共查询到20条相似文献,搜索用时 15 毫秒
1.
Stankova I Chuchkov K Wutzler P Schmidtke M 《Nucleosides, nucleotides & nucleic acids》2010,29(10):760-767
In the present study we have synthesized esters of acyclovir with cinnamic acids (p-coumaric, ferulic, and sinapic acids) and evaluated them for their antiviral and antioxidant potential. The antiviral activity of the newly synthesized compounds has been tested against human herpes virus 1 (HSV-1) in vitro. The results indicate that none of the synthesized compounds inhibits the tested virus strain. The antioxidant properties have been studied using 2,2-diphenyl-1-picrylhydrazyl (DPPH)* test. 相似文献
2.
Synthesis,antioxidative and antiviral activity of hydroxycinnamic acid amides of thiazole containing amino acid 总被引:1,自引:0,他引:1
The synthesis and the biological (antioxidant and antiviral) activities of novel hydroxycinnamic acid amides of a thiazole
containing TFA.valine-4-carboxylic acid ethyl ester are reported. The amides have been synthesized from p-coumaric, ferulic and sinapic acids with the corresponding TFA.valine-thiazole-4-carboxylic acid ethyl ester using the coupling
reagent N-ethyl-N′-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) and 4-(dimethylamino) pyridine (DMAP) as a catalyst. The antioxidant
properties of the newly synthesized amides have been studied for then antioxidative activity using 2,2-diphenyl-1-picrylhydrazyl
(DPPH)* test. The newly synthesized compounds have been tested against the replication in vitro of influenza virus A (H3N2)
and human herpes virus 1 and 2 (HSV-1 and HSV-2). 相似文献
3.
Deepika Sharma Pradeep Kumar Vikramjeet Judge Rakesh Narang Erik De Clercq 《Journal of enzyme inhibition and medicinal chemistry》2013,28(5):1161-1168
In the present study we have synthesized (4-nitrophenyl)-[2-(substituted phenyl)-benzoimidazol-1-yl]-methanones, (2-bromophenyl)-[2-(substituted phenyl)-benzoimidazol-1-yl]-methanone analogues (1–14) and evaluated them for their antimicrobial and antiviral potential. The results of antimicrobial screening indicated that none of the synthesized compounds were effective against the tested bacterial strains. Compounds 3, 11, 13 and compounds 5, 11, 12 were found to be active against Aspergillus niger and Candida albicans respectively, and may be further developed as antifungal agents. Furthermore, evaluation against a panel of different viruses pointed out the selective activity of compounds 5 and 6 against vaccinia virus and Coxsackie virus B4. 相似文献
4.
C. Mathé C. Périgaud G. Gosselin J.-L. Imbach 《Nucleosides, nucleotides & nucleic acids》2013,32(1-3):437-446
Abstract 2-Mercapto-5,6-dichlorobenzimidazole β-D-ribofuranonucleoside derivatives 8–10 have been synthesized and their antiviral properties examined. According to the glycosylation procedure used, the β-D-N-1 isomer (and the N, N-bis-riboside) or the β-D-S2-isomer have been obtained. All the prepared compounds were tested for their activity against a variety of RNA and DNA viruses, but they did not show significant antiviral activity. 相似文献
5.
《Nucleosides, nucleotides & nucleic acids》2013,32(4-7):755-758
3′-deoxy-3′-C-trifluoromethyl- (3), 2′,3′-dideoxy-3′-C-trifluoromethyl- (5) and 2′,3′-dideoxy-2′,3′-didehydro-3′-C-trifluoromethyladenosine (6) derivatives have been synthesized and their antiviral properties examined. All these derivatives were stereospecifically prepared by glycosylation of adenine with a trifluoromethyl sugar precursor (1), followed by appropriate chemical modifications. The prepared compounds were tested for their activity against HIV, but they did not show an antiviral effect. 相似文献
6.
Abstract 3′-Deoxy-β-L-erythro- (3), 3′-deoxy-β-L-thero- (6), 2′-fluoro- (7) and 2′-azido-2′,3′-dideoxy-β-L-erythro- (10) pentofuranonucleoside derivatives of thymine have been synthesized and their antiviral properties examined. All these derivatives were stereospecifically prepared by glycosylation of thymine with a suitable peracylated 3-deoxy-L-erythro-pentofuranose sugar (1), followed by appropriate chemical modifications. The prepared compounds were tested for their activity against HIV, but they did not show an antiviral effect. 相似文献
7.
Marzena Rządkowska Elżbieta Szacoń Agnieszka A. Kaczor Barbara Rajtar Łukasz Świątek Małgorzata Polz-Dacewicz 《Journal of enzyme inhibition and medicinal chemistry》2016,31(5):787-795
Novel 1-(1-aryl-4,5dihydro-1H-imidazoline)-3-chlorosulfonylourea derivatives 3a–3f were synthesized in the reaction of 1-aryl-4,5-dihydro-1H-imidazol-2-amines with chlorosulfonyl isocyanate. The second series of compounds 4a–4f was prepared from the respective 1-(1-aryl-4,5-dihydro-1H-imidazoline)-3-chlorsulfonylureas 3a–3f and 1,1′-carbonyldiimidazole (CDI). The selected compounds were tested for their activity against Herpes simplex virus and coxsackievirus B3 (CVB3). It was determined that three derivatives, i.e 3d, 4a and 4d are active against Herpes simplex virus (HSV-1). Compounds 3d and 4c are active against CVB3. Their favorable activity can be primarily attributed to their low lipophilicity values. Moreover, the lack of substituent in the phenyl moiety or 4-methoxy substitution can be considered as the most beneficial for the antiviral activity. 相似文献
8.
《Nucleosides, nucleotides & nucleic acids》2013,32(10):1907-1917
Abstract A series of acyclic C-nucleoside analogs of 2,6-dichloro- and 2,6,7-trichloroimidazo[1,2-a]pyridine were synthesized and tested for antiviral activity. The appropriate hydroxymethyl-substituted heterocycles were treated successively with thionyl chloride, an appropriate nucleophile, then diisopropylethylamine to obtain the desired acyclic nucleoside analogs. These compounds were evaluated for activity against human cytomegalovirus and herpes simplex virus, type 1. Two of the dichloro analogs, but none of the trichloro analogs demonstrated slight antiviral activity (IC50's = 20–45 µM) at non-cytotoxic concentrations. 相似文献
9.
Michel Legraverend Christiane Huel Aurelio Zerial Marc Lemaitre Emile Bisagni 《Nucleosides, nucleotides & nucleic acids》2013,32(5):639-647
Abstract Two new carbocyclic pyrrolo[2,3-d]pyrimidine nucleoside analogs related to the antiherpetic agent RP54 247 ( 8 ) have been synthesized. These compounds exhibited no antiviral activity in vitro toward herpes simplex virus type 1, human cytomegalovirus, and human immunodeficiency virus 1. 相似文献
10.
《Journal of enzyme inhibition and medicinal chemistry》2013,28(4):671-676
A series of new quinolone-3-carboxylic acids as HIV-1 integrase inhibitors featuring a fluorine atom at C-5 position were synthesized and evaluated for their antiviral activity in C8166 cell culture. These newly synthesized compounds showed anti-HIV activity against wild-type virus with an EC50 value ranging from 29.85 to 0.032 μΜ. The most active compound 4e exhibited activity against wild-type virus and the mutant virus A17 with an EC50 value of 0.032 and 0.082 μΜ, respectively. Preliminary structure–activity relationship of these 5-fluoroquinolone-3-carboxylic acids was also investigated. 相似文献
11.
《Nucleosides, nucleotides & nucleic acids》2013,32(5-8):857-859
Abstract Hitherto unknown 2′-deoxy-2′-C-trifluoromethyl-β-D-ribonucleoside derivatives bearing the five naturally occurring nucleic acid bases have been synthesized. The compounds were tested for their activity against HIV, HBV and several RNA viruses, but they did not show significant antiviral effect. 相似文献
12.
Socrates C. H. Cavalcanti Yuejun Xiang M. Gary Newton Raymond F. Schinazi Yung-Chi Cheng Chung K. Chu 《Nucleosides, nucleotides & nucleic acids》2013,32(10):2233-2252
Abstract A series of 2′,3′-dideoxy-2′-fluoro-L-threo-pentofuranosyl nucleosides has been synthesized as potential antiviral agents. The synthesized compounds were evaluated against HIV-1, HBV, HSV-1, and HSV-2. Among the synthesized analogues, only the cytosine derivative showed moderate antiviral activity against HIV and HBV. 相似文献
13.
Claire Pierra Sureyya Olgen Sócrates C. H. Cavalcanti Yung-Chi Cheng Raymond F. Schinazi Chung K. Chu 《Nucleosides, nucleotides & nucleic acids》2013,32(1-2):253-268
Abstract Cyclopropyl carbocyclic nucleosides have been synthesized from the key intermediate 2 which was converted to the mesylated cyclopropyl methyl alcohol 3. Condensation of compound 3 with various purine and pyrimidine bases gave the desired nucleosides. All synthesized nucleosides were evaluated for antiviral activity and cellular toxicity. Among them adenine 22 and guanine 23 derivatives showed moderate antiviral activity against HIV-1 and HBV. None of the other compounds showed any significant antiviral activities against HIV-1, HBV, HSV-1 and HSV-2 in vitro up to 100μM. 相似文献
14.
《Nucleosides, nucleotides & nucleic acids》2013,32(5):735-748
Several new pyrazolo[4,3‐c]quinolin‐3‐one ribonucleosides (5a–g) and their corresponding heterocycle moieties (3a–g) were synthesized and evaluated against vaccinia virus (VV) and herpes simplex virus type 1 (HSV‐1). The derivatives 3c and 3d showed modest inhibitory activity against vaccinia virus reaching 70% at a concentration of 100 µM. All heterocyclic compounds (3a–f) showed a modest inhibition against HSV‐1, reaching the maximal inhibitory effect around 20–30%. The antiviral effects of most of the pyrazolo[4,3‐c]quinolin‐3‐one ribonucleosides (5a–f) on VV and HSV were not impressive. 相似文献
15.
Christos A. Kontogiorgis Kyriakos Savvoglou Dimitra J. Hadjipavlou-Litina 《Journal of enzyme inhibition and medicinal chemistry》2013,28(1):21-29
Several coumarin derivatives have been reported to present multiple biological activities and especially anti-inflammatory/antioxidant activities. Recently the synthesis and in vivo/in vitro anti-inflammatory /antioxidant activities of several new coumarin derivatives with a 7-azomethine linkage have been reported. In the present study these derivatives were further tested for their antioxidant ability. Some of them were found in vitro to inhibit lipid peroxidation and to strongly scavenge superoxide radicals. Compound 3 was found to potently inhibit cyclooxygenase-1 (COX-1) and the yeast-induced rat paw oedema. The most active compounds within the set were tested against adjuvant-induced arthritis. Compound 3 was found to significantly protect the rats from adjuvant-induced arthritis (when it is administered from the first day or when it is administered the fourteenth day, with the first symptoms of the disease). An attempt was made to delineate the possible mechanism of action of the studied compounds. 相似文献
16.
Nassar MI Mohamed TK El-Toumy SA Gaara AH El-Kashak WA Brouard I El-Kousy SM 《Carbohydrate research》2011,(1):142-67
Investigation of the aqueous alcoholic extract of Pyruscalleryana Decne. leaves led to the isolation of two new phenolic acids glycosides, namely protocatechuoylcalleryanin-3-O-β-glucopyranoside (1) and 3′-hydroxybenzyl-4-hydroxybenzoate-4′-O-β-glucopyranoside (2), together with nine known compounds among them lanceoloside A and methylgallate, which have been isolated for the first time from the genus Pyrus. Structures of the isolated compounds were established by spectroscopic analysis, including UV, IR, HRESI-MS, and 1D/2D NMR. The total extract and some isolated compounds were determined against DPPH (2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydrazinyl radical, for their free radical scavenging activity, the total alcoholic extract showed strong antioxidant activity while the two new compounds showed weak antioxidant activity. 相似文献
17.
Simões LR Maciel GM Brandão GC Kroon EG Castilho RO Oliveira AB 《Letters in applied microbiology》2011,53(6):602-607
Aims: To investigate the in vitro antiviral activity of Distictella elongata (Vahl) Urb. ethanol extracts from leaves (LEE), fruits (FEE), stems and their main components. Methods and Results: The antiviral activity was evaluated against human herpesvirus type 1 (HSV‐1), murine encephalomyocarditis virus (EMCV), vaccinia virus Western Reserve (VACV‐WR) and dengue virus 2 (DENV‐2) by the 3‐(4, 5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) colorimetric assay. LEE presented anti‐HSV‐1 [EC50 142·8 ± 5·3 μg ml?1; selectivity index (SI) 2·0] and anti‐DENV‐2 activity (EC50 9·8 ± 1·3 μg ml?1; SI 1·5). The pectolinarin ( 1 ) isolated from LEE was less active against HSV‐1 and DENV‐2. A mixture of the triterpenoids ursolic, pomolic and oleanolic acids was also obtained. Ursolic and oleanolic acids have shown antiviral activity against HSV‐1. A mixture of pectolinarin ( 1 ) and acacetin‐7‐O‐rutinoside ( 2 ) was isolated from FEE and has presented anti‐DENV‐2 activity (EC50 11·1 ± 1·6 μg ml?1; SI > 45). Besides the antiviral activity, D. elongata has disclosed antioxidant effect. Conclusions: These data shows that D. elongata has antiviral activity mainly against HSV‐1 and DENV‐2, besides antioxidant activity. These effects might be principally attributed to flavonoids isolated. Significance and Impact of the Study: Distictella elongata might be considered a promising source of anti‐dengue fever phytochemicals. 相似文献
18.
A selective method for synthesizing (E)-fluorovinyl was developed. Novel acyclic (E)-fluorovinyl versions of neplanocin A were designed and selectively synthesized as potential antiviral agents. The condensation of the bromide 7 with the nucleosidic bases (5-FU, C, A, G) and the deprotection afforded the desired acyclic fluorovinyl nucleosides. The synthesized compounds 11, 12, 13, and 16 were evaluated for their antiviral activity. The guanine derivative 16 showed toxicity-dependent anti-HIV-1 activity in MT-4 cells. 相似文献
19.
20.
Jonathan L. Sessler Darren J. Magda Vincent Lynch Gilbert M. Schiff David I. Bernstein 《Nucleosides, nucleotides & nucleic acids》2013,32(3):431-448
Abstract The putative antiviral agent, (S)-2-amino-7-(2,3-dihydroxy-propyl) purine (1b), and its achiral analogue, 2-amino-7-(2-hydroxyethyl) purine (2), were synthesized by a procedure involving alkylation at N7 of guanosine followed by deribosylation and deoxygenation. Evidence for the stereochemical integrity of the former preparation was obtained from the X-ray diffraction structure of the novel tricyclic compound, (S)-6H, 7H, 8H-2-amino-7-hydroxy-[1,4] oxazepino [1,2,3-d, elpurine (17, obtained by a similar synthetic sequence. Compound (1a), a regioisomer of the known antiviral agent, (S)-9-(2,3-dihydroxypropyl) adenine ((S)-DHPA), was tested and found to be inactive in tissue culture against herpes virus type-2, rotavirus, poliovirus, and parainfluenza virus. 相似文献