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1.
A number of methylfuro[3,2-g]quinolin-7(8H)-ones, which can be considered isosters of methylpsoralens, were synthesized. The synthesis was performed starting from the appropriate methyl quinolin-2-ones on which the methylfuran ring was condensed. The molar absorptivity at long wavelengths of these compounds is remarkably higher than that of the corresponding methylpsoralen isosters; this fact may lead to an improved photo-binding to the biological targets. 相似文献
2.
P. Rodighiero M. Palumbo S. Marciani Magno P. Manzini O. Gia R. Piro A. Guiotto 《Journal of heterocyclic chemistry》1986,23(5):1405-1410
A number of new tetracyclic furocoumarin derivatives with a linear structure or with various angular arrangements, were synthetized. The new compounds are characterized for having an additional cyclohexene or phenyl ring condensed at the 4′,5′ double bond of the furan ring of the furocoumarin nucleus. The syntheses were performed starting from the appropriate hydroxycoumarins on which the tetrahydrobenzofuran or benzofuran moiety was built. Methyl groups have been introduced into positions which look most promising for enhancement of the photoreactivity of the compounds toward DNA. 相似文献
3.
O Gia S Mobilio A Chilin P Rodighiero M Palumbo 《Journal of photochemistry and photobiology. B, Biology》1988,2(4):435-442
The spectroscopic and DNA-binding properties of a number of pyrrolocoumarin derivatives, including linear tricyclic, angular tricyclic, linear tetracyclic and angular tetracyclic compounds were investigated. The compounds we examined form non-covalent complexes with duplex DNA, probably of the intercalation type. The binding constants are comparable with the constants found for the furocoumarin analogues. Although for some of the compounds the photoreactivity with DNA is comparable with that of 8-MOP, pyrrolocoumarins behave as monofunctional reagents. This fact is explained in terms of an increased delocalization of the 4',5' double bond in the pyrrole moiety. Denaturation-renaturation experiments and HPLC analysis of the photoadducts confirm that pyrrolocoumarins are essentially monofunctional DNA-photobinding agents. 相似文献
4.
3,5-Propanopiperidine derivatives as potential analgesics 总被引:1,自引:0,他引:1
E Oki S Oida Y Ohashi A Yoshida T Kamoshita 《Chemical & pharmaceutical bulletin》1974,22(5):1014-1021
5.
F. Ivy Carroll Bertold D. Berrang C. Preston Linn 《Journal of heterocyclic chemistry》1981,18(5):941-946
In this paper we present the synthesis of 8-(4′-amino-1′methyl-butylamino)-5-(β,β,β-trifluoroethoxy)-1,6-naphthyridine ( 4 ), 8-(4′-amino-1′methylbutylamino)-6-methyl-1,6-naphthyricline-5-one ( 5 ), two 1-alkyl-3-(4′-amino-1′-methylbutylamino)-7-methyl-1,8-naphthyridin-4-ones ( 20a ) and 20b ), 3-(1′-amino-4′-methylbutyl-amino)-l-ethyl-7-methyl-l,8-naphthyridin-4-one (20c), and 4-(4′-diethylamino-1′-methylbutylamino)-7-methyl-1,7-naphthyridin-8-one ( 28 ). The compounds were evaluated for antimalarial activity in the Plasmodium berghei screen and found to be inactive. 相似文献
6.
7.
de Campos-Buzzi F Padaratz P Meira AV Corrêa R Nunes RJ Cechinel-Filho V 《Molecules (Basel, Switzerland)》2007,12(4):896-906
Nine acetamidochalcones were synthesized and evaluated as antinociceptive agents using the mice writhing test. Given intraperitoneally all the compounds were more effective than the two reference analgesic drugs (acetylsalicylic acid and acetaminophen) used for comparison. N-{4-[(2E)-3-(4-nitrophenyl)prop-2-enoyl]phenyl}acetamide (6) was the most effective compound and was therefore selected for more detailed studies. It caused dose-related inhibition in the writhing test, being about 32 to 34-fold more potent than the standard drugs. It was also effective in the second phase of the formalin test and the capsaicin test. These acetamidochalcones, especially compound 6, might be further used as models to obtain new and more potent analgesic drugs. 相似文献
8.
2-Bromopyridine and 2-bromo-6-methoxymethylpyridine reacted with an excess of 1-phenylethylamine at reflux giving the aminopyridine derivatives 3a and 3b respectively. 相似文献
9.
A series of 4-aminomethyl-1,2,3,4-tetrahydroisoquinoline derivatives were prepared as potential CNS-agents acting via amino-acid neurotransmitter systems. The compounds were synthesized from 1,2,3,4-tetra-hydro-1-oxoisoquinoline-4-carboxylic acids obtained by dipolar cycloaddition reactions of imines with homo-phthalic anhydride. Among the compounds tested 5c and 5m showed sub-micromolar affinity for the NMDA receptor and represent a structurally novel class of ligand for this site. 相似文献
10.
Laurent Soulre Pascal Hoffmanna Frdric Bringaud 《Journal of heterocyclic chemistry》2003,40(5):943-947
N‐(p‐Nitrophenoxy)carbonyl‐3‐morpholino‐sydnonimine (NCMS) has been prepared from 3‐morpholinosydnonimine hydrochloride. Using the Griess assay and the superoxide‐mediated reduction of ferricytochrome c, the nitric oxide (NO?) and superoxide anion (O2?‐) ‐ releasing properties in phosphate buffer pH 7.4 of this novel peroxynitrite donor was studied and compared with the known 3‐morpholino‐sydnonimine (SIN‐1). From compound NCMS, a series of N‐substituted sydnonimine derivatives were easily prepared that contain purine or melaminophenyl groups which specify a recognition by a trypanosomal purine transporter. The ability of these new sydnonimines to inhibit the uptake of [23H]adenosine on Trypanosoma equiperdum was studied. 相似文献
11.
Several 5-benzoyl-2-thiobenzimidazole and 2-thiobenzimidazole aliphatic acids, esters, and N,N-dialkyl-carboxamides and thiocarboxamides were prepared by reacting bromo aliphatic acids, bromo aliphatic esters, and N,N-dialkylcarbamoyl or thiocarbamoyl chlorides with 5-benzoyl-2-thiobenzimidazole or 2-thiobenzimidazole in the presence of base. 2-Thiocarbomethoxy- and 2-thiocarboethoxybenzimidazole were prepared by the reaction of 2-thiobenzimidazole with methyl or ethyl chloroformate in the presence of base. However, the reaction of 5-benzoyl-2-thiobenzimidazole with ethyl chloroformate, afforded 5-benzoyl-2-ethylthiobenz-imidazole. 相似文献
12.
Uri Golik 《Journal of heterocyclic chemistry》1972,9(1):21-24
Malonimidoacetic acid derivatives (VIII, XIII) were synthesized as a potential penicillin analogs, hut they failed to inhibit the growth of bacteria when tested in vitro against a range of Gram-positive and Gram-negative microorganisms. 相似文献
13.
O. Habarova O. Bobiļeva E. Loža N. Romančikova 《Chemistry of Heterocyclic Compounds》2011,47(6):719-727
Inhibition of histone deacetylase activity appears as an original and effective approach for the treatment of cancer. A series of novel quinoline-containing derivatives has been synthesized and found that some of these compounds possess nanomolar histone deacetylase inhibitory activity. 相似文献
14.
[structure: see text] As part of our program investigating the use of ethynylated acenes in organic electronics, we have prepared a series of functionalized tetracene derivatives in search of a material with red emission suitable for use in display technologies. A number of such compounds with functionalization on the alkyne and/or the acene ring were easily prepared in one or two steps from commercially available materials. Solution fluorescence quantum efficiencies were generally good for these derivatives, which possessed emission maxima spanning the range 540-637 nm. Simple light-emitting diodes fabricated from these compounds showed that one of the derivatives did exhibit red electroluminescence. 相似文献
15.
Jhonsee Rani Telu Naveen Kuntala Kavitha Kankanala Venkanna Banothu Sarbani Pal Jaya Shree Anireddy 《Journal of heterocyclic chemistry》2021,58(4):969-982
We describe the synthesis, characterization, and in vitro antibacterial evaluation of a library of novel compounds based on 1,2,3-triazolo phosphonate framework along with the evaluation of DNA gyrase inhibitory potential of a promising molecule in silico. Preparation of these compounds was carried out via a multistep sequence comprising of the Abramov reaction followed by the Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC) as the key steps. Various α-hydroxyphosphonate derivatives containing either a secondary or tertiary alcohol at the α position were prepared. When screened for their antibacterial activities in vitro using a Gram-positive (Staphylococcus aureus) and three Gram-negative (Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa) strains, majority of these derivatives exhibited reasonable to good effects with the analogue 5k being active against all the strains. The SAR analysis indicated that the activity was influenced by the position of the α-hydroxyphosphonate moiety as well as the substituent present on the benzene ring attached to the 1,2,3-triazole ring. Moreover, the compound 5k showed strong interactions with the DNA active site when docked into the DNA gyrase in silico. Thus, the 1,2,3-triazolo phosphonate derivative 5k appeared to be a novel and promising hit molecule that deserves further study as a potential antibacterial agent. 相似文献
16.
Sandra Gemma Francesc Martí Emanuele Gabellieri Giuseppe Campiani Ettore Novellino Stefania Butini 《Tetrahedron letters》2009,50(41):5719-5953
Introduction in therapy of the naturally occurring trioxane artemisinin opened a new era in malaria treatment and prompted the development of semisynthetic and synthetic derivatives characterized by the presence of the key peroxide bridge. The 1,2-dioxane ring is present in some natural endoperoxides such as plakortin and dihydroplakortin, which are endowed with interesting antimalarial properties. Here we describe the development of a versatile stereocontrolled synthetic strategy to 1,2-dioxanes functionalized at the critical C3, C4, and C6 positions, potentially useful for the development of innovative antimalarials. 相似文献
17.
Mussardo P Corda E González-Ruiz V Rajesh J Girotti S Martín MA Olives AI 《Analytical and bioanalytical chemistry》2011,400(2):321-327
The interaction between DNA and several newly synthesized derivatives of the natural anticancer compound luotonin A has been
studied. The results from our work reveal an effective and selective alkaloid/double-stranded DNA (ds-DNA) interaction. In
the presence of increasing amounts of ds-DNA, a noticeable fluorescence quenching of the luotonin A derivatives under study
was observed. However, this effect did not take place when single-stranded DNA (ss-DNA) was employed. The association constant
alkaloids/ds-DNA was calculated by quantitation of such a quenching effect. The influence of other quenchers, namely Co2+ and Br− on the native fluorescence of luotonin A and derivatives was also studied, and a remarkable quenching effect was observed
for both ions. We have also investigated how by binding DNA the alkaloids could get protected from the external Co2+ and Br− quenchers. The Stern–Volmer constants (K
SV) for Co2+ and Br− quenching effect on the studied alkaloids were considerably reduced (10–50%) after incubation of the compounds in the presence
of DNA with regard to the K
SV values in absence of DNA. An increase in the fluorescence anisotropy values of luotonins was also produced only in the presence
of ds-DNA but not in the case of ss-DNA. To better characterize the nature of that interaction, viscosimetry assays and ethidium
bromide displacement studies were conducted. With regard to DNA reference solutions, the viscosity of solutions containing
DNA and luotonin A derivatives was reduced or not significantly increased. It was also observed that the studied compounds
were unable to displace the intercalating agent ethidium bromide. All of these results, together with the obtained association
constants values (K
ass = 2.2 × 102 – 1.3 × 103), support that neither covalent nor intercalating interactions luotonin A derivatives/ds-DNA are produced, leading to the
conclusion that these alkaloids bind ds-DNA through the minor groove. The specific changes in the fluorescence behavior of
luotonin A and derivatives distinguishing between ss-DNA and ds-DNA binding, lead us to propose these compounds as attractive
turn-off probes to detect DNA hybridization. 相似文献
18.
3-azabicyclo(3.3.1)nonane derivatives as potential analgesics 总被引:1,自引:0,他引:1
19.
Ryuichi Iemura Tsuneo Kawashima Toshikazu Fukuda Keizo Ito Goro Tsukamoto 《Journal of heterocyclic chemistry》1987,24(1):31-37
Several types of benzimidazole derivatives were prepared and were screened for H 1-antihistaminic activity. Most of the compounds showed potent antihistaminic activity in vitro. Among them 2-[(1-piperazinyl)methyl]-benzimidazoles 14 and 2-[(1-homopiperazinyi)methyl]benzimidazoles 15 exhibited potent activity also in vivo. 相似文献
20.
The tetrazole is an important functionality of the most of energetic materials due to 80% nitrogen content, stability, and
high enthalpy of formation. The present structure–property relationship study focuses on the optimized geometries of tetrazole
derivatives obtained from density functional theory (DFT) calculations at B3LYP/6-31G* levels. The heat of formation (HOF)
of tetrazole derivatives have been calculated by designing the appropriate isodesmic reactions. The increase in nitro groups
on azole rings shows the remarkable increase in HOF. Density has been predicted by using CVFF force field. Increase in the
nitro group increases the density. Detonation properties of the designed compounds were evaluated by using the Kamlet–Jacobs
equation based on predicted densities and HOFs. Designed tetrazole derivatives show detonation velocity (D) over 8 km/s and detonation pressure (P) of about 32 GPa. Thermal stability was evaluated via bond dissociation energies (BDE) of the weakest C–NO2 bond at B3LYP/6-31G* level. Charge on the nitro group has been used to assess the sensitivity correlation. Overall, the study
implies that designed compounds of this series are found to be stable and expected to be the novel candidates of high energy
materials (HEMs). 相似文献