Antitrypanosomal activity of epi-polygodial from Drimys brasiliensis and its effects in cellular membrane models at the air-water interface.

abstract：:Urease is an important enzyme which breaks urea into ammonia and carbon dioxide during metabolic processes. However, an elevated activity of urease causes various complications of clinical importance. The inhibition of urease activity with small molecules as inhibitors is an effective strategy for therapeutic interven...

journal_title：Bioorganic chemistry

authors： Hameed A,Khan KM,Zehra ST,Ahmed R,Shafiq Z,Bakht SM,Yaqub M,Hussain M,de la Vega de León A,Furtmann N,Bajorath J,Shad HA,Tahir MN,Iqbal J

更新日期：2015-08-01 00:00:00

abstract：:Hydrogen sulfide (H2S) is a biologically important gaseous molecule that exhibits promising protective effects against a variety of pathological processes. For example, it was recognized as a blood pressure lowering agent. Aligned with the need for easily modifiable platforms for the H2S supply, we report here the pre...

journal_title：Bioorganic chemistry

authors： Zaorska E,Hutsch T,Gawryś-Kopczyńska M,Ostaszewski R,Ufnal M,Koszelewski D

更新日期：2019-07-01 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：: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 4-imidazolylflavans having a variety of substituents on the 2-phenyl ring was synthesized and investigated for their inhibitory effect against aromatase. Structure-activity relationships of these compounds were determined. An additional chlorine atom or a cyano group at the 4' position did not enhance arom...

journal_title：Bioorganic chemistry

authors： Pouget C,Yahiaoui S,Fagnere C,Habrioux G,Chulia AJ

更新日期：2004-12-01 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：:The fruit of the white mulberry tree (Morus alba L.) is a multiple fruit with a sweet flavor commonly consumed around the world. Chemical investigation of the fruits led to the isolation of two indole acetic acid derivatives (1 -2) including a new compound, which turned out to be an isolation artifact, 3S-(β-D-glucopy...

journal_title：Bioorganic chemistry

authors： Yu JS,Lee D,Lee SR,Lee JW,Choi CI,Jang TS,Kang KS,Kim KH

更新日期：2018-02-01 00:00:00

abstract：:Novel ammonium and betaine derivatives of p-tert-butylthiacalix[4]arene in cone and 1,3-alternate conformation were synthesized with high yields for the first time. The obtained compounds form in water spherical nanoparticles. It was shown by molecular docking calculations and in vitro experiments that amino and betai...

journal_title：Bioorganic chemistry

authors： Padnya PL,Bayarashov EE,Zueva IV,Lushchekina SV,Lenina OA,Evtugyn VG,Osin YN,Petrov KA,Stoikov II

更新日期：2020-01-01 00:00:00

abstract：:A series of six novel and six known thieno[2,3-d]pyrimidin-4-amines 2-13 were synthesized, and further were used as a starting material for preparation of a small series of eight novel thieno[2,3-d]pyrimidin-4-phthalimides 14-21. Eight compounds, five amine and three phthalimide derivatives, inhibited bovine pancreati...

journal_title：Bioorganic chemistry

authors： Ts Mavrova A,Dimov S,Yancheva D,Kolarević A,Ilić BS,Kocić G,Šmelcerović A

更新日期：2018-10-01 00:00:00

abstract：:3-Amino-1-aryl-1H-benzo[f]chromene-2-carbonitrile derivatives were synthesized from three-component reaction of arylaldehyde, malononitrile and 2-naphthol in the presence of 1, 4-bis(4-ferrocenylbutyl)piperazine as a new catalyst. Cytotoxic potencies of the compounds were tested on HT-29 cells. 3-Amino-1-(4-fluorophen...

journal_title：Bioorganic chemistry

authors： Ahagh MH,Dehghan G,Mehdipour M,Teimuri-Mofrad R,Payami E,Sheibani N,Ghaffari M,Asadi M

更新日期：2019-12-01 00:00:00

abstract：:Analkali tolerant α-l-rhamnosidase has been purified to homogeneity from the culture filtrate of a new fungal strain, Fusarium moniliforme MTCC-2088, using concentration by ultrafiltration and cation exchange chromatography on CM cellulose column. The molecular mass of the purified enzyme has been found to be 36.0 kDa...

journal_title：Bioorganic chemistry

authors： Kumar D,Yadav S,Yadava S,Yadav KDS

更新日期：2019-03-01 00:00:00

abstract：:The fungus Mucor circinelloides exhibits high potential for green chemistry and technological applications. Recently M. circinelloides, which so far was considered mainly as a platform for biodiesel production, was found to exhibit high ene-reductase activity. In our current research we applied this promising microorg...

journal_title：Bioorganic chemistry

authors： Janicki I,Kiełbasiński P,Szeląg J,Głębski A,Szczęsna-Antczak M

更新日期：2020-03-01 00:00:00

abstract：:Succinimides are well recognized heterocyclic compounds in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Researches in medicinal chemistry field have isolated and synthesized succinimide derivatives with multiple medicinal properties including anticonvulsant, a...

journal_title：Bioorganic chemistry

authors： Zhao Z,Yue J,Ji X,Nian M,Kang K,Qiao H,Zheng X

更新日期：2020-12-15 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：:Alzheimer's Disease (AD) is a progressive neurodegenerative disorder that effects 50 million people worldwide. In this review, AD pathology and the development of novel therapeutic agents targeting AD were fully discussed. In particular, common approaches to prevent Aβ production and/or accumulation in the brain inclu...

journal_title：Bioorganic chemistry

authors： Iraji A,Khoshneviszadeh M,Firuzi O,Khoshneviszadeh M,Edraki N

更新日期：2020-04-01 00:00:00

abstract：:Aldose reductase (AR) catalyzes the NADPH-dependent reduction of glucose to sorbitol in the polyol pathway, which plays an important role in the development of diabetic complications including cataract, retinopathy, nephropathy, and neuropathy. AR has been considered as an important target to heal these long-term diab...

journal_title：Bioorganic chemistry

authors： Sever B,Altıntop MD,Demir Y,Akalın Çiftçi G,Beydemir Ş,Özdemir A

更新日期：2020-09-01 00:00:00

abstract：:Herein, we synthesized a series of twelve benzoxazole and benzothiazole derivatives incorporated with phthalimide core as anticancer agents. The most active compounds were 5a and 5g against HepG2 and MCF7 cell lines with IC50 = 0.011 and 0.006 μM, respectively. They evaluated against EGFR and HER2 enzymes. From cell c...

journal_title：Bioorganic chemistry

authors： Philoppes JN,Lamie PF

更新日期：2019-08-01 00:00:00

abstract：:A new series of triazolopyrimidines and thiazolopyrimidine hydrobromides was designed and prepared as topoisomerase II inhibitors. Screening of all synthesized compounds was carried out by the National Cancer Institute (NCI) of USA. Activity against 60 human cancer cell lines representing different cancer types was de...

journal_title：Bioorganic chemistry

authors： Nemr MTM,AboulMagd AM

更新日期：2020-10-01 00:00:00

abstract：:Convenient structures such as 2,4-diketo esters have been widely used as an effective pattern in medicinal chemistry and pharmacology for drug discovery. 2,4-Diketonate is a common scaffold that can be found in many biologically active and naturally occurring compounds. Also, many 2,4-diketo ester derivatives have bee...

journal_title：Bioorganic chemistry

authors： Joksimović N,Janković N,Davidović G,Bugarčić Z

更新日期：2020-12-01 00:00:00

abstract：:A new series of derivatives characterized by the presence of the 3,4,5-trimethoxylbenzamide substituted benzofurans were synthesized and evaluated for antiproliferative activity against four cancer cell lines and one normal human cell line. Among them, derivative 6g with greatest cytotoxicity significantly inhibited t...

journal_title：Bioorganic chemistry

authors： Li Q,Jian XE,Chen ZR,Chen L,Huo XS,Li ZH,You WW,Rao JJ,Zhao PL

更新日期：2020-09-01 00:00:00

abstract：:Inhibition of α-glucosidase is one of the important approaches in designing antidiabetic drugs for its role in decrease of the carbohydrates digestion to avoid post-prandial increase in blood sugar levels in diabetic patients. In the present study we designed a novel series of 2-acetylbenzofuran hydrazones (L1-L7) and...

journal_title：Bioorganic chemistry

authors： Khan S,Tariq M,Ashraf M,Abdullah S,Al-Rashida M,Khalid M,Taslimi P,Fatima M,Zafar R,Shafiq Z

更新日期：2020-09-01 00:00:00

abstract：:An E461G mutation of beta-galactosidase results in the disappearance of the high pL (L = H, D) downward break in the rate profiles for k(cat)/K(m) for wild-type enzyme-catalyzed hydrolysis of 4-nitrophenyl beta-D-galactopyranoside (Gal-OPNP) and a decrease from (k(cat))(HOH)/(k(cat))(DOD) = 1.7 to (k(cat))(HOH)/(k(cat...

journal_title：Bioorganic chemistry

authors： Richard JP,Huber RE,McCall DA

更新日期：2001-06-01 00:00:00

abstract：:Some derivatives containing pyrido[2,3-d:6,5d']dipyrimidine-4,5-diones (9a-f), tetrahydropyrido[2,3-d]pyrimidine-6-carbonitriles (11a-c) and 6-(4-acetylphenyl)-2-thioxo-2,3,5,6,7,8-hexahydro-1H-pyrimido[4,5-d]pyrimidin-4-one (12) were synthesized from 6-amino-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one (8). The anti-infla...

journal_title：Bioorganic chemistry

authors： Abdelgawad MA,Bakr RB,Azouz AA

更新日期：2018-04-01 00:00:00

abstract：:Carbamyl is considered a privileged structure in medicinal chemistry. It has a wide range of biological activities such as antimicrobial, anticancer, anti-epilepsy, for which the best evidence is a number of marketed carbamyl-containing drugs. Carbamyl is formed of primary amine and carbonyl moieties that act as hydro...

journal_title：Bioorganic chemistry

authors： Wang K,Zhu H,Zhao H,Zhang K,Tian Y

更新日期：2020-05-01 00:00:00

abstract：:A novel 1(2), 2(18)-diseco indole diterpenoid, drechmerin H (1), was isolated from the fermentation broth of Drechmeria sp. together with a new indole diterpenoid, 2'-epi terpendole A (3), and a known analogue, terpendole A (2). Their structures were determined by HRESIMS, 1D and 2D NMR, ECD, and X-ray single crystal ...

journal_title：Bioorganic chemistry

authors： Zhao JC,Luan ZL,Liang JH,Cheng ZB,Sun CP,Wang YL,Zhang MY,Zhang TY,Wang Y,Yang TM,Wu YY,Zhang YX,Zhao XY,Ma XC

更新日期：2018-09-01 00:00:00

abstract：:Acute lymphoblastic leukemia (ALL) or white blood cell cancer is one of the major causes that kills many children worldwide. Although various therapeutic agents are available for ALL treatment, the new drug discovery and drug delivery system are needed to improve their effectiveness, to reduce the toxicity and side-ef...

journal_title：Bioorganic chemistry

authors： Chittasupho C,Aonsri C,Imaram W

更新日期：2021-01-01 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：:Euphoroids A-C (1-3), three new ent-abietane-type diterpenoids, together with ten known analogues (4-13) were obtained from the roots of Euphorbia ebracteolata. The structures of these compounds were determined by extensive spectroscopic data analysis, including UV, HRESIMS, 1D-, and 2D-NMR data. The inhibitory effect...

journal_title：Bioorganic chemistry

authors： Han C,Peng Y,Wang Y,Huo X,Zhang B,Li D,Leng A,Zhang H,Ma X,Wang C

更新日期：2018-12-01 00:00:00

abstract：:In this study, a series of B-ring fluoro substituted bis-chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and evaluated for their ability to inhibit xanthine oxidase (XO) and growth inhibitory activity against MCF-7 and Caco-2 human cancer cell lines, in vitro. According to the results o...

journal_title：Bioorganic chemistry

authors： Burmaoglu S,Ozcan S,Balcioglu S,Gencel M,Noma SAA,Essiz S,Ates B,Algul O

更新日期：2019-10-01 00:00:00

abstract：:The stilbenoid resveratrol (1) was subjected to regioselective acetylation catalysed by Candida antarctica lipase (CAL) to obtain 4'-acetylresveratrol (2). CAL biocatalysed regioselective alcoholysis of 3,5,4'-triacetylresveratrol (3), 3,5,4'-tributanoylresveratrol (6), and 3, 4, 5'-trioctanoylresveratrol (9) afforded...

journal_title：Bioorganic chemistry

authors： Cardile V,Lombardo L,Spatafora C,Tringali C

更新日期：2005-02-01 00:00:00