- Pharmacological characterization of the cardiovascular effect of Nibethione: ex vivo, in vivo and in silico studies
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Objective: This work describes the vasorelaxant and antihypertensive effects and the mechanism of action on vascular smooth muscle cells of Nibethione, a synthetic thiazolidinedione derivative. Additionally, evidence of its cytotoxicity is assessed. Methods: Nibethione (NB) was synthesized, and its vasorelaxant effect and mechanism of action were assessed through ex vivo experiments. Molecular docking studies were used to predict the mode of interaction with L-type Ca2+ channel, and in vivo antihypertensive activity was assayed on spontaneously hypertensive rats (SHR). The cytotoxicity potential was evaluated in porcine aortic endothelial cells (PAECs) from primary explants. Key findings: Nibethione vasorelaxant effect was efficient on KCl (80?mm) and NE-contraction. This effect was deleteriously modified in the presence of potassium channel block drugs, while the maximal contraction induced with NE was significantly decreased by NB; the CaCl2-induced contraction was abolished entirely. In vivo experiments showed that NB decreased diastolic blood pressure in 20.3 percent after its administration on SHR. The molecular docking showed that NB blocks L-type Ca2+ channel, and in vitro tests showed that NB did not produce cytotoxic activity on PAECs (IC50 >1000?μm). Conclusions: Nibethione showed in vivo antihypertensive and ex vivo vasorelaxant effects with implication of voltage-dependent L-type Ca2+ channel blocking, and this may contribute to the research of novel antihypertensive drugs.
- Sánchez-Recillas, Amanda,Navarrete-Vázquez, Gabriel,Hidalgo-Figueroa, Sergio,Bonilla-Hernández, Marcos,Ortiz-Andrade, Rolffy,Ibarra-Barajas, Maximiliano,Yá?ez-Pérez, Víctor,Sánchez-Salgado, Juan Carlos
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Read Online
- Synthesis, molecular modeling, selective aldose reductase inhibition and hypoglycemic activity of novel meglitinides
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In the present study, a novel generation of selective aldose reductase ALR2 inhibitors with significant hypoglycemic activities was designed and modulated based on rhodanine scaffold joined to an acetamide linker in between two lipophilic moieties. The synthesis of the novel compounds was accomplished throughout simple chemical pathways. Molecular docking was performed on B-cell membrane protein SUR1, aldehyde reductase ALR1 and aldose reductase ALR2 active sites. Compounds 10B, 11B, 12B, 15C, 16C, 26F and 27F displayed the highest hypoglycemic activities with 80.7, 85.2, 87, 82.3, 83.5, 81.4 and 85.3% reduction in blood glucose levels, respectively. They were more potent than the standard hypoglycemic agent repaglinide with 65.4% reduction in blood glucose level. Compounds 12B and 15C with IC50 0.29 and 0.35 μM were more potent than the standard ALR2 inhibitor epalrestat with IC50 0.40 μM. They were selective towards ALR2 over ALR1 134 and 116 folds, respectively. Molecular docking studies matched with the in-vitro and in-vivo results to elucidate the dual activities of both compounds 12B and 15C as potent antagonists for ALR2 over ALR1 and good agonists for the SUR1 protein.
- Salem, Manar G.,Abdel Aziz, Yasmine M.,Elewa, Marwa,Nafie, Mohamed S.,Elshihawy, Hosam A.,Said, Mohamed M.
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- Benzoxazolyl linked benzylidene based rhodanine and analogs as novel antidiabetic agents: synthesis, molecular docking, and in vitro studies
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Benzoxazolyl linked meta- and para-substituted new chemical entities (5a–5h) featuring thiazolidinedione, rhodanine, hydantoin, and thiohydantoin moieties were synthesized and characterized by 1H NMR, 13C NMR, FT-IR, and HRMS spectra
- Singh, Varinder,Singh, Amanjot,Singh, Gagandeep,Verma, Raman K.,Mall, Rajiv
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p. 1905 - 1914
(2021/08/27)
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- Facile synthesis of 5-arylidene rhodanine derivatives using Na2SO3 as an eco-friendly catalyst. Access to 2-mercapto-3-aryl-acrylic acids and a benzoxaborole derivative
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A simple, efficient and environment-friendly procedure for the synthesis of 5-arylidene rhodanines derivatives via a Knoevenagel type reaction was developed using rhodanine, a variety of differently substituted aldehydes and Na2SO3 a
- Boureghda, Chaima,Boulcina, Raouf,Dorcet, Vincent,Berrée, Fabienne,Carboni, Bertrand,Debache, Abdelmadjid
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supporting information
(2020/12/21)
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- Introducing broadened antibacterial activity to rhodanine derivatives targeting enoyl-acyl carrier protein reductase
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Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50=3.18μM for Mtb InhA; IC50=10nM for DNA Gyrase B) with positive controls. Structure–activity relationship discussion and molecular docking model revealed the significance of rhodanine moiety and derived methoxyl on meta-position, pointing out orientations for future modification.
- Sun, Zhi-Gang,Xu, Yun-Jie,Xu, Jian-Fei,Liu, Qi-Xing,Yang, Yu-Shun,Zhu, Hai-Liang
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p. 125 - 129
(2019/03/28)
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- Green synthesis, biological activity evaluation, and molecular docking studies of aryl alkylidene 2, 4-thiazolidinedione and rhodanine derivatives as antimicrobial agents
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Aims and Objective: The magic scaffolds rhodanine and thiazolidine are very important heterocyclic compounds in drug design and discovery. Those are important heterocyclic compounds that have attracted a great deal of attention due to the fact that they e
- Akhavan, Malihe,Bekhradnia, Ahmadreza,Foroughifar, Naser,Pasdar, Hoda
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p. 716 - 727
(2020/01/30)
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- Discovery and development of novel rhodanine derivatives targeting enoyl-acyl carrier protein reductase
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A series of rhodanine derivatives RB1–RB23 were synthesized through a two-round screening. Their Mycobacterial tuberculosis (Mtb) InhA inhibitory activity and Mtb growth blocking capability were evaluated. The most potent hit compound RB23 indicated compa
- Xu, Jian-Fei,Wang, Tian-Tian,Yuan, Qing,Duan, Yong-Tao,Xu, Yun-Jie,Lv, Peng-Cheng,Wang, Xiao-Ming,Yang, Yu-Shun,Zhu, Hai-Liang
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p. 1509 - 1516
(2019/03/05)
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- Synthesis, in-vitro cytotoxicity and antimicrobial evaluations of some novel thiazole based heterocycles
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Condensation of rhodanine (1) with pyrazol-3(2H)-one derivatives (2a-f) gave 5-substituted-2-thioxo-1,3- thiazolidin-4-one derivatives (3a-f). Reaction of compound (1) with 2-arylmethylidene-malononitrile (4a-d) yielded the unexpected derivatives (5a-d). The latter compounds were subjected to cyclization reactions with malononitrile under different basic conditions, hydroxylamine hydrochloride and/or thiourea to furnish the fused thiazole derivatives (6a-d) and (8-10a-d). Coupling of (1) with diazotized aromatic amines (11a-c) in pyridine afforded the arylhydrazones (12a-c). Fusion of latter compounds with malononitrile afforded the thiazolopyridazine derivatives (13a-c). The structures of the newly synthesized compounds were elucidated via spectral data and elemental analyses. The in-vitro cytotoxic activity of compounds (3a-f) against the cell line MCF-7 was evaluated. Also, the synthesized products were investigated for their antibacterial and antifungal activities against six standard organisms including the G- bacteria, Staphylococcus aureus and Bacillus subtilis, G+ bacteria, Escherichia coli and Proteus vulgaris in addition to fungi, Candida albicans and Aspergillus flavus.
- El-Mawgoud, Heba Kamal Abd
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p. 1314 - 1323
(2019/12/23)
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- Molecular modeling of drug-pathophysiological Mtb protein targets: Synthesis of some 2-thioxo-1, 3-thiazolidin-4-one derivatives as anti-tubercular agents
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Twenty novel 2-thioxo-1, 3-thiazolidin-4-one derivatives (5a-5t) were synthesized and evaluated for their antitubercular activity. The structure of the compounds was confirmed by IR, NMR and Mass Spectroscopy methods. In addition, single-crystal X-ray diffraction was performed for compound 5a. All the synthesized compounds were screened for their in-vitro antimycobacterial activity against MTB (H37RV, ATCC No: 27294) by Alamar Blue assay method. Compounds 5r, 5k, 5t displayed most potent in-vitro activity with MICs of 0.05, 0.1, 0.2 μg/ml concentrations respectively which are comparatively potent than the standards. Molecular docking and dynamics simulations were performed to find out the plausible mechanism of the titled compounds.
- Noorulla,Suresh, Ayyadurai Jerad,Devaraji, Vinod,Mathew, Bijo,Umesh, Devi
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p. 682 - 696
(2017/07/13)
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- A Facial Synthesis and Anticancer Activity of (Z)-2-((5-(4-nitrobenzylidene)-4-oxo-4,5-dihydrothiazol-2-yl)amino)-substituted Acid
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In order to explore the anticancer and antimicrobial activity associated with the thiazole framework, we synthesized the new series (Z)-2-((5-(4-nitrobenzylidene)-4-oxo-4,5-dihydrothiazol-2-yl)amino)-substituted acid derivatives 6a–l. All the synthesized compounds were evaluated for anticancer and antimicrobial activity in vitro. Among these, the compounds 6a, 6b, 6c, 6e, 6f, 6g, 6h, 6i, 6j, and 6k showed highest antibacterial and antifungal activity. The compound 6a exhibited significant antibacterial activity against Bacillussubtilis, whereas compound 6j displays significant antifungal activity against fungal strains, that is, A.?oryzae. The in vitro anticancer studies revealed that 6e, 6g, 6h, 6k, and 6l are the most active compounds against MCF-7 and BT-474 human breast cancer cell lines, which can be regarded as the promising drug candidate for development of anticancer drugs.
- Pansare, Dattatraya N.,Shelke, Rohini N.,Shinde, Devanand B.
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p. 3077 - 3086
(2017/10/06)
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- [Et3NH][HSO4] catalyzed efficient synthesis of 5-arylidene-rhodanine conjugates and their antitubercular activity
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Abstract: We have described a highly efficient, safer protocol for the synthesis of 5-arylidene-rhodanine conjugates catalyzed by Bronsted acidic ionic liquid [Et3NH][HSO4] in excellent yields. The protocol offers cost-effective, environmentally benign, solvent-free conditions and recycle–reuse of the catalyst. The synthesized 5-arylidene-rhodanine conjugates were characterized on the basis of 1H NMR, 13C NMR and HRMS spectral data. A series of 5-arylidene-rhodanine derivatives 3a–h, 4a–h were synthesized and evaluated for their in vitro antitubercular activity against dormant Mycobacterium tuberculosis H37Ra and M. bovis BCG strains. Moreover, compounds 3a, 3b, 3e, 3f, 3g, 3h and 4f exhibited good antitubercular activity and were also evaluated for anti-proliferative activity against MCF-7, A549 and HCT116 cell lines using modified MTT assay and found to be noncytotoxic. Compounds 3a–h and 4f were further screened for their antibacterial activity against four bacteria strains to assess their selectivity towards M. tuberculosis. Furthermore, in silico ADME prediction of all the tested compounds followed the criteria for orally active drug and, therefore, these compounds may have a good potential for eventual development as oral agents. Graphical Abstract: [Figure not available: see fulltext.]
- Subhedar, Dnyaneshwar D.,Shaikh, Mubarak H.,Nawale, Laxman,Yeware, Amar,Sarkar, Dhiman,Shingate, Bapurao B.
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p. 6607 - 6626
(2016/07/12)
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- Microwave-Assisted condensation reactions of acetophenone derivatives and activated methylene compounds with aldehydes catalyzed by boric acid under solvent-free conditions
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We here disclosed a new protocol for the condensation of acetophenone derivatives and active methylene compounds with aldehydes in the presence of boric acid under microwave conditions. Implementation of the reaction is simple, healthy and environmentally
- Brun, Elodie,Safer, Abdelmounaim,Carreaux, Franois,Bourahla, Khadidja,L'Helgoua'ch, Jean-Martial,Bazureau, Jean-Pierre,Villalgordo, Jose Manuel
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p. 11617 - 11631
(2015/08/06)
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- A facile synthesis of (Z)-5-(substituted)-2-(methylthio)thiazol-4(5H)-one using microwave irradiation and conventional method
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A new effective approach to the synthesis of some new (Z)-5-(substituted)- 2-thioxothiazolidin-4-one 3a-l and (Z)-5-(substituted)-2-(methylthio)thiazol- 4(5H)-one 5a-l is reported under microwave irradiation as well as conventional conditions.
- Pansare, Dattatraya N.,Shinde, Devanand B.
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supporting information
p. 1107 - 1110
(2014/02/14)
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- A facile synthesis of (Z)-5-(substituted)-2-(methylthio)thiazol-4(5H)-one using microwave irradiation and conventional method
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A new effective approach to the synthesis of some new (Z)-5-(substituted)-2-thioxothiazolidin-4-one 3a-l and (Z)-5-(substituted)-2-(methylthio)thiazol-4(5H)-one 5a-l is reported under microwave irradiation as well as conventional conditions.
- Pansare, Dattatraya N.,Shinde, Devanand B.
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p. 1107 - 1110
(2015/02/19)
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- Evaluation of michael-type acceptor reactivity of 5-benzylidenebarbiturates, 5-benzylidenerhodanines, and related heterocycles using NMR
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Despite existing experimental and computational tools to assess the risk, the non-specific chemical modification of protein thiol groups remains a significant source of false-positive hits, particularly in academic drug discovery. Herein, we describe the
- Arsovska, Emilija,Trontelj, Jurij,Zidar, Nace,Tomai, Tihomir,Mai, Lucija Peterlin,Kikelj, Danijel,Plavec, Janez,Zega, Anamarija
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p. 637 - 644
(2014/12/11)
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- Facile and convenient synthesis of 5-arylalkylidenerhodanines by electrocatalytic crossed aldol condensation
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An electrochemically induced catalytic crossed Aldol condensation of one equivalent of rhodanine with various aromatic aldehydes and ketones in ethanol in an undivided cell in the presence of sodium bromide as an electrolyte results in the formation of th
- Veisi, Hojat,Vafajoo, Zahra,Maleki, Behrooz,Maghsoodlou, Malek Taher
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p. 672 - 677
(2013/07/26)
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- Urea/thiourea catalyzed, solvent-free synthesis of 5-arylidenethiazolidine- 2,4-diones and 5-arylidene-2-thioxothiazolidin-4-ones
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An efficient and organo-catalyzed method has been developed for the synthesis of 5-arylidenethiazolidine-2,4-diones and 5-arylidene-2- thioxothiazolidin-4-ones via Knoevenagel condensation of arylaldehydes 1 and 2,4-thiazolidinedione 2a/2-thioxothiazolidin-4-one 2b under mild conditions. Urea-adduct 4 and azomethine 5 also afford arylidene-products 3 by reacting with 2a-b via addition-elimination reaction. This protocol has the features of use of inexpensive, ecofriendly readily available, effective catalyst system viz. urea/thiourea, avoidance of volatile solvents, excellent yield and simple work-up procedure.
- Shah, Sakshi,Singh, Baldev
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experimental part
p. 5388 - 5391
(2012/09/22)
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- Privileged scaffolds or promiscuous binders: A comparative study on rhodanines and related heterocycles in medicinal chemistry
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Rhodanines and related five-membered heterocycles with multiple heteroatoms have recently gained a reputation of being unselective compounds that appear as "frequent hitters" in screening campaigns and therefore have little value in drug discovery. However, this judgment appears to be based mostly on anecdotal evidence. Having identified various rhodanines and related compounds in screening campaigns, we decided to perform a systematic study on their promiscuity. An amount of 163 rhodanines, hydantoins, thiohydantoins, and thiazolidinediones were synthesized and tested against several targets. The compounds were also characterized with respect to aggregation and electrophilic reactivity, and the binding modes of rhodanines and related compounds in published X-ray cocrystal structures were analyzed. The results indicate that the exocyclic, double bonded sulfur atom in rhodanines and thiohydantoins, in addition to other structural features, offers a particularly high density of interaction sites for polar interactions and hydrogen bonds. This causes a promiscuous behavior at concentrations in the "screening range" but should not be regarded as a general knockout criterion that excludes such screening hits from further development. It is suggested that special criteria for target affinity and selectivity are applied to these classes of compounds and that their exceptional and potentially valuable biomolecular binding properties are consequently exploited in a useful way.
- Mendgen, Thomas,Steuer, Christian,Klein, Christian D.
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supporting information; experimental part
p. 743 - 753
(2012/03/11)
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- Structure-based design of a new series of d-glutamic acid based inhibitors of bacterial UDP-N-acetylmuramoyl-l-alanine: D-glutamate ligase (MurD)
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MurD ligase is one of the key enzymes participating in the intracellular steps of peptidoglycan biosynthesis and constitutes a viable target in the search for novel antibacterial drugs to combat bacterial drug-resistance. We have designed, synthesized, and evaluated a new series of d-glutamic acid-based Escherichia coli MurD inhibitors incorporating the 5-benzylidenethiazolidin-4- one scaffold. The crystal structure of 16 in the MurD active site has provided a good starting point for the design of structurally optimized inhibitors 73-75 endowed with improved MurD inhibitory potency (IC50 between 3 and 7 μM). Inhibitors 74 and 75 showed weak activity against Gram-positive Staphylococcus aureus and Enterococcus faecalis. Compounds 73-75, with IC 50 values in the low micromolar range, represent the most potent d-Glu-based MurD inhibitors reported to date.
- Toma?i?, Tihomir,Zidar, Nace,?ink, Roman,Kova?, Andreja,Blanot, Didier,Contreras-Martel, Carlos,Dessen, Andréa,Müller-Premru, Manica,Zega, Anamarija,Gobec, Stanislav,Kikelj, Danijel,Peterlin Ma?i?, Lucija
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supporting information; experimental part
p. 4600 - 4610
(2011/09/14)
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- Solvent-free synthesis of 5-benzylidene-2-thioxothiazolidin-4-ones and thiazolidine-2,4-diones catalysed by glycine under microwave irradiation
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A novel and clean synthesis of 5-benzylidene-2-thioxothiazolidin-4-ones and thiazolidine-2,4-diones has been achieved in good yields by condensation of aromatic aldehydes with rhodanine or thiazolidine-2,4-dione under microwave irradiation using glycine a
- Yang, Ben-Yong,Yang, De-Hong
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experimental part
p. 238 - 239
(2011/07/09)
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- Synthesis and characterization of (Z)-5-arylmethylidenerhodanines with photosynthesis-inhibiting properties
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A series of rhodanine derivatives was prepared. The synthetic approach, analytical and spectroscopic data of all synthesized compounds are presented. Lipophilicity of all the discussed rhodanine derivatives was analyzed using the RP-HPLC method. The compo
- Opletalova, Veronika,Dolezel, Jan,Kralova, Katarina,Pesko, Matus,Kunes, Jiri,Jampilek, Josef
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experimental part
p. 5207 - 5227
(2011/08/06)
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- A solvent-free protocol for the green synthesis of arylalkylidene rhodanines in a task-specific ionic liquid
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2-Hydroxyethylammonium formate acts as a task-specific ionic liquid (TSIL) for the Knoevenagel condensation of carbonyl compounds with rhodanine to afford arylalkylidene rhodanines under solvent-free conditions and in good-to-excellent yields. Additionally, compared with those in organic solvents, the yields obtained in the presence of our ionic liquid (IL) were significantly increased. The detailed mechanism of the catalytic effect of TSIL is also reported for the first time.
- Alizadeh, Abdolhamid,Khodaei, Mohammad M.,Eshghi, Ali
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experimental part
p. 514 - 518
(2010/08/04)
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- Discovery of novel 5-benzylidenerhodanine and 5-benzylidenethiazolidine-2, 4-dione inhibitors of MurD ligase
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We have designed, synthesized, and evaluated 5-benzylidenerhodanine-and 5-benzylidenethiazolidine-2,4-dione-based compounds as inhibitors of bacterial enzyme MurD with E. coli IC50 in the range 45-206 μM. The high-resolution crystal structure o
- Zidar, Nace,Toma?i?, Tihomir,?ink, Roman,Rupnik, Veronika,Kova?, Andreja,Turk, Samo,Patin, Delphine,Blanot, Didier,Contreras Martel, Carlos,Dessen, Andréa,Müller Premru, Manica,Zega, Anamarija,Gobec, Stanislav,Peterlin Ma?i?, Lucija,Kikelj, Danijel
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supporting information; experimental part
p. 6584 - 6594
(2010/11/17)
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- Fungicide activity of 5-(4-chlorobenzylidene)-(Z)-2-dimethylamino-1,3- thiazol-4-one against Cryptococcus neoformans
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The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested a
- Insuasty, Braulio,Gutierrez, Alexander,Quiroga, Jairo,Abonia, Rodrigo,Nogueras, Manuel,Cobo, Justo,Svetaz, Laura,Raimondi, Marcela,Zacchino, Susana
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scheme or table
p. 48 - 53
(2010/06/14)
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- Iodine catalysed synthesis of 5-(arylmethylidene)rhodanines by grinding under solvent-free conditions
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5-(Arylmethylidene)rhodanines have been synthesised in 88-95% yields by Knoevenagel condensation of various aromatic aldehydes with rhodanine in the presence of a catalytic amount of iodine at room temperature by grinding under solvent-free conditions.
- Wang, Hongshe,Zeng, June
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experimental part
p. 374 - 376
(2009/12/31)
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- Synthesis and biological evaluation of new glutamic acid-based inhibitors of MurD ligase
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Mur ligases catalyze the biosynthesis of the UDP-MurNAc-pentapeptide precursor of peptidoglycan, an essential polymer of bacterial cell-wall. They constitute attractive targets for the development of novel antibacterial agents. Here we report on the synth
- Tomasic, Tihomir,Zidar, Nace,Rupnik, Veronika,Kovac, Andreja,Blanot, Didier,Gobec, Stanislav,Kikelj, Danijel,Masic, Lucija Peterlin
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scheme or table
p. 153 - 157
(2009/05/07)
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- Green synthesis of 5-benzylidene rhodanine derivatives catalyzed by 1-butyl-3-methyl imidazolium hydroxide in water
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A basic functionalized ionic liquid, 1-butyl-3-methyl imidazolium hydroxide ([bmim][OH]), catalyzed the Knoevenagel condensation of rhodanine with aromatic aldehydes. It proceeded smoothly in water to afford the 5-benzylidene rhodamine derivatives in high yields at room temperature. This new method offers several advantages, such as excellent yields, short reaction times, and simple procedure. The catalyst can be reused at least 5 times without significant loss of activity.
- Gong, Kai,He, Zhi-Wei,Xu, Ying,Fang, Dong,Liu, Zu-Liang
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experimental part
p. 913 - 915
(2009/09/06)
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- Facile synthesis of 5-benzylidene rhodamine derivatives under microwave irradiation
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A series of 5-benzylidenerhodamine derivatives were synthesized by the cross-aldol condensation of an aromatic aldehyde with rhodamine or rhodamine acetic acid in sodium acetate/acetic acid under microwave irradiation. The reaction was completed in 8-20 min with 63-94% yields and was environmentally benign with easy workup. Copyright Taylor & Francis Group, LLC.
- Zhou, Jian-Feng,Song, Yuan-Zhi,Zhu, Feng-Xia,Zhu, Yu-Lan
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p. 3297 - 3303
(2007/10/03)
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- PHAMACEUTICAL PREPARATIONS COMPRISING INSULIN
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Novel preparations comprising ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer wherein the ligand is extended by protamine that are capable of prolonging the ac-tion of insulin preparations.
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Page/Page column 130
(2010/02/15)
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- SAR and mode of action of novel non-nucleoside inhibitors of hepatitis C NS5b RNA polymerase
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Novel non-nucleoside inhibitors of the HCV RNA polymerase (NS5b) with sub-micromolar biochemical potency have been identified which are selective for the inhibition of HCV NS5b over other polymerases. The structures of the complexes formed between several
- Powers, Jay P.,Piper, Derek E.,Li, Yang,Mayorga, Veronica,Anzola, John,Chen, James M.,Jaen, Juan C.,Lee, Gary,Liu, Jinqian,Peterson, M. Greg,Tonn, George R.,Ye, Qiuping,Walker, Nigel P. C.,Wang, Zhulun
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p. 1034 - 1046
(2007/10/03)
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- Stabilised insulin compositions
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The present invention provides pharmaceutical compositions comprising insulin and novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The resulting preparations have improved physical and chemical stability.
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Page/Page column 54
(2008/06/13)
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- PHARMACEUTICAL PREPARATIONS COMPRISING ACID-STABILISED INSULIN
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Novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer that are capable of prolonging the action of insulin preparations are disclosed.
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Page/Page column 127
(2010/02/08)
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- Novel ligands for the hisb10 zn2+ sites of the r-state insulin hexamer
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Novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer that are capable of prolonging the action of insulin preparations are disclosed.
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- Efficient synthesis of 3-acyl-5-arylmethylene-4-oxothiazolidine-2-thiones
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An efficient procedure was suggested for preparing 3-acyl-5-arylmethylene- 4-oxothiazolidine-2-thiones.
- Aronova,Ginak
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p. 164 - 165
(2007/10/03)
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- The synthesis and SAR of rhodanines as novel class C β-lactamase inhibitors
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β-Lactam antibiotics such as the cephalosporins and penicillins have diminished clinical effectiveness due to the hydrolytic activity of diverse β-lactamases, especially those in molecular classes A and C. A structure-activity relationship (SAR) study of
- Grant, Eugene B.,Guiadeen, Deodialsingh,Baum, Ellen Z.,Foleno, Barbara D.,Jin, Haiyong,Montenegro, Deborah A.,Nelson, Erin A.,Bush, Karen,Hlasta, Dennis J.
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p. 2179 - 2182
(2007/10/03)
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