Synthesis and Antiviral Activity of Novel Acyclic Nucleosides:  Discovery of a Cyclopropyl Nucleoside with Potent Inhibitory Activity against Herpesviruses

1998 ◽  
Vol 41 (8) ◽  
pp. 1284-1298 ◽  
Author(s):  
Takaaki Sekiyama ◽  
Satoshi Hatsuya ◽  
Yasuhiro Tanaka ◽  
Mamoru Uchiyama ◽  
Nobukazu Ono ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Inhibitory Activity ◽  
Acyclic Nucleosides ◽  
Potent Inhibitory Activity

scholarly journals Massiliamide, a cyclic tetrapeptide with potent tyrosinase inhibitory properties from the Gram-negative bacterium Massilia albidiflava DSM 17472T

2020 ◽  
Author(s):  
Andri Frediansyah ◽  
Jan Straetener ◽  
Heike Brötz-Oesterhelt ◽  
Harald Gross
Keyword(s):  
Absolute Configuration ◽  
Inhibitory Activity ◽  
Liquid Culture ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
Negative Bacterium ◽  
Gram Negative ◽  
The Absolute ◽  
Potent Inhibitory Activity ◽  
Cyclic Tetrapeptide

AbstractA cyclic tetrapeptide, designated massiliamide, was isolated from the liquid culture of the Gram-negative bacterium Massilia albidiflava DSM 17472T. The structure was elucidated through extensive spectroscopic analysis, including HR-MS and 1D and 2D NMR experiments. The absolute configuration was determined using the Marfey´s method. Massiliamide showed potent inhibitory activity towards tyrosinase with an IC50 value of 1.15 µM and no cytotoxicity.

Synthesis and antibacterial evaluation of novel Schiff's base derivatives of nitroimidazole nuclei as potent E. coli FabH inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (97) ◽  
pp. 54217-54225 ◽  
Author(s):  
Xin Zhang ◽  
Chetan B. Sangani ◽  
Li-Xin Jia ◽  
Pi-Xian Gong ◽  
Fang Wang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Schiff’S Base ◽  
E Coli ◽  
Derivatives Of ◽  
Antibacterial Evaluation ◽  
Potent Inhibitory Activity

Series of novel Schiff's base derivatives have been synthesized. Compound 10q showed the most potent inhibitory activity (IC50 = 2.6883 μM).

Pyrimidine Acyclic Nucleotide Analogues with Aromatic Substituents in C-5 Position

2007 ◽  
Vol 72 (7) ◽  
pp. 927-951 ◽  
Author(s):  
Marcela Krečmerová ◽  
Antonín Holý ◽  
Milena Masojídková
Keyword(s):  
Antiviral Activity ◽  
Cell Cultures ◽  
Inhibitory Activity ◽  
Thymidine Phosphorylase ◽  
Sodium Hydride ◽  
Phosphonic Acids ◽  
Nucleotide Analogues ◽  
Varicella Zoster ◽  
Subsequent Hydrolysis ◽  
Phosphonate Esters

NH2-protected 5-phenylcytosine and its derivatives 2a-2d were treated with (2S)-2-[(trityloxy)methyl]oxirane (3) followed by etherification with diisopropyl [(tosyloxy)methyl]phosphonate (5) in the presence of sodium hydride. The intermediary phosphonate esters 6 were debenzoylated and subsequently transformed to free phosphonic acids, i.e. (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-phenylcytosine (5-phenyl-HPMPC) derivatives (8a-8d) by the action of bromotrimethylsilane and subsequent hydrolysis. Deamination of these compounds with 3-methylbutyl nitrite afforded corresponding (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-phenyluracil (5-phenyl-HPMPU) derivatives (9a-9d). R-Enantiomers 14 and 15 were prepared analogously starting from (2R)-2-[(trityloxy)methyl]oxirane. 5-Benzyl-, 5-[(1-naphthyl)methyl]- and 5-[(2-naphthyl)methyl]HPMPU (24a-24c) and -HPMPC (25a-25c) were synthesized from appropriate 5-arylmethyl-4-methoxypyrimidin-2(1H)-ones similarly as described for 5-phenyl derivatives. Antiviral activity was found for (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-phenyluracil (9a) (HSV-1 and HSV-2) and (R)-1-[3-hydroxy2-(phosphonomethoxy)propyl]-5-phenylcytosine (14) (cytomegalovirus and varicella-zoster virus), both tested in cell cultures. Some of the 5-phenyluracil derivatives possessed inhibitory activity against thymidine phosphorylase from SD-lymphoma.

EVALUATION OF SOME MEDICINAL PLANTS AS PUTATIVE HIV-PROTEASE INHIBITORS

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 24-28
Author(s):  
A.A Rege ◽  
◽  
A. S Chowdhary
Keyword(s):  
Inhibitory Activity ◽  
In Vitro Study ◽  
Hiv Protease ◽  
Tinospora Cordifolia ◽  
Ocimum Sanctum ◽  
Hiv Protease Inhibitors ◽  
Hiv Reverse Transcriptase ◽  
Anti Hiv ◽  
Potent Inhibitory Activity

Aqueous extracts of Ocimum sanctum Linn., Tinospora cordifolia (Willd.) Miers ex Hook. f. & Thoms, Withania somnifera Dunal, Avicennia officinalis Linn. and Rhizophora mucronata Lam. were included for the present in vitro study. Pepsin was used as a substitute for HIV-protease to evaluate inhibitory activity of these extracts, as pepsin has close resemblance with HIV-protease in proteolytic activity. O. sanctum revealed the highest inhibitory activity followed by R. mucronata. In our earlier study, O. sanctum and R. mucronata exerted anti-HIV activity via multiple mechanisms of action; viz., interference with the gp120 / CD4 interaction and inhibition of HIV-reverse transcriptase. In the present study, they also showed potent inhibitory activity against pepsin enzyme (indirectly against HIV-protease) which may be due their flavonoids content.

scholarly journals Diarylheptanoids of Curcuma comosa with Inhibitory Effects on Nitric Oxide Production in Macrophage RAW 264.7 Cells

2015 ◽  
Vol 10 (1) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Nilubon Sornkaew ◽  
Yuan Lin ◽  
Fei Wang ◽  
Guolin Zhang ◽  
Ratchanaporn Chokchaisiri ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Activity ◽  
Raw 264.7 Cells ◽  
Racemic Mixture ◽  
Raw 264.7 ◽  
Nitric Oxide Production ◽  
Inhibitory Effects ◽  
Curcuma Comosa ◽  
Oxide Production ◽  
Potent Inhibitory Activity

Eight new diarylheptanoids, a 1.2:1 mixture of (3S)- and (3 R)-1-(4-hydroxyphenyl)-7-phenyl-(4 E,6 E)-4,6-heptadien-3-ol (1a and 1b), a racemic mixture of (3S)- and (3 R)-1-(4-hydroxyphenyl)-3-methoxy-7-phenyl-(4 E,6 E)-4,6-heptadiene (2a and 2b), a ca. 1:1 mixture of (3S)- and (3 R)-1-(4-hydroxy-3-methoxyphenyl)-3-methoxy-7-phenyl)-(4 E,6 E)-4,6-heptadiene (3a and 3b), 3-acetoxy-1-(3,4-dihydroxyphenyl)-7-phenylheptan-5-ol (4), (3 R)-1-(4,5-dihydroxyphenyl)-7-phenyl-(6 E)-6-hepten-3,2′-epoxide (5), and thirteen known diarylheptanoids, 6-12, a 3:1 mixture of 13a and 13b, and 14-17, were isolated from the rhizomes of Curcuma comosa from Sakon Nakhon, northeastern part of Thailand. The isolated compounds were evaluated for their antiinflammatory activities on the inhibition of lipopolysaccharide-induced nitric oxide production in macrophage RAW 264.7 cells and the diarylheptanoids 1a and 1b mixture and 14 exhibited potent inhibitory activity.

scholarly journals INHIBITION ACTIVITY OF CLEOME SPECIES EXTRACT ON ONION GUEST ROOT

2019 ◽  
pp. 1-2
Author(s):  
SUTTHIDUEAN CHUNHAKARN ◽  
PRAKAIDAO YINGSANGA ◽  
LADA MATHURASA
Keyword(s):  
Root Growth ◽  
Ethyl Acetate ◽  
Crude Extract ◽  
Inhibitory Activity ◽  
Crop Productivity ◽  
Distilled Water ◽  
Crude Extracts ◽  
Cleome Spinosa ◽  
Whole Plants ◽  
Potent Inhibitory Activity

Objective: Biological control is useful in agricultural. Allelopathy plays an important factor in crop productivity. The effect of allelopathy is able to produce and release allelochemicals or phytochemicals to inhibit or stimulate seed germination, seeding growth, shoot and root growth of other crops. The aim of this study was to evaluate the inhibitory activity of Cleome viscose and Cleome spinosa extracts on onion guest roots length.Methods: The whole plants of C. viscose and C. spinosa were extracted with dichloromethane, ethyl acetate, methanol and distilled water, respectively. Each group of onion guests was sprayed at various concentrations as 100, 200, 400, 800 and 1600 parts per million for the treatment. The root growth was measured every day for 1 month.Results: At concentration of 1600 ppm, methanol crude extract of C. spinose showed the highest percent inhibitory activity value of 91.68. Ethyl acetate and methanol crude extracts of C. viscose showed strong inhibitory activity with percentage values of 90.17 and 90.90, respectively, at concentration of 1600 ppm. Moreover, the methanol extract of C. viscose and C. spinosa evaluated higher inhibitory activity than other solvent. However, distilled water crude extract of C. spinose showed weak inhibitory activity with the percentage value of 40.05 at concentration of 1600 ppm.Conclusions: In this study, the methanol crude extract of C. spinose showed potent inhibitory activity on root growth. Moreover, ethyl acetate and methanol crude extracts of C. viscose evaluated strong inhibitory activity. C. viscose and C. spinosa extracts possessed allelochemicals for postharvest biology and technology in plants.

scholarly journals Potent inhibitory activity of HSR-6071, a new antiallergic agent, on Passive Cutaneous Anaphylaxis(PCA).

1990 ◽  
Vol 52 (1) ◽  
pp. 87-94 ◽  
Author(s):  
Eiichi MAKINO ◽  
Tetsuo OHASHI ◽  
Hiromi TAKAHASHI ◽  
Hideo KATO ◽  
Yasuo ITO ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Passive Cutaneous Anaphylaxis ◽  
Antiallergic Agent ◽  
Potent Inhibitory Activity
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