1,721,074 research outputs found
Antiherpes virus agents: A review
No full textA review with 33 refs. In this review, after some considerations about the structure of the virus and the viral replicative cycle, herpes virus diseases in man are described. The most important antiherpes virus drugs until now discovered are then reported analyzing and examg. their chem. structure related to their mechanism of action and their pharmacol. activity. Finally, defects of antiherpes virus drugs currently in therapy are shown, in order to outline which directions future developments will have to follow
Synthesis and stereochemistry of (Z)- and (E)-(3,4,5-trimethoxy)-a,ß-dimethylcinnamic acids and diastereoisomeric intermediate ß-hydroxy esters
No full textSynthesis and pharmacological activity of 1-phenyl-2-oxa-5-azabicyclo[4.4.0]decane derivatives
No full textTitle compds. I (Z = O, H2; R = H, Me) and II were prepd., and they showed central nervous system stimulant and anticonvulsant activity. Thus, a 2-aminocyclohexanol deriv. was treated with ClCH2COCl and NaOH to give amide III, and III and KOCMe3 in C6H6 were kept at room temp. to give I (Z = O, R = H)
Sintesi e stereochimica degli acidi (Z)- e (E)-(3,4,5-trimetossi)-alfa,beta-dimetilcinnamico e dei beta-idrossiesteri diastereoisomeri intermedi.
No full textSynthesis and affinity for serotonin and dopamine transporters of some benzophenone oxime ether derivatives
No full textIn a previous study, we reported the synthesis of several 3-(methylenaminoxymethyl)-substituted piperidine derivatives and their ability to interfere with the transmission mediated by biogenic amines. The present study describes the preparation of some new oxime derivatives and their capacity to inhibit serotonin (SERT) and dopamine (DAT) transporters expressed at the level of the rabbit cortex and the striatal membranes, respectively. All the compounds showed Ki values in the micromolar range on both transporters
Sintesi e proprietà inibitrici nei confronti delle cicloossigenasi di ammidi dell'acido 2-(4-metilsulfonilfenil)-1-ciclopentenico e di suoi analoghi eteroaromatici
No full textSynthesis and in-vitro antitumour activity of new naphthyridine derivatives on human pancreatic cancer cells
No full textObjectives The aim of the study was to evaluate the antitumour effect in vitro of newly
synthesized 7-substituted-2,3-dihydro-1,8-naphthyridines.
Methods Characterization tools included cell viability assay, caspase 3/7 induction, DNA
fragmentation, fibroblastic growth factor type 1 receptor kinase inhibition, and in-vitro
antiangiogenic analysis.
Key findings Treatment of MIA PaCa-2 human pancreatic cancer cells with test
compounds showed time- and concentration-dependent cytotoxicity with IC50 values in
the micromolar range. Compounds with an aminoalkyl or a diaminoalkyl side chain at the
7-position exhibited remarkable cytotoxicity, whereas the presence of a methyl group or a
cyclic amine in the same position led to a significant decrease in their biological activity.
Cytotoxicity screening demonstrated that the most active was compound 11 (mean 50%
inhibition of cell proliferation [IC50] 11 mM). This compound had an in-vitro antitumor
efficacy superior to 5-fluorouracil (the lowest cell viability value after treatment [Emax]
0.2% and 19%, respectively) and proved to be less toxic than 5-fluorouracil against noncancerous
human oral epithelial cells. In addition, compound 11 induced apoptosis in MIA
PaCa-2 cells and it was able to promote antiangiogenic effects in vitro. Finally, its
cytotoxicity was enhanced in pancreatic cancer cells stimulated with fibroblastic growth
factor, while no substantial effect was observed on human bronchial smooth muscle cells
stimulated with the same growth factor.
Conclusions These findings suggest that 1,8-naphthyridine derivatives are a promising
class of compounds in cancer research. In particular, the antitumor activity of compound 11
is worth further investigation
Structure-activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide
No full textThe (E)- and (2)-m-(trifluoromethy1)-a,/I-dimethylcbamamidaensd some of their N-alkyl derivatives were prepared
and pharmacologically tested as anticonvulsant agents in order to verify if a ring substituent, like the m-CF3 group,
different from a halogen but possessing the same electronic effect could lead to equally active compounds. Some
(E)-m-(trifluoromethy1)-a-methyaln-d -non-methyl-substituted-cinnamamidews ere also prepared and tested. In
the a,P-dimethyl series the results show that the m-CF3 group leads to producta more active than the one8 unsubstituted
on the phenyl ring but still less active than the p-halogen-substituted compounds previously studied. In the a-methyl
and non-methyl-substituted series, the trend shows the m-CF3 group being able to produce less toxic and, in some
cases, more active products than the previously studied amide
Derivati della 3-imminossimetilpiperidina inibitori dell’uptake delle monoammine nelle frazioni sinaptosomiali cerebrali.
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