Design, synthesis and pharmacological screening of a series of N1-(substituted) aryl-5,7-dimethyl-2-(substituted)pyrido(2,3-d)-pyrimidin-4(3H)-ones as potential histamine H1-receptor antagonists.

abstract：:This work has been focused on testing the influence of two selected Pt(II) complexes cisplatin, Pt(NH₃)₂Cl₂, and [Pt(dach)Cl₂] on the activity of porcine pancreatic phospholipase A₂ (PLA₂). It has been assumed that this enzyme plays a role in carcinogenesis and that it could be a target in the tumour therapy. The resu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Radisavljević M,Kamčeva T,Bugarčić ŽD,Petković M

更新日期：2013-08-01 00:00:00

abstract：UNLABELLED:Abstract In biological systems, the Keap1/Nrf2/antioxidant response element pathway determines the ability of mammalian cells to adapt and survive conditions of oxidative, electrophilic and inflammatory stress by regulating the production of cytoprotective enzymes NAD(P)H:quinone oxidoreductase 1 (NQO1, EC ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ghorab MM,Higgins M,Alsaid MS,Arafa RK,Shahat AA,Dinkova-Kostova AT

更新日期：2014-12-01 00:00:00

abstract：:Phthalates, used in medical devices (MDs), have been identified as reproductive and developmental toxicants. Their toxicity varies somewhat depending on the specific phthalate and is in part linked to the activation of Peroxisome Proliferating-Activated Receptors (PPARs). So, the use of MDs containing targeted phthala...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kambia N,Farce A,Belarbi K,Gressier B,Luyckx M,Chavatte P,Dine T

更新日期：2016-01-01 00:00:00

abstract：:A series of novel benzene sulfonamides (previously evaluated as selective cyclooxygenase-2 inhibitors) has been profiled against human carbonic anhydrases I, II, IV and VII in an attempt to observe the manifestation of the well established "tail" approach for designing potent, isoform-selective inhibitors of carbonic ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Supuran CT,Kalinin S,Tanç M,Sarnpitak P,Mujumdar P,Poulsen SA,Krasavin M

更新日期：2016-01-01 00:00:00

abstract：:Two new series of heterocyclic derivatives with potential anticancer activity, in which a pyrrolo[1,2-b]pyridazine or a pyrrolo[2,1-a]phthalazine moiety was introduced in place of the 3'-hydroxy-4'-methoxyphenyl ring of phenstatin have been synthesised and their structure-activity relationship (SAR) was studied. Fourt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Popovici L,Amarandi RM,Mangalagiu II,Mangalagiu V,Danac R

更新日期：2019-12-01 00:00:00

abstract：:The tyrosine kinase inhibitory action of the derivatives of N-Phenyl-N'-{4-(4-quinolyloxy)phenyl}urea is quantitatively analyzed using multiple regression analysis. The analysis has helped to ascertain the role of different substituents in explaining the observed inhibitory actions of these compounds for two receptors...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma BK,Sharma SK,Singh P,Sharma S

更新日期：2008-04-01 00:00:00

abstract：:The mechanism of inhalation anesthesia remains to be fully elucidated. While certain neuronal membrane proteins are considered sites of action, cytosolic proteins may also be targets. We hypothesize that inhaled anesthetics may act via glyceraldehyde 3-phosphate dehydrogenase (GAPDH), which has recently been shown to ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Swearengin TA,Fibuch EE,Seidler NW

更新日期：2006-10-01 00:00:00

abstract：:A set of novel quinolone-triazole conjugates (12-31) were synthesized in three steps in good yields starting from 2-phenylquinoline-4-carboxylic acid. All the intermediates, as well as the final 1,2,4-triazolyl quinolines were fully characterized by their detailed spectral analysis utilizing different techniques such ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Verbanac D,Malik R,Chand M,Kushwaha K,Vashist M,Matijašić M,Stepanić V,Perić M,Paljetak HČ,Saso L,Jain SC

更新日期：2016-01-01 00:00:00

abstract：:Melatonin (MLT) is a well-known free-radical scavenger, involving in the prevention of cellular damage that can lead to cancer, ageing and a variety of neurodegenerative diseases. Research on MLT-related compounds has been required to optimise the maximum pharmaceutical activity with the lowest side effects. In our on...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shirinzadeh H,Ince E,Westwell AD,Gurer-Orhan H,Suzen S

更新日期：2016-12-01 00:00:00

abstract：:Neurodegenerative disorders are consequences of progressive and irreversible loss of neurons due to unwanted apoptosis which involves caspases, a group of cysteine proteases that cleave other proteins and inactivate them. Among several different groups of caspase enzymes, caspases-3 plays a key role in apoptosis and a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma S,Ravichandran V,Jain PK,Mourya VK,Agrawal RK

更新日期：2008-06-01 00:00:00

abstract：:We report the biochemical and structural characterisation of a beta-carbonic anhydrase (β-CA) from Trichomonas vaginalis, a unicellular parasite responsible for one of the world's leading sexually transmitted infections, trichomoniasis. CAs are ubiquitous metalloenzymes belonging to eight evolutionarily divergent grou...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Urbański LJ,Di Fiore A,Azizi L,Hytönen VP,Kuuslahti M,Buonanno M,Monti SM,Angeli A,Zolfaghari Emameh R,Supuran CT,De Simone G,Parkkila S

更新日期：2020-12-01 00:00:00

abstract：:In mammalian skin, melanocyte proliferation and melanogenesis can be stimulated by keratinocytes, fibroblasts and other regulatory factors. To determine whether hydroxybenzyl alcohols (HBAs) show more inhibitory in melanocytes cultured alone or in melanocytes co-cultured with keratinocytes, we developed a murine melan...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Liu SH,Chu IM,Pan IH

更新日期：2008-08-01 00:00:00

abstract：:The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters ofN-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact e...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Aguirre-Alvarado C,Zaragoza-Martínez F,Rodríguez-Páez L,Nogueda B,Baeza I,Wong C

更新日期：2007-04-01 00:00:00

abstract：:The present study describes the synthesis of a series of new 4-aminoquinoline-derived thiazolidines and evaluation of their antimalarial activity against a NF-54 strain of Plasmodium falciparum in vitro and N-67 strain of Plasmodium yoelii in vivo. Among the series, two compounds, 2-(4-chloro-phenyl)-thiazolidine-4-ca...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Solomon VR,Haq W,Srivastava K,Puri SK,Katti SB

更新日期：2013-06-01 00:00:00

abstract：:Nineteen 5-nitrothiazolylthiosemicarbazones were synthesized from 5-nitrothiazole by three-step synthesis and evaluated for in vitro activities against seven mycobacterial species. Among them, N-(5-nitro-1, 3-thiazol-2-yl)-2-((Z)-4-[(phenylmethyl)oxy]phenylmethylidene)hydrazine-1-carbothioamide (4m) was found to be th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sriram D,Yogeeswari P,Senthilkumar P,Sangaraju D

更新日期：2010-02-01 00:00:00

abstract：:The synthesis of new 4-[2-(alkylamino)ethylthio]pyrrolo[1,2-a]quinoxaline derivatives la-1 is described in five or six steps starting from various substituted nitroanilines 2a-e. The bioisostere 5-[2-(alkylamino)ethylthio]pyrrolo[1,2- a]thieno[3,2-e]pyrazine 1m was also prepared. The new derivatives were evaluated as ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vidaillac C,Guillon J,Moreau S,Arpin C,Lagardère A,Larrouture S,Dallemagne P,Caignard DH,Quentin C,Jarry C

更新日期：2007-10-01 00:00:00

abstract：:An array of novel spiro imidazolidine derivatives was synthesized in dry media and was screened for their anti-microbial activities. Structure-activity relationship results revealed that compounds 22, 23 against P.aeruginosa, 24 against S.aureus, 24, 25 against K.pneumonia, 27 against S.aureus, β-H.streptococcus, 29 a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kanagarajan V,Thanusu J,Gopalakrishnan M

更新日期：2011-04-01 00:00:00

abstract：:The inhibition of monoamine oxidase B (MAO-B) could be an effective approach for the treatment of various neurological disorders. In this study, a series of 1, 4-benzodioxan-substituted chalcone derivatives were designed, synthesised and evaluated for their inhibitory activity against human MAO-B (hMAO-B). The majorit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kong Z,Sun D,Jiang Y,Hu Y

更新日期：2020-12-01 00:00:00

abstract：:A new series of 6, 7-dihydroxy-3-(methylphenyl) chromenones, including three new derivatives, i.e. 6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one (OPC); 6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one (MPC); 6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one (PPC) and one previously described, namely 6,7-dihydroxy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Basaran I,Sinan S,Cakir U,Bulut M,Arslan O,Ozensoy O

更新日期：2008-02-01 00:00:00

abstract：:A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Wang C,Xu S,Peng L,Zhang B,Zhang H,Hu Y,Zheng P,Zhu W

更新日期：2019-12-01 00:00:00

abstract：CONTEXT:Bacterial sphingomyelinase (SMase) is thought to play a crucial role in bacterial evasion of the immune response during the early stages of infections. OBJECTIVE:The objective of this study was to predict the chemical structure required for competitive SMase inhibition, then synthesize and test the effect of p...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Oda M,Imagawa H,Kato R,Yabiku K,Yoshikawa T,Takemoto T,Takahashi H,Yamamoto H,Nishizawa M,Sakurai J,Nagahama M

更新日期：2014-06-01 00:00:00

abstract：:An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newl...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mohamed MI,Zaky HT,Kandile NG

更新日期：2013-12-01 00:00:00

abstract：:Seven triterpenoid saponins were identified in methanolic extracts of seeds of the Zolfino bean landrace (Phaseolus vulgaris L.) by HPLC fractionation, revealing their ability to inhibit highly purified human recombinant aldose reductase (hAKR1B1). Six of these compounds were associated by MS analysis with the followi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Balestri F,De Leo M,Sorce C,Cappiello M,Quattrini L,Moschini R,Pineschi C,Braca A,La Motta C,Da Settimo F,Del-Corso A,Mura U

更新日期：2019-12-01 00:00:00

abstract：:The present study shows the chemical profile and the in vitro properties (antioxidant and inhibition of nitric oxide production) of the Origanum heracleoticum L. (Lamiaceae). The ethanolic extract of the aerial parts is characterized by terpenes and fatty acids. The extract, with high total phenol and flavonoid conten...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Conforti F,Marrelli M,Menichini F,Tundis R,Statti GA,Solimene U,Menichini F

更新日期：2011-06-01 00:00:00

abstract：:A revisited synthesis of 2-aryl-6-methyl-1,2-dihydro-1H-pyridin-4-ones and their saturated analogues 2-aryl-6-methylpiperidin-4-ols is described. A five steps procedure, using the sulfinimine chemistry, to prepare a key intermediate beta-(6-chloronicotinic)-beta-amino ester is also reported. In vivo spontaneous workin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Leflemme N,Freret T,Boulouard M,Dallemagne P,Rault S

更新日期：2005-12-01 00:00:00

abstract：:The current study was designed to assess the inhibitory activity of Broussonetia papyrifera-derived polyphenols against 3-chymotrypsin-like and papain-like coronavirus cysteine proteases. The isolated compounds were broussochalcone B (1), broussochalcone A (2), 4-hydroxyisolonchocarpin (3), papyriflavonol A (4), 3'-(3...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Park JY,Yuk HJ,Ryu HW,Lim SH,Kim KS,Park KH,Ryu YB,Lee WS

更新日期：2017-12-01 00:00:00

abstract：:The reactivity of [1,2,3]triazolo[1,5-a]pyridines 1 is described. Triazolopyridines react with electrophiles in two contrasting ways, giving 3-substituted triazolopyridines 2, or products 3, resulting from triazolo ring opening with loss of molecular nitrogen. The triazolopyridines can be lithiated at -40 degrees C by...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abarca-González B

更新日期：2002-12-01 00:00:00

abstract：:The increasing prevalence of drug resistant bacteria is a pandemic problem. Metallo-β-lactamases (MBLs) are one of the main causes of drug resistance due to hydrolysis of β-lactam antibiotics. Thus, the development of effective inhibitors of MBLs remains urgent. The compound thiomaltol was used as a lead compound to i...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Schlesinger SR,Bruner B,Farmer PJ,Kim SK

更新日期：2013-02-01 00:00:00

abstract：:The synthesis and biological evaluation of some novel thiazolofluorenones, thiazolofluorenes and thiazoloanthraquinones, substituted with amino side-chains are described. These polyheterocyclic compounds have been synthesized via the corresponding imino-1,2,3-dithiazoles. Their cytotoxic activity and their eventual se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chabane H,Pierre A,Leonce S,Pfeiffer B,Renard P,Thiery V,Guillaumet G,Besson T

更新日期：2004-12-01 00:00:00

abstract：:Synthesis of a novel series of structurally related pyrazoloquinoline nucleosides is described. All the newly synthesized compounds were examined for their in vitro antiviral activity against herpes simplex type-1 as shown by two different bioassays, namely; crystal violet staining or the MTS tetrazolium dye measureme...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bekhit AA,El-Sayed OA,Aboul-Enein HY,Siddiqui YM,Al-Ahdal MN

更新日期：2004-02-01 00:00:00