Novel Linezolid analogues with antiparasitic activity against Hymenolepis nana.

abstract：:The marine environment remains a rich source for the discovery and development of novel bioactive compounds. The present paper describes the design, synthesis and biological evaluation of a library of small molecule heterocyclic mimetics of the marine 2,5-diketopiperazine barettin which is a powerful natural antioxida...

journal_title：Bioorganic chemistry

authors： Labrière C,Andersen JH,Albrigtsen M,Hansen JH,Svenson J

更新日期：2019-03-01 00:00:00

abstract：:Several novel N-substituted N-nitrosohydroxylamines were synthesized. They all inhibited mushroom tyrosinase, but the type of inhibition was different depending on the substituent. Some N-(mono- or dihydroxybenzyl)-N-nitrosohydroxylamines exhibited uncompetitive inhibition with respect to L-dopa. Among them, compound ...

journal_title：Bioorganic chemistry

authors： Shiino M,Watanabe Y,Umezawa K

更新日期：2003-04-01 00:00:00

abstract：:A series of bis-indolone-N-oxides, 1a-f, was prepared from bis(ethynyl)benzenes and o-halonitroaryls and studied for their in vitro antiplasmodial activities against Plasmodium falciparum and representative strains of bacteria and candida as well as for their cytotoxicity against a human tumor cell line (MCF7). They d...

journal_title：Bioorganic chemistry

authors： Najahi E,Valentin A,Téné N,Treilhou M,Nepveu F

更新日期：2013-06-01 00:00:00

abstract：:Simple biomembrane models, namely micellar aggregates formed by enantiopure sodium N-acylprolinates, are able to convert the racemic mixture of bilirubin-IXalpha into an enantiomerically enriched mixture, thus suggesting a possible role of chirality in bilirubin toxicity due to the perturbation of neuron membrane dyna...

journal_title：Bioorganic chemistry

authors： Ceccacci F,Giansanti L,Mortera SL,Mancini G,Sorrenti A,Villani C

更新日期：2008-10-01 00:00:00

abstract：:The relationship between structure and activity of insect oostatic decapeptide (Aed-TMOF) analogues in flesh fly was analyzed. The highest oostatic activity was exhibited by the pentapetide and tetrapeptide analogues, H-Tyr-Asp-Pro-Ala-Pro-OH and H-Tyr-Asp-Pro-Ala-OH, respectively. The tetrapeptide, either native or t...

journal_title：Bioorganic chemistry

authors： Slaninová J,Bennettová B,Nazarov ES,Simek P,Holík J,Vlasáková V,Hlavácek J,Cerný B,Tykva R

更新日期：2004-08-01 00:00:00

abstract：:It has been found that alpha-effects in nucleophilic reactions, unexpectedly large nucleophilicity due to adjacent unpaired electrons, are strongly dependent on the structure of substrate. The nucleophilic cleavages of 4-nitrobenzoate esters and 4-methylbenzoate esters by HOO- have been systematically investigated in ...

journal_title：Bioorganic chemistry

authors： Nomura Y,Kubozono T,Hidaka M,Horibe M,Mizushima N,Yamamoto N,Takahashi T,Komiyama M

更新日期：2004-02-01 00:00:00

abstract：:Building on the conclusions of previous inhibition studies with pyridinium-benzenesulfonamides from our team and on the X-ray crystal structure of the lead compound identified, a series of 24 pyridinium derivatives of 3-aminobenzenesulfonamide was synthesized and investigated for carbonic anhydrase inhibition. The new...

journal_title：Bioorganic chemistry

authors： Akocak S,Güzel-Akdemir Ö,Kishore Kumar Sanku R,Russom SS,Iorga BI,Supuran CT,Ilies MA

更新日期：2020-10-01 00:00:00

abstract：:A series of benzimidazole-oxindole conjugates were synthesized and evaluated for their cytotoxic activity. The cytotoxicity assay results suggest that conjugates 5c and 5p exhibit promising cytotoxicity against human breast cancer cell line (MCF-7). The Cell cycle analysis revealed that these conjugates induced cell c...

journal_title：Bioorganic chemistry

authors： Kamal A,Nagaseshadri B,Nayak VL,Srinivasulu V,Sathish M,Kapure JS,Suresh Reddy C

更新日期：2015-12-01 00:00:00

abstract：:A series of novel 2-Amino-4-Methylthiazole analogs were developed via three-step reaction encompassing hydrazine-1-carboximidamide motif to combat Gram-positive and Gram-negative bacterial and fungal infections. Noticeably, the thiazole-carboximidamide derivatives 4a-d displayed excellent antimicrobial activity and th...

journal_title：Bioorganic chemistry

authors： Omar AM,Ihmaid S,Habib EE,Althagfan SS,Ahmed S,Abulkhair HS,Ahmed HEA

更新日期：2020-06-01 00:00:00

abstract：:Natural antioxidants and vitamins have potential to protect biological systems from peroxidative damage induced by peroxyl radicals, α-tocopherol (Vitamin E, lipid soluble) and ascorbic acid (vitamin C, water soluble), well known natural antioxidant molecules. In the present study we described the synthesis and biolog...

journal_title：Bioorganic chemistry

authors： Muripiti V,Brijesh L,Rachamalla HK,Marepally SK,Banerjee R,Patri SV

更新日期：2019-02-01 00:00:00

abstract：:In this study, we prepared a novel amino cellulose derivative (benzyl cellulose-g-poly [2-(N,N-Dimethylamino)ethyl methacrylate]) via a homogeneous ATRP method. The successful synthesis of the novel amino cellulose was confirmed by FT-IR and 1H NMR. This study addressed the different characteristics of the prepared po...

journal_title：Bioorganic chemistry

authors： Shokri M,Moradi S,Amini S,Shahlaei M,Seidi F,Saedi S

更新日期：2021-01-01 00:00:00

abstract：:Phosphatidylinositol 3-kinase (PI3K) pathway regulates various cellular processes, such as proliferation, growth, autophagy and apoptosis. Class I PI3K is frequently mutated and overexpressed in a lot of human cancers and PI3K was considered as a target for therapeutic treatment of cancer. In this study, we designed a...

journal_title：Bioorganic chemistry

authors： Ding HW,Yu L,Bai MX,Qin XC,Song MT,Zhao QC

更新日期：2019-12-01 00:00:00

abstract：:A series of new N-acyl 8,9-dihydro-4-methoxy-7H-2-benzo[de]quinolinalkanamines have been prepared and tested for their ability to activate pigment granule aggregation in Xenopus laevis melanophores and bind to the recombinant human MT(1) and MT(2) melatonin receptor subtypes expressed in NIH 3T3 cells. Compounds with ...

journal_title：Bioorganic chemistry

authors： Tsotinis A,Eleutheriades A,Hough KA,Davidson K,Sugden D

更新日期：2007-04-01 00:00:00

abstract：:A facile synthetic strategy has been developed for the generation of structurally diverse N-fused heterocycles. The formation of fused 1,2,3-triazole indolo and pyrrolodiazepines proceeds through an initial Knoevenagel condensation followed by intramolecular azide-alkyne cycloaddition reaction at room temperature with...

journal_title：Bioorganic chemistry

authors： Gour J,Gatadi S,Pooladanda V,Ghouse SM,Malasala S,Madhavi YV,Godugu C,Nanduri S

更新日期：2019-12-01 00:00:00

abstract：:The inhibition of viral targets might provide new therapies for coronavirus disease abbreviated as COVID-19. The rational drug design identified as much of the recent discoveries of potent drugs molecule against any targets. This results in an improvement in bindings for better potency and selectivity. The drugs conta...

journal_title：Bioorganic chemistry

authors： Jawaid Akhtar M

更新日期：2020-08-01 00:00:00

abstract：:The galactofuranose moiety found in many surface constituents of microorganisms is derived from UDP-D-galactopyranose (UDP-Galp) via a unique ring contraction reaction catalyzed by a FAD-dependent UDP-Galp mutase. When the enzyme is reduced by sodium dithionite, its catalytic efficiency increases significantly. Since ...

journal_title：Bioorganic chemistry

authors： Huang Z,Zhang Q,Liu HW

更新日期：2003-12-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA), a type II membrane glycoprotein, is considered an excellent target for the diagnosis or treatment of prostate cancer. We previously investigated the effect of β- and γ-amino acids with (S)- or (R)-configuration in the S1 pocket on the binding affinity for PSMA. However, compr...

journal_title：Bioorganic chemistry

authors： Kwon H,Lim H,Ha H,Choi D,Son SH,Nam H,Minn I,Byun Y

更新日期：2020-11-01 00:00:00

abstract：:In continuation of our previous work on the investigation of CDK9 inhibitors bearing indole moiety for the discovery of novel anticancer agents, novel methylenehydrazine-1-carboxamide derivatives with (5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-indole scaffold were designed, synthesized, and evaluated for the CDK9 i...

journal_title：Bioorganic chemistry

authors： Hu H,Wu J,Ao M,Zhou X,Li B,Cui Z,Wu T,Wang L,Xue Y,Wu Z,Fang M

更新日期：2020-09-01 00:00:00

abstract：:There is much interest in the use of phytoestrogens such as coumestrol in breast cancer intervention due to their antiestrogenic activity and multiple modes of tumor cell death. However, the clear beneficial effects of naturally occurring estrogen mimetic coumestrol remain controversial due to experimental evidence th...

journal_title：Bioorganic chemistry

authors： Luo G,Tang Z,Li X,Hou Q,Chen Y,Lao K,Xiang H

更新日期：2019-04-01 00:00:00

abstract：:A novel series of homonucleosides and their double-headed analogs containing theophylline, 1,3,4-oxadiazole, and variant nucleobases was designed and synthesized. The new derivatives were fully characterized by HRMS, FT-IR, 1H NMR, and 13C NMR. The cytotoxic activities of all prepared compounds were screened in vitro ...

journal_title：Bioorganic chemistry

authors： El Mansouri AE,Oubella A,Mehdi A,AitItto MY,Zahouily M,Morjani H,Lazrek HB

更新日期：2020-12-15 00:00:00

abstract：:Novel lead compounds as anticancer agents with the ability to circumvent emerging drug resistance have recently gained a great deal of interest. Thiazolidinones are among such compounds with well-established biological activity in the field of oncology. Here, we designed, synthesized and characterized a series of thia...

journal_title：Bioorganic chemistry

authors： Tahmasvand R,Bayat P,Vahdaniparast SM,Dehghani S,Kooshafar Z,Khaleghi S,Almasirad A,Salimi M

更新日期：2020-11-01 00:00:00

abstract：:The chemical investigation of the fruits of a mangrove Sonneratia apetala collected from the Beibu Gulf led to the isolation of four new compounds, sonneradons A-D (1-4), as well as 18 known compounds (5-22). The structures of the new compounds were elucidated based on extensive spectroscopic analysis, and the structu...

journal_title：Bioorganic chemistry

authors： Yi X,Jiang S,Qin M,Liu K,Cao P,Chen S,Deng J,Gao C

更新日期：2020-06-01 00:00:00

abstract：:Lambertellin (1) and ergosta-5,7,22-trien-3-ol (2) were isolated from the solid rice fermentation of the plant pathogenic fungus Pycnoporus sanguineus MUCL 51321. Their structures were elucidated using comprehensive spectroscopic methods. The isolated compounds were tested on lipopolysaccharide (LPS)-stimulated RAW 26...

journal_title：Bioorganic chemistry

authors： Jouda JB,Mfotie Njoya E,Mbazoa CD,Zhou Z,Meli Lannang A,Wandji J,Shiono Y,Wang F

更新日期：2018-10-01 00:00:00

abstract：:We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4(3H)-quinazolinon-2-yl)thio]anilide derivatives (2-16) and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and acute myeloid leukemia (HL-60 and K562) cells. To reveal their selectivity toward canc...

journal_title：Bioorganic chemistry

authors： Alkahtani HM,Abdalla AN,Obaidullah AJ,Alanazi MM,Almehizia AA,Alanazi MG,Ahmed AY,Alwassil OI,Darwish HW,Abdel-Aziz AA,El-Azab AS

更新日期：2020-01-01 00:00:00

abstract：:A series of iminothiazolines (4a-j) featuring 2,4,5-trichlorophenyl moiety and aroyl/heteroaroyl substituents has been prepared from readily accessible thioureas. In-vitro screening against glucosidase enzymes showed highly specific inhibition of α-glucosidase with a marked dependence of the potency upon the nature of...

journal_title：Bioorganic chemistry

authors： Kazmi M,Zaib S,Amjad ST,Khan I,Ibrar A,Saeed A,Iqbal J

更新日期：2017-10-01 00:00:00

abstract：:Five new maleimide derivatives, (+)- and (-)- farinomalein F (1), (+)- and (-)- farinomalein G (2), farinomalein H (3) and one new linearly fused prenylated indole alkaloid phomoamide (8), along with five known compounds 4-7 and 9 were isolated from the mangrove endophytic fungus Phomopsis sp. SYSUQYP-23. Their struct...

journal_title：Bioorganic chemistry

authors： Chen Y,Zhang L,Zou G,Li C,Yang W,Liu H,She Z

更新日期：2020-04-01 00:00:00

abstract：:Cyclooxygenase-2 is one of the prominent enzymes to cause an increased production of prostaglandins during inflammation and immune responses. Cyclooxygenase-2 expression is up-regulated in inflammatory conditions owing to the induction by different inflammatory stimuli including cytokines, and therefore, the expressio...

journal_title：Bioorganic chemistry

authors： Chakraborty K,Francis P

更新日期：2020-10-01 00:00:00

abstract：:Chemical investigation of the roots of Croton crassifolius led to the isolation of five pyran-2-one derivatives, including two brand new compounds (1-2), one new natural product (3) and two known compounds (4-5). Their structures and absolute configurations were established by spectroscopic analyses as well as compari...

journal_title：Bioorganic chemistry

authors： Tian JL,Yao GD,Zhang YY,Lin B,Zhang Y,Li LZ,Huang XX,Song SJ

更新日期：2018-09-01 00:00:00

abstract：:Colchicine site antimitotic agents typically suffer from low aqueous solubilities and are formulated as phosphate prodrugs of phenolic groups. These hydroxyl groups are the aim of metabolic transformations leading to resistance. There is an urgent need for more intrinsically soluble analogues lacking these hydroxyl gr...

journal_title：Bioorganic chemistry

authors： Álvarez R,Aramburu L,Gajate C,Vicente-Blázquez A,Mollinedo F,Medarde M,Peláez R

更新日期：2020-05-01 00:00:00

abstract：:A series of thirteen novel 2,4-thiazolidinedione derivatives were synthesized through three step reaction procedure. The title compounds were synthesized by Knoevenagel condensation at the 5th position of the 2,4-thiazolidinedione ring. Various physicochemical and spectral studies were conducted to characterize the sy...

journal_title：Bioorganic chemistry

authors： Ranjan Srivastava A,Bhatia R,Chawla P

更新日期：2019-08-01 00:00:00