin derivatives: modifications of C-8 hydroxy and C-9 keto groups.

    abstract::A series of leinamycin derivatives were synthesized and evaluated for antitumor activity. Modifications at C-8 and C-9 positions revealed a broad structure-activity relationship in vitro and some derivatives showed potent antiproliferative activity against HeLa S3 cells. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Kanda Y,Ashizawa T,Saitoh Y,Saito H,Gomi K,Okabe M

    更新日期:1998-04-21 00:00:00

  • Synthesis and Vasorelaxant Evaluation of Novel 7-Methoxyl-2,3-disubstituted-quinoxaline Derivatives.

    abstract::An array of novel 7-methoxyl-2,3-disubstituted quinoxaline derivatives was designed, synthesized and their potential antihypertensive activities were examined, in an attempt to discover potent small molecules with vasorelaxant effects. The vasoactivities of these compounds on vascular tone, as well as underlying mecha...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Zheng CB,Gao WC,Pang PP,Ma X,Peng LC,Yang L,Li X

    更新日期:2021-01-11 00:00:00

  • Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands.

    abstract::New carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives were designed and synthesized as potential positron emission tomography AMPA (2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid) receptor ligands to image brain diseases. The single crystal structure ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Gao M,Kong D,Clearfield A,Zheng QH

    更新日期:2006-04-15 00:00:00

  • N-Heteroaryl glycinamides and glycinamines as potent NPY5 antagonists.

    abstract::Subtype specific ligands are needed to evaluate the therapeutic potential of modulating the brain's neuropeptide Y system. The benzothiazepine glycinamide 1a was identified as an NPY5 antagonist lead. While having acceptable solubility, the compound was found to suffer from high clearance and poor exposure. Optimizati...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wu L,Lu K,Desai M,Packiarajan M,Joshi A,Marzabadi MR,Jubian V,Andersen K,Chandrasena G,Boyle NJ,Walker MW

    更新日期:2011-09-15 00:00:00

  • Rapid 'one-pot' synthesis of a novel benzimidazole-5-carboxylate and its hydrazone derivatives as potential anti-inflammatory and antimicrobial agents.

    abstract::A novel series of N-arylidene-2-(2,4-dichloro phenyl)-1-propyl-1H-benzo[d] imidazole-5-carbohydrazides having different substitution on the arylidene part were synthesized in good yield. The core nucleus benzimidazole-5-carboxylate (5) was efficiently synthesized by 'one-pot' nitro reductive cyclization reaction betwe...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Vasantha K,Basavarajaswamy G,Vaishali Rai M,Boja P,Pai VR,Shruthi N,Bhat M

    更新日期:2015-04-01 00:00:00

  • Discovery of a 6-(pyridin-3-yl)benzo[d]thiazole template for optimization of hedgehog and PI3K/AKT/mTOR dual inhibitors.

    abstract::Vismodegib is the first FDA approved cancer therapy based on inhibition of aberrant hedgehog signaling. Like most cancer therapies, vismodegib suffered from resistance, even during clinical development. Numerous reports demonstrated that simultaneous blockage of hedgehog and PI3K/AKT/mTOR pathways resulted in signific...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Yang Z,Ma H,Sun Z,Luo L,Tian S,Zheng J,Zhang X

    更新日期:2015-09-01 00:00:00

  • Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.

    abstract::The structure-activity relationships of 5,6-positions of aminopyridine carboxamide-based c-Jun N-terminal Kinase (JNK) inhibitors were explored to expand interaction with the kinase specificity and ribose-binding pockets. The syntheses of analogues and the impact of structural modification on in vitro potency and cell...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Liu G,Zhao H,Liu B,Xin Z,Liu M,Kosogof C,Szczepankiewicz BG,Wang S,Clampit JE,Gum RJ,Haasch DL,Trevillyan JM,Sham HL

    更新日期:2006-11-15 00:00:00

  • Synthesis and biological evaluation of L- and D-configuration 1,3-dioxolane 5-azacytosine and 6-azathymine nucleosides.

    abstract::Novel L- and D-configuration dioxolane 5-azacytosine and 6-azathymine nucleosides have been synthesized and evaluated for biological activity. (-)-(2S,4S)-1-[2-(Hydroxymethyl)-1,3-dioxolan-4-yl]-5-azacytosine (6) showed significant activity against HBV, whereas the D-configuration analogue (14) has been found to exhib...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Luo MZ,Liu MC,Mozdziesz DE,Lin TS,Dutschman GE,Gullen EA,Cheng YC,Sartorelli AC

    更新日期:2000-09-18 00:00:00

  • Discovery of a potent and selective adenylyl cyclase type 8 agonist by docking-based virtual screening.

    abstract::Adenylyl cyclases (ACs), which are responsible for catalyzing the conversion of adenosine triphosphate (ATP) into the second messenger cyclic adenosine monophosphate (cAMP), play a critical role in cell signal transduction. In this study, a combined approach involving docking-based virtual screening, with the combinat...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Weng Z,Xu G,Chen D,Yang Y,Song G,Shen W,Zhang S,Wang L,Yang W,Zuo Z

    更新日期:2020-01-15 00:00:00

  • d(TGGGAG) with 5'-nucleobase-attached large hydrophobic groups as potent inhibitors for HIV-1 envelop proteins mediated cell-cell fusion.

    abstract::The Hotoda's sequence substituted with TBDPS via 5'-end nucleobase existed as parallel quadruplex structure and exhibited inhibitory activities in an HIV-1 envelop proteins mediated cell-cell fusion assay. This result demonstrated that the 5'-aromatic groups of the Hotoda's sequence are allowed to have a large spatial...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Chen W,Xu L,Cai L,Zheng B,Wang K,He J,Liu K

    更新日期:2011-10-01 00:00:00

  • Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.

    abstract::Compound 2 was previously identified as a potent inhibitor of factor XIa lacking oral bioavailability. A structure-based approach was used to design analogs of 2 with novel P1 moieties with good selectivity profiles and oral bioavailability. Further optimization of the P1 group led to the identification of a 4-chlorop...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Pinto DJ,Smallheer JM,Corte JR,Austin EJ,Wang C,Fang T,Smith LM 2nd,Rossi KA,Rendina AR,Bozarth JM,Zhang G,Wei A,Ramamurthy V,Sheriff S,Myers JE Jr,Morin PE,Luettgen JM,Seiffert DA,Quan ML,Wexler RR

    更新日期:2015-04-01 00:00:00