Synthesis Characterization and Antibacterial Activity of Terazosin Hydrochloride Drug and Market Formulation

Author(s):  
Anshul Kumar ◽  
Rajnish Kumar ◽  
Avijit Mazumdar

Terazosin hydrochloride is an anti-hypertensive drug which is used to treat the diseases of hypertension. The literature survey shows the proposed synthesis of Terazosin hydrochloride derived from the starting material of 2-chloro-6, 7-dimethoxy–quinazoline-4-amine in the presence of 2-methoxy ethanol with n- benzyl piperazine to form the product. The Terazosin derivatives were prepared with the help of literature survey were 1, 4-bis-(furan-2-yl-carbonl) piperazine, 1, 4-bis-(tertrahydrofuran-2-yl) carbonyl piperazine, and 1-(4-amino-6, 7-dimethoxy- quinazoline-2-yl)- 4-formyl- piperazine were prepared by maintaining environmental condition. The characterization done for prepared derivative was done through 1H-NMR, MASS and IR Spectroscopy. The antibacterial activity of prepared derivatives was performed on the various bacteria like E. coli, Pseudomonas aeruginosa, Shigella sonneii, Klebsiella pneumonia, Staphylococcus aureus, Shigella flexneri, Vibrio cholera, Bacillus subtilis, Pseudomonas fluorescens, Pseudomonas aeruginosa, Staphylococcus aureus. The desired derivatives shown maximum zone of inhibition using concentration prepared 100µg and 200µg using standard drug. The derivatives that shows maximum inhibition 6, 7-dimethoxy-2-piperazine-1-yl-quinazoline -4-amine and minimum was shown by 1, 4-bis-(furan-2-yl-carbonl) piperazine, 1,4-bis-(tertrahydrofuran- 2-yl) carbonyl piperazine. The result should that prepared Terazosin derivatives shows potent actively when compared with standard ciprofloxacin.

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5437
Author(s):  
Mohammed Kara ◽  
Amine Assouguem ◽  
Omkulthom Mohamed Al kamaly ◽  
Safaâ Benmessaoud ◽  
Hamada Imtara ◽  
...  

Apple vinegar is a natural product widely used in food and traditional medicine as it contains many bioactive compounds. The apple variety and production methods are two factors that play a major role in determining the quality of vinegar. Therefore, this study aims to determine the quality of apple vinegar samples from different varieties (Red Delicious, Gala, Golden Delicious, and Starking Delicious) prepared by three methods using small apple pieces, apple juice, and crushed apple, through determining the physicochemical properties and antibacterial activity of these samples. The antibacterial activity was studied against five pathogenic bacteria: Staphylococcus aureus, Klebsiella pneumonia, Escherichia coli (ATB: 57), Escherichia coli (ATB: 97), and Pseudomonas aeruginosa, using two methods, disk diffusion and microdilution, for determining the minimum inhibitory concentrations and the minimum bactericidal concentrations. The results of this study showed that the lowest pH value was 3.6 for Stark Delicious, obtained by liquid fermentation, and the highest acetic acid values were 4.7 and 4% for the vinegar of Red Delicious and Golden Delicious, prepared by solid fermentation, respectively. The results of the antibacterial activity showed considerable activity of apple vinegar on the tested strains. Generally, the Staphylococcus aureus strain appears less sensitive and Pseudomonas aeruginosa seems to be very sensitive against all samples, while the other strains have distinct sensitivities depending on the variety studied and the method used. A higher antibacterial activity was found in vinegar obtained by the apple pieces method and the Red Delicious variety, with a low MIC and MBC recorded, at 1.95 and 3.90 µL/mL, respectively. This study has shown that the choice of both apple variety and production method is therefore an essential step in determining and aiming for the desired quality of apple vinegar.


2009 ◽  
Vol 6 (3) ◽  
pp. 743-746 ◽  
Author(s):  
T. Arunachalam ◽  
R. Bhakyaraj ◽  
A. K. Sasi

Metal complex of Mn(II), Co(II), Ni(II) and Cu(II) with benzoic acid have been prepared and characterized by physiochemical methods. On the basis of electronic spectra and magnetic susceptibility measurement in conjunction with infrared spectra, six coordinated octahedral structure have been proposed to all the complexes. The benzoic acid and their complexes have been tested for their antibacterial activity against the bacteriaE. coli,Bacillus subtilis,Pseudomonas aeruginosaandStaphylococcus aureus. Further, the non electrolytic nature of all the synthesized complexes was identified from conductivity measurements.


2017 ◽  
Vol 9 (1) ◽  
Author(s):  
Lalit Yadav ◽  
Ravi Mani Tripathi ◽  
Ram Prasad ◽  
Ramesh Namdeo Pudake ◽  
Jagjiwan Mittal

2018 ◽  
Vol 14 (1) ◽  
pp. 179
Author(s):  
Ika Prestianti ◽  
Maswati Baharuddin ◽  
Sappewali Sappewali

<p>Penyakit infeksi akibat bakteri merupakan masalah serius dalam kesehatan. Antibakteri alami yang dapat digunakan untuk menghambat pertumbuhan bakteri yaitu sarang lebah hutan (<em>Apis dorsata</em>) (propolis, kantong madu, kantong telur dan kantong pollen) yang mengandung senyawa metabolit sekunder seperti flavonoid, tanin dan asam fenolat.Tujuan dari penelitian ini adalah megetahui aktivitas antibakteri ekstrak sarang lebah hutan dari setiap pelarut yang digunakan dan untuk mengetahui pengaruh konsentrasi ekstrak sarang lebah hutan terhadap pertumbuhan bakteri <em>Staphylococcus aureus, Escherichia coli </em>dan<em> Pseudomonas aeruginosa</em>. Pengujian antibakteri dilakukan dengan metode difusi kertas cakram dengan lama perendaman   1 jam kemudian diinkubasi selama 3 x 24 jam. Hasil penelitian menunjukkan bahwa aktivitas antibakteri ekstrak metanol sarang lebah memiliki aktivitas tertinggi pada bakteri  <em>E. coli </em>yaitu 3,8 mm pada konsentrasi 8%, ekstrak etil asetat sarang lebah pada bakteri <em>S. a ureus </em>yaitu 3,72 mm pada konsentrasi 8% dan ekstrak n-heksan sarang lebah pada bakteri <em>E. coli </em>yaitu 16,1 mm pada konsentrasi 8%. Pengaruh konsentrasi ekstrak yaitu semakin tinggi konsentrasi ekstrak maka semakin besar pula daya hambat ekstrak terhadap pertumbuhan bakteri <em>S</em>.<em> aureus, E</em>.<em> coli </em>dan<em> P</em>.<em> aeruginosa</em>.</p><p><strong>Antibacterial Evaluation of Extract Beehive (<em>Apis dorsata</em>) on Growth <em>Staphylococcus aureus</em>, <em>Escherichia coli</em> and <em>Pseudomonas aeruginosa</em></strong>. Bacterial infectious diseases are serious health problems. One of natural antibacterial that can be used to inhibit bacterial growth is honeycomb (propolis, honey bag, egg bag and pollen bag) containing secondary metabolite compounds such as flavonoids, tannins and phenolic acids. The purpose of this research is to know the antibacterial activity of honeycomb extract from each solvent used and to know the effect of honeycomb extract concentration on the growth of <em>S</em>.<em> aureus</em>, <em>E</em>. <em>coli</em> and <em>P</em>.<em> aeruginosa</em> bacteria. Antibacterial testing was performed by the method of paper disc diffusion with soaking time 1 hour then incubated for 3 x 24 hours. The results showed that antibacterial activity of methanol honeycomb extract had the highest activity in <em>E. coli</em> bacteria i.e., 3.8 mm at 8% concentration, ethyl acetate honey extract on <em>S. aureus</em> bacteria ie 3.72 mm at 8% concentration and n extract n-hexan honeycomb in <em>E. coli</em> bacteria that is 16,1 mm at 8% concentration. The higher extract concentration the greater the inhibitory activity of extract on the growth of <em>S</em>.<em> aureus</em>, <em>E. coli</em> and <em>P</em><em>.</em><em> aeruginosa</em> bacteria.</p>


2019 ◽  
Vol 62 (2) ◽  
pp. 97-100
Author(s):  
Taif Shah ◽  
Niyaz Ali ◽  
Zahir Shah ◽  
Azam Hayat

The current study was conducted to determine the antibacterial activity of 50 crude and processed honey samples produced by Apis mellifera and stingless bee. All the honey samples were collected from different places of Districts Dir, Swat and Oghi of Khyber Pakhtunkhwa Province, Pakistan and were tested against the six ATCC bacterial species including E. coli ATCC number 25922, Pseudomonas aeruginosa ATCC number 27853, Staphylococcus aureus ATCC number 6538, Enterococcus faecalis ATCC number 19433, Salmonella typhi ATCC number 19943 and Klebsiella pneumoniae ATCC number 27736. The honey samples showed variable zones of inhibition by using Agar well plate technique. E. coli showed 17-23 mm, S. typhi 31-37 mm, E. faecalis 28 mm, P. aeruginosa 14-15 mm, K. pneumoniae 20-24 mm and Staph. aureus 19-25 mm. Most of the honey samples used in this study showed broad spectrum antibacterial activity.


2017 ◽  
Vol 9 (4) ◽  
pp. 619
Author(s):  
Fatehi Naima ◽  
Houcine BENMEHDI ◽  
Allali Hocine ◽  
Oulednecir Nawal

<p>The initial introduction of new medicinal agents into the health care system sometimes, requires information beyond that is recorded in libraries relying instead, on reports available through traditions and healers within a society. This paper explored the antibacterial activity of aqueous and hydromethanolic extracts of nine folkloric medicinal plant from Bechar region (southwest Algeria) namely: <em>A. nardus, A. schoenanthus, G. vulgaris, </em>two species of<em> H. scoparia green &amp; red, P. laevigata, R. tripartita, T. gallica</em> and <em>T. nudatum</em>, frequently used in the local traditional medicine. The antibacterial activity of different extracts were evaluated by using disc diffusion method agar and antibiotics susceptibility of ten selected microorganisms: seven reference strains, <em>Bacillus cereus, Enterococcus faecalis, Staphylococcus aureus</em>,<em> Escherichia coli</em>,<em> Klebsiella pneumoniae, Pseudomonas aeruginosa</em>, <em>Salmonella typhi</em>, and three clinically isolated strains, <em>Escherichia coli</em> (Urinary Tract Infection), <em>Escherichia coli</em> (Vaginal Infection) and <em>Staphylococcus aureus </em>(Skin Infection).</p><p>The maximum antibacterial activity was recorded against the gram negative reference strains <em>Pseudomonas aeruginosa</em>and<em> Escherichia coli</em> with a maximum inhibition diameter of 15.6 ± 0.5 and 15.0 ± 1.4 mm respectively displayed by the aqueous extract of <em>T. gallica, </em>followed by the activity detected by the hydromethanolic extract of <em>R. tripartita</em> against the gram negative reference strain <em>Pseudomonas aeruginosa </em>(14.6±1.2 mm) and the aqueous and hydromethanolic extracts of <em>R. tripartita</em> against the gram negative reference strains <em>Pseudomonas aeruginosa</em> and<em> Escherichia coli</em> with a maximum inhibition diameter of 14.3 ± 2.0 and 14.3±0.5 mm, respectively.</p><p>According to the present study, <em>H. scoparia red, P. laevigata, R. tripartita, and T. gallica</em>can be served as broad spectrum antibiotic and used as a potent source of natural antibacterial agents by replacing commercially available synthetic drug that may have a large number of side effects.</p>


Author(s):  
В.Т. Долгих ◽  
Л.Г. Пьянова ◽  
Т.И. Долгих ◽  
В.А. Лихолобов ◽  
О.В. Корпачева ◽  
...  

Цель исследования - изучение антибактериальной активности гранулированных углеродных сорбентов по отношению к патогенной микрофлоре в условиях различной продолжительности контакта с сорбентом. Методика. Исследовали антибактериальные свойства гранулированного сорбента ВНИИТУ-1, обработанного гидромеханически, окисленного и стабилизированного до нормативных значений рН и модифицированного поли-N-винилпирролидоном (ПВП) ВНИИТУ-1 по отношению к патогенным микроорганизмам: Staphylococcus aureus, Pseudomonas aeroginosa, Klebsiella pneumonia, Escherichia coli, Streptococcus agalactiae, а также к их смесям. Все микроорганизмы представляли собой клинические штаммы, выделенные из ран пациентов. Предварительно тест-микроорганизмы были исследованы на чувствительность к современным антибиотикам. Опытным путем подбирали такие разведения и количество засеваемого материала, чтобы выросшие на чашке Петри колонии можно было сосчитать. Бактерии сорбировали из физиологического раствора с концентрацией микробных клеток 3 х 10 колониеобразующих единиц в 1 мл исследуемой пробы (КОЕ/мл). В пробирку типа Эппендорф вносили сорбент в количестве 0,5 мл, добавляли 1 мл микробной взвеси, встряхивали для удаления пузырьков воздуха и выдерживали в термостате в течение 1, 3, 6 и 24 ч. По истечении заданного времени контакта сорбента с патогенной микрофлорой отбирали надосадочную жидкость в объеме 100 мкл, засевали на стерильные агаровые пластины чашек Петри с питательной средой ГМФ-агар. Засеянные чашки Петри помещали в СО-инкубатор 15АС (Япония) вверх дном и инкубировали при температуре 37 ± 1°С в течение 24 ± 2 ч. При подсчете колоний, выросших на чашке Петри, учитывали только те чашки, на которых выросло более 300 изолированных колоний. Результаты. Гранулированный сорбент ВНИИТУ-1 обладает антибактериальным действием в отношении как грамположительных, так и грамотрицательных бактерий, а также их смеси. Сроки проявления антибактериального эффекта сорбента зависят от вида микроорганизмов и времени их контакта с образцом. Присутствие в составе сорбента модификатора ПВП усиливает его антибактериальные свойства. Полимермодифицированный образец обладает пролонгированным антибактериальным эффектом в отношении широкого спектра микроорганизмов (E. coli, St. aureus, P. aeruginosae и St. aureus) и смеси их культур. Заключение. Показана возможность повышения антибактериальных свойств гранулированных углеродных сорбентов по отношению к патогенной микрофлоре путем их модификации поли-N-винилпирролидоном. Дальнейшая разработка и применение углеродных сорбентов как средств сорбционной терапии является перспективным подходом к местному лечению гнойных ран. The purpose: Study the antibacterial activity of granulated carbon sorbents in relation to the pathogenic microflora under the conditions of different period of contact with sorbent. Methods. It has been investigated the antibacterial properties of VNIITU-1 granulated sorbent, which was hydromechanically treated, oxidized and stabilized up to pH standard parameters and VNIITU-1 modified poly-N-vinylpyrrolidone (PVP) against the pathogenic micro-organisms, including Staphylococcus aureus, Pseudomonas aeroginosa, Klebsiella pneumonia, Escherichia coli, Streptococcus agalactiae, and their mixes. All bacteria were clinical strains derived from the wounds of patients. Dilutions and amount of inoculated material were experimentally selected for further calculation of the grown colonies on the Petri dish. Bacteria were sorbed from the saline solution with bacteria concentration of 3 х 10 of the colony forming units in 1 ml of test sample (CFU/ ml). Eppendorf tube was added the sorbent 0.5 ml and bacterial suspension 1 ml; then the tube was shaken to remove the air bubbles and incubated for 1, 3, 6 and 24 hr. Upon the expiry of the target time for sorbent with pathogenic flora contact the supernatant fluid was collected in 100 ul and inoculated on the sterile agar plates of the Petri dishes with GMF agar nutrient medium. Inoculated Petri dishes were placed upside down in СО incubator 15AC (Japan) and incubated at 37 ± 1°C for 24 ± 2 hours. When counting the colonies growing on the Petri dish, they took into consideration only the dishes where more than 300 isolated colonies were grown. If more than 300 colonies were grown, «> 3x102 CFU/ml» was recorded in the protocol. Results. Granulated sorbent VNIITU-1 has an antibacterial effect against both gram-positive and gram-negative bacteria, and their mixes. Time period for manifestations of the sorbent antibacterial effect depends on the type of microorganisms and time of contact. PVP presence in sorbent composition enhances the antibacterial effect of the sorbent. Resin-modified sample has a prolonged antibacterial effect against a broad spectrum of microorganisms (E. coli, St. aureus, P. aeruginosae and St. aureus) and mixtures of their cultures. Conclusion. It has been determined the possibility for increasing of antibacterial properties of granulated carbon sorbents against the pathogenic microflora by their modification with poly-N-vinylpyrrolidone. Further development and application of carbon sorbents as the means for sorption therapy is a perspective approach for the local treatment of purulent wounds.


2019 ◽  
Vol 31 (2) ◽  
pp. 125-130

This study aimed to determine antimicrobial activity of extracts of Tamarindus indica L. leaves (Magyee). It was the laboratory-based quasi experimental study design. Study sites were the University of Pharmacy (Mandalay and Yangon) and the Department of Medical Research (Yangon). The leaves of Tamarindus indica L. were extracted with petroleum ether, ethanol and distilled water by successive Soxhlet extraction method. Physicochemical and phytochemical studies were conducted according to reference analytical procedures. In vitro antimicrobial activity of three extracts of Tamarindus indica L. leaves were studied on control strains of bacteria (Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Klebsiella pneumoniae) by agar disc diffusion method. Phytochemical analysis of Tamarindus indica L. leaves showed the presence of alkaloids, amino acids, carbohydrates, flavonoids, glycosides, polyphenol, starches, steroids/terpenoids, tannins, reducing sugars and anthroquinone. Ethanolic and aqueous extracts exhibited significant antibacterial activities against Pseudomonas aeruginosa and Staphylococcus aureus. Both aqueous and ethanolic extracts possessed promising antibacterial activity on Pseudomonas aeruginosa and Staphylococcus aureus. This was an important finding upon pathogenic organisms causing food-borne diseases, skin and soft tissue infection. The petroleum ether extract did not show antibacterial activity against all tested organisms. With ethanolic extracts, the minimum inhibitory concentrations (MIC) results were 6.25 mg/ml for P. aeruginosa, S. aureus and 25 mg/ml for E. coli. For aqueous extracts, the MIC of P. aeruginosa and S. aureus were 12.5 mg/ml and K. pneumoniae was 25 mg/ml, respectively. Oral acute administration of 5000 mg/kg mice body weight of ethanolic and aqueous extracts of Tamarindus indica L. leaves resulted in no mortality. Therefore, the crude extracts from Tamarindus indica L. leaves had antimicrobial activity against K. pneumoniae, P. aeruginosa, S. aureus and E. coli.


2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Amal Ramzi ◽  
Bouchra Oumokhtar ◽  
Yassine Ez zoubi ◽  
Touria Filali Mouatassem ◽  
Moussa Benboubker ◽  
...  

Background. The microbiological risk of the hospital environment, including inert surfaces, medical devices, and equipment, represents a real problem. Objective. This study is aimed at demonstrating and assessing the antibacterial activity of three synthetic disinfectants classified as quaternary ammoniums on different bacterial strains (Gram-negative and Gram-positive like Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Staphylococcus aureus) isolated from the hospital environment. The reference strains included Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 29213, and Pseudomonas aeruginosa ATCC 27853 used as negative control strains. Method. Three quaternary ammonium disinfectants were tested: DDN9® (0.5%) which contains didecylmethylpolyoxyethylammonium propionate as an active substance, spray (0.4%) containing quaternary ammonium compounds, and Phagosurf ND® (0.4%) with didecyldimethylammonium chloride. Their effect was evaluated using the disk diffusion technique and the broth dilution methods, allowing the Minimum Inhibitory Concentration (MIC) and then the Minimum Bactericidal Concentration (MBC). Result. Only the growth of Gram-positive bacteria and some strains of Gram-negative bacteria were inhibited by the three synthetic disinfectants. NDD9® demonstrated an antibacterial effect only against the Gram-positive strains (S. aureus and S. aureus ATCC 29213) with a MIC of 0.25 mg/ml. The disinfectant spray showed effect against all four strains including E. coli (9), S. aureus, E. coli ATCC 25922, and P. aeruginosa ATCC 27853 with an inhibitory concentration of 4 mg/ml, while the growth of S. aureus ATCC 29213 was inhibited at 2 mg/ml. The third disinfectant, Phagosurf ND®, inhibited only the growth of S. aureus ATCC 29213 at a MIC of 4 mg/ml. Conclusion. This study is the first here in Morocco to evaluate the bacterial activity of products intended for the control of the healthcare environment. The results obtained on the three disinfectants tested reveal an ineffectiveness against some isolated strains from the hospital environment.


2017 ◽  
Vol 8 (1) ◽  
Author(s):  
Renu Narendra Jaisinghani

Quercetin is a polyphenolic flavonoid with potential chemoprotective properties. In the present work its antibacterial properties were studied against Staphylococcus aureus, Escherichia coli, Shigella flexneri, Proteus vulgaris, Pseudomonas aeruginosa, Lactobacillus casei var shirota by broth dilution method. Quercetin inhibited S. aureus, P. aeruginosa at concentration 20 mcg/mL while P. vulgaris and E. coli were inhibited at concentration 300 mcg/mL and 400 mcg/mL respectively. Shigella flexneri and Lactobacillus casei var shirota were completely indifferent even at concentration of 500 mcg/mL.


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