scholarly journals Synthesis of 2-{[2-(2-oxo-1-azacycloalkyl)acetamido]phenoxy}acetic acids and their activity as aminopeptidase M inhibitors

2008 ◽  
Vol 73 (8-9) ◽  
pp. 771-780
Author(s):  
Oldřich Farsa ◽  
Milan Dockal ◽  
Jana Kováciková ◽  
Mária Benesová

A series of 9 phenoxyacetic acids substituted in the o-, m-, and p-position of benzene ring with 2-(2-oxo-1-azacycloalkyl)acetamidic moiety containing 5-7-membered ?-lactam ring was prepared by a 4-step synthetic procedure. Five selected substances of this series were tested in vitro for inhibition of porcine kidney aminopeptidase M. 2-{4-[2-(2-Oxoperhydroazepin-1-yl)acetamido]phenoxy}acetic acid exhibited the highest activity with Ki = 243.6 ?M.

2009 ◽  
Vol 24 (3) ◽  
pp. 876-882 ◽  
Author(s):  
M. Shahar Yar ◽  
M. Afroz Bakht ◽  
A. A. Siddiqui ◽  
M. M. Abdullah ◽  
Erik De Clercq

2009 ◽  
Vol 24 ◽  
pp. 82-88 ◽  
Author(s):  
Saraswoti Aryal ◽  
Sanu Devi Joshi

Rauvolfia serpentina (L.) ex. Kurz is an important medicinal plant. Callus induction and regeneration was studied from stem explant of in-vitro grown plant of Rauvolfia serpentina(L.) Benth. ex Kurz (Apocynaceae) on Murashige Skoog (1962) medium supplemented with 1mg/l 2,4-Dichlorophenocy acetic acid (2,4-D) and 1mg/l Kinetin (Kn). Vigorous growth of callus occurs after 4 weeks of culture. Callus was sub-cultured on Murashige and Skoog (MS) medium supplemented with different concentration of 2, 4-D (0.5-3.0 mg/l) and 10% coconut milk. Regeneration of plantlets occurred on MS medium containing 3 mg/1 of 2, 4-D and 10% coconut milk. These plantlets were rooted on MS medium supplemented with 1 mg/l IAA .The regenerated plantlets were able to grow on soil after short period ofacclimatization. Key words: Explant; In-vitro culture; MS medium;  2, 4 Dichlorophenoxy acetic acid; Kinetin; Callus; Tissue culture; Coconut milk. Journal of Natural History Museum Vol. 24, 2009 Page: 82-88


Author(s):  
Roshni Jha ◽  
Anjali Minj
Keyword(s):  

A changed Pulsincap measurements type of metronidazole was created to target tranquilize discharge in the colon. Groups of hard gelatin cases were treated with formaldehyde keeping the tops in that capacity. Metronidazole pellets arranged by expulsion spheronization technique were consolidated into these particular container shells and stopped with polymers guar gum, hydroxypropylmethylcellulose 10K, carboxymethylcellulose sodium and sodium alginate independently at fixations 20 mg, 30 mg and 40 mg. The filled cases were totally covered with 5% cellulose acetic acid derivation phthalate to forestall variable gastric purging. All the definitions were tested to decide sedate substance and the capacity of the adjusted Pulsincap to give colon-explicit medication conveyance was surveyed by in vitro tranquilize discharge concentrates in cushion pH 1.2 for 2 h, pH 7.4 (reproduced intestinal liquid) for 3 h and pH 6.8 (animated colonic liquid) for 7 h. The outcomes showed that critical medication discharge happened simply after 5 h from the beginning of analysis.


2020 ◽  
Vol 20 (1) ◽  
pp. 69-75
Author(s):  
Santi M. Mandal ◽  
Subhanil Chakraborty ◽  
Santanu Sahoo ◽  
Smritikona Pyne ◽  
Samaresh Ghosh ◽  
...  

Background: The need for suitable antibacterial agents effective against Multi-drug resistant Gram-negative bacteria is acknowledged globally. The present study was designed to evaluate the possible antibacterial potential of an extracted compound from edible flowers of Moringa oleifera. Methods: Five different solvents were used for preparing dried flower extracts. The most effective extract was subjected to fractionation and further isolation of the active compound with the highest antibacterial effect was obtained using TLC, Column Chromatography and reverse phase- HPLC. Approaches were made for characterization of the isolated compound using FTIR, NMR and Mass spectrometry. Antibacterial activity was evaluated according to the CLSI guidelines. Results: One fraction of aqueous acetic acid extract of M. oleifera flower was found highly effective and more potent than conventional antibiotics of different classes against Multi-drug resistant Gram-negative bacilli (MDR-GNB) when compared. The phytochemical analysis of the isolated compound revealed the presence of hydrogen-bonded amine and hydroxyl groups attributable to unsaturated amides. Conclusion: The present study provided data indicating a potential for use of the flowers extract of M. oleifera in the fight against infections caused by lethal MDR-GNB. Recommendations: Aqueous acetic acid flower extract of M. oleifera is effective, in-vitro, against Gram-negative bacilli. This finding may open a scope in pharmaceutics for the development of new classes of antibiotics.


Soil Systems ◽  
2021 ◽  
Vol 5 (2) ◽  
pp. 26
Author(s):  
Rihab Djebaili ◽  
Marika Pellegrini ◽  
Massimiliano Rossi ◽  
Cinzia Forni ◽  
Maria Smati ◽  
...  

This study aimed to characterize the halotolerant capability, in vitro, of selected actinomycetes strains and to evaluate their competence in promoting halo stress tolerance in durum wheat in a greenhouse experiment. Fourteen isolates were tested for phosphate solubilization, indole acetic acid, hydrocyanic acid, and ammonia production under different salt concentrations (i.e., 0, 0.25, 0.5, 0.75, 1, 1.25, and 1.5 M NaCl). The presence of 1-aminocyclopropane-1-carboxylate deaminase activity was also investigated. Salinity tolerance was evaluated in durum wheat through plant growth and development parameters: shoot and root length, dry and ash-free dry weight, and the total chlorophyll content, as well as proline accumulation. In vitro assays have shown that the strains can solubilize inorganic phosphate and produce indole acetic acid, hydrocyanic acid, and ammonia under different salt concentrations. Most of the strains (86%) had 1-aminocyclopropane-1-carboxylate deaminase activity, with significant amounts of α-ketobutyric acid. In the greenhouse experiment, inoculation with actinomycetes strains improved the morpho-biochemical parameters of durum wheat plants, which also recorded significantly higher content of chlorophylls and proline than those uninoculated, both under normal and stressed conditions. Our results suggest that inoculation of halotolerant actinomycetes can mitigate the negative effects of salt stress and allow normal growth and development of durum wheat plants.


Animals ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 108
Author(s):  
Yichong Wang ◽  
Sijiong Yu ◽  
Yang Li ◽  
Shuang Zhang ◽  
Xiaolong Qi ◽  
...  

Nutritional strategies can be employed to mitigate greenhouse emissions from ruminants. This article investigates the effects of polyphenols extracted from the involucres of Castanea mollissima Blume (PICB) on in vitro rumen fermentation. Three healthy Angus bulls (350 ± 50 kg), with permanent rumen fistula, were used as the donors of rumen fluids. A basic diet was supplemented with five doses of PICB (0%–0.5% dry matter (DM)), replicated thrice for each dose. Volatile fatty acids (VFAs), ammonia nitrogen concentration (NH3-N), and methane (CH4) yield were measured after 24 h of in vitro fermentation, and gas production was monitored for 96 h. The trial was carried out over three runs. The results showed that the addition of PICB significantly reduced NH3-N (p < 0.05) compared to control. The 0.1%–0.4% PICB significantly decreased acetic acid content (p < 0.05). Addition of 0.2% and 0.3% PICB significantly increased the propionic acid content (p < 0.05) and reduced the acetic acid/propionic acid ratio, CH4 content, and yield (p < 0.05). A highly significant quadratic response was shown, with increasing PICB levels for all the parameters abovementioned (p < 0.01). The increases in PICB concentration resulted in a highly significant linear and quadratic response by 96-h dynamic fermentation parameters (p < 0.01). Our results indicate that 0.2% PICB had the best effect on in-vitro rumen fermentation efficiency and reduced greenhouse gas production.


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