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Obtainment of semi-synthetic derivatives

Keywords Lignans; Piper cubeba; (-)-cubebin; Semisynthetic derivatives; Antibacterial activity

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to form pyrazole derivatives of piperine.

KCSR (PhD student) isolated the precursor from the plant, synthesized the derivatives, evaluated the biological activity, running the laboratory work, analyzing data and drafted the paper. RL (PhD student) contributed to biological assays. GVS (PhD student) contributed to chromatographic analysis of plant material. PMP and AHJ contributed to critical reading of the manuscript. VRE and CHGM contributed to biological assays. MAS contributed to isolation and identification of compounds. WRC contributed to the identification of derivatives. JKB contributed to critical reading of the manuscript. MLAS designed the study and supervised the laboratory. All the authors have read the final manuscript and approved the submission.

Synthesis and Antileishmanial activity of Piperoyl-Amino ..

L. is examined as the king of species worldwide by virtue of its principle piperine. In Ayurveda, since from the ancient times, it is known as “Yogvahi”. It is one of the important alkaloids of Pepper fruits (Family Piperaceae) and has been found to have numerous medicinal properties such as antioxidant, antiplatelet, anti-inflammatory, antihypertensive, hepatoprotective, antithyroid, antitumor, antiasthmatic activity and also have significant role as fertility enhancer. The present review discusses the biosynthetic pathway, extraction process, chemistry and various analytical methods of piperine. It also describes the structural modification of piperine and its various effects on biological system. The utility of piperine as a bioenhancer for certain antibacterial- antibiotics and a potent inhibitor of drug metabolism are also discussed. Thus, review provides knowledgeable erudition on the piperine which paves way for further work.

the synthesis of derivatives ..

In general, tablets containing one or more of the piperazine derivatives have a similar price to ecstasy, typically EUR 3–4 a tablet.

13077 (2015).By structural modification of piperine, some piperine-basedphenylsulfonylhydrazone derivatives exhibited an unprecedented andpotent narcotic activity against the oriental armyworm, Mythimnaseparata (Walker).

studied the antimicrobial activity of derivatives of 1 extracted from Piper cubeba, compared to other oral micro-organisms. The antimicrobial activity was tested on seven of the oral cavity pathogens: Enterococcus faecalis, Streptococcus salivarius, Streptococcus sanguinis, Streptococcus mitis, Streptococcus mutans, Streptococcus sobrinus and Candida albicans. The compounds were effective on most of the pathogens studied.

Synthesis of Hydrazine Derivatives ..

Contaminants resulting from the synthesis of 3,4-(methylenedioxy)amphetamine (MDA) via condensation between nitroethane and piperonal].

Synthetic procedures and characterizationdata for piperine analogues; shell script for evaluation of costs;Python script to divide MACCS fingerprints into bite strings; parametersobtained for model 3; full composition of 10 trees in model 4; anda table with the full list of descriptors calculated. This materialis available free of charge via the Internet at .

One hundred forty-three 2D descriptorsimplemented in MOE were calculated. The full list is provided in (Table S1A). Descriptorsshowing no variance were removed from the data set, and the remaining125 descriptors (, Table S1B) underwent feature selection by the BestFirst algorithmimplemented in the software package WEKA version 3.7.9. Consequently,the six descriptors left (set 6D) were used for further classificationstudies (Table ). Additionally, as a referencedescriptor set, we used 11 descriptors of physicochemical properties(set PHYSCHEM) from the list of 125 descriptors described above (Table ). These descriptors allow us to trace molecularfeatures important for biological activity and have previously showngood performance in application to ligand-based studies. As an attempt to trace the structural featuresrelevant to the activity of piperine derivatives, MACCS fingerprints(MACCS Keys; MDL Information Systems, Inc., San Leandro, CA) werecomputed in MOE. MACCS are a set of structural keys, where each keydescribes a small substructure consisting of up to 10 non-hydrogenatoms. A Python script () was applied to divide the fingerprints into bit strings. The latterwere further used in the classification studies as descriptor set“MACCS”.

Efficiency of piperine derivatives was ..
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PDF Downloads : Oriental Journal of Chemistry

There are no readily-available screening tests for CPP or the other phenylpiperazine derivatives. In the mass spectrum, the principal ions (m/z) of CPP are 154 (base peak), 196, 156, 56 and 138. However, mass spectrometry does not distinguish CPP from its isomers (oCPP and pCPP).

NSAIDs (Ibuprofen, Naproxen, Aspirin) and …

In illicit products, the typical dose of BZP ranges from 50 to 200 mg. In Europe, BZP is often found in combination with other piperazine derivatives (e.g. CPP, TFMPP, DBZP) and less commonly mixed with other well-known substances such as , , ketamine and caffeine. A study in Belgium conducted by the Scientific Institute of Public Health reported that the amount of CPP in tablets in 2008 was between 90 and 110 mg for more than 40 % of cases (of 32 samples). For comparison, when used in psychiatry in challenge tests of the serotonin system, the dose of CPP is typically 50 mg for a 70 kg person.

Naturopathic Causes and Treatment of Erectile Dysfunction

Recent publications have highlighted the numerous biological activities attributed to the lignan (-)-cubebin (1), Piper cubeba L. f., Piperaceae, and ongoing studies have focused on its structural optimization, in order to obtain derivatives with greater pharmacological potential. The aim of this study was the obtainment of (1), its semisynthetic derivatives and evaluation of antibacterial activity. The extract of the seeds of P. cubeba was chromatographed, subjected to recrystallization and was analyzed by HPLC and spectrometric techniques. It was used for the synthesis of: (-)-O-methylcubebin (2), (-)-O-benzylcubebin (3), (-)-O-acetylcubebin (4), (-)-O-(N, N-dimethylamino-ethyl)-cubebin (5), (-)-hinokinin (6) and (-)-6.6'-dinitrohinokinin (7). The evaluation of the antibacterial activity has been done by broth microdilution technique for determination of the minimum inhibitory concentration and the minimum bactericidal concentration against Porphyromonas gingivalis, Prevotella nigrescens, Actinomyces naeslundii, Bacteroides fragilis and Fusobacterium nucleatum. It was possible to make an analysis regarding the relationship between structure and antimicrobial activity of derivatives against microorganisms that cause endodontic infections. The most promising were minimum inhibitory concentration =50 µg/ml against P. gingivalis by (2) and (3), and minimum inhibitory concentration =100 µg/ml against B. fragilis by (6). Cytotoxicity assays demonstrated that (1) and its derivatives do not display toxicity.

16/12/2017 · Synthesis and Biological Evaluation of ..

Antibacterial activity of (-)-cubebin isolated from Piper cubeba and its semisynthetic derivatives against microorganisms that cause endodontic infections

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