Synthesis, characterization and biological activity of Pyrazoline derivatives

Pyrazoline is dihydropyrazole having only one endocyclic double bond. Synthesis of pyrazoline derivatives from chalcones is an active arena of investigation due to established pharmacological result. In present study, chalcones were prepared by reacting of acetophenone with benzaldehyde. Then prepared chalcones react with isoniazid in the presence of glacial acetic acid results pyrazoline derivative. Physical parameters such as color, crystal structure, solubility, melting point, retardation factor (Rf) and % yield was evaluated. Confirmations of structures of all synthesized derivatives, were done by spectroscopic data of IR, 1HNMR and Mass spectroscopy. Also, all synthesized compounds were evaluated for antibacterial activity against B. subtilis, S. aureus, P.aeruginosa and E.coli, and antifungal activity was accomplished against C. albicans and A. niger at the different conc. and concluded that some compounds have excellent antimicrobial activity and most of the synthesized compounds exhibits moderate antimicrobial activity.

Synthesis and Prognosis of Anti-inflammatory Activity of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3h)-one

The article presents a modified method for the synthesis of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one and the predict of their anti-inflammatory activity. The proposed method for obtaining tetrahydrothienopyrimidine derivatives is preparatively effective and simple. Their synthesis was carried out by heterocyclization of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in the medium of glacial acetic acid with the catalytic addition of dimethyl sulfoxide. Preliminary prognosis of anti-inflammatory activity in silico method allowed us to identify the most promising compounds. Of these, the 4b structure containing a 2-hydroxyphenyl fragment in the second position of pyrimidine-4(3H)-one may be of the greatest interest. It seems appropriate to further study the spectrum of biological activity of the studied compounds.

Validated HPTLC Method for the Estimation of Oxetacaine in Pharmaceutical Formulations

Oxetacaine is a potent local anesthetics used to relieve pain associated with peptic ulcer. The current method details about a rapid, accurate and precise HPTLC technique for the assessment of Oxetacaine in Pharmaceutical formulation. Chromatographic resolution was carried out on precoated HPTLC plates (Silica gel 60 F254 on Aluminum plate) employing methanol: water: glacial acetic acid (8: 1.8: 0.2 v/v/v) as mobile phase. Densitometric assessment was carried out at 220nm [Camag TLC Scanner III with winCATs software (version – 1.3.4)]. The drug was identified with a Rf value of 0.61. The reliability of the projected method was ascertained by evaluating various validation parameters as per ICH guidelines. The proposed technique can evaluate ten or more formulation units concurrently in a single run and affords a more rapid and cost-effective QC tool for regular analysis of Oxetacaine in pharmaceutical formulations.

Validation Of Spectrophotometry-Visble Method On The Determination Of Borax Levels In Meatballs

Borax, in illictic additive substance, is added on certain food product as a e preservative and rubbery. Therefore, the determination of borax in the food product such as meatball is very impotant in view of meatball is a food product often consumed by community. Vis- Spectrophotometric method with curcumine 0.125% as a reagent and glacial acetic acid-sulphuric acid has been used for determination of borax in this research. Curcumin reagent was selected because sensitivity of the method and the reproducibility of the results are affected by quality of the reagent other than rigorous observance of the reaction conditions (temperature, time, reagent quantities). Glacial acetic acid- sulphuric acid was used to create acid condition, so that curcumin and boron form a violetred 2:1 complex called rosocyanin. The optimum result was obtained when 1/. ml solution of 0.125% curcuumin and 1.0 ml concentrated sulphuric acid were added and the absorbance was measured after 70 minutes at 547 nm. The results showed linear regression y = 1.3127x – 0.0994, r = 0.9690 > r table (n = 5) is 0.878 and p = 0.007 (p< 0.01) and Vxo is was 15,53%. The detection limit and quantitation limit were 9.7.10-4 ppm and 2.94. 10-3 ppm respectively. The recovery and coefficient variation were 47.56%±3,92%. Determination of borax in three meatball samples which were taken from a location in Surabaya showed that the sample contained borax with concentration of 0.0205; 0.0151; 0.0210 (% w/w) respectively.

1009. Biofilm Formation in Acinetobacter Baumannii Clinical Isolates

Background Multidrug resistant Acinetobacter baumannii (MDR-Ab) is a Gram-negative bacterium known for causing severe nosocomial infections, attributed in part to its formation of biofilm. Siderophore is a virulence factor known to support biofilm formation by regulating iron availability. In this study, we screened 44 isolates of MDR-Ab from our Gram-negative repository to determine the strains that phenotypically form biofilm and produce siderophore. The results were compared to Pseudomonas aeruginosa PAO1, which produces both biofilm and siderophore. Methods Isolates were grown overnight in minimal M9 medium supplemented with casamino acids and hydroxyquinones at 37°C. Bacterial cells were normalized (to OD 600=0.01) and a standard diluted 10-3 tube was used in the study. A 96-well plate was inoculated with 100 microliters of each isolate in quadruplicates. This process was repeated in Tygon tubes with 50 microliters of each isolate in triplicates. The plate and Tygon tubes were incubated statically for 48 hours at 30°C and then stained with crystal violet. The contents were dissolved in 33% glacial acetic acid and analyzed by spectrophotometry to measure biofilm formation. Siderophore secretion was measured in supernatants with Chrome Azurol S (CAS) reagent and production was observed on CAS agar plates. Results High levels of biofilm formation were observed in 8 strains of MDR-Ab in the 96-well plate (3, 4, 9, 22, 61, 1010, 1012, 1022) and 6 strains in Tygon tubes (3, 4, 16, 66, 1002, 1010) (Fig. 1). There was minimal siderophore production in MDR-Ab isolates compared to PAO1 in both the 96-well plate and Tygon tubes (Fig. 2). Only 4 strains lacked siderophore production on CAS agar and were inversely negative for the secretion in medium. Figure 1 Biofilm formation in a 96-well plate and Tygon tubes (A) High levels of biofilm formation were observed in MDR-Ab strain numbers 3, 4, 9, 22, 61, 1010, 1012, 1022 in the 96-well plate. (B) High levels of biofilm formation were observed in MDR-Ab strain numbers 3, 4, 16, 66, 1002, 1010 in Tygon tubes. Figure 2 Degree of siderophore production in a 96-well plate and Tygon tubes Siderophore production of MDR-Ab was limited compared to PAO1 after inoculation in a 96-well plate (A) and in Tygon tubes (B). Conclusion Many strains of MDR-Ab readily form biofilm. Overall siderophore production is lower in MDR-Ab compared to consistent production by PAO1, but this does not appear to affect MDR-Ab’s ability to form biofilm. Unlike in PAO1, biofilm formation in MDR-Ab may occur independently of siderophore production. This research serves as a basis for understanding future MDR-Ab biofilm elimination in patient catheters and indwelling devices. Disclosures All Authors: No reported disclosures

Synthesis of S-glycosides analogues containing Thiouracil unite and Evaluated as antibacterial and Antifungal active

Preparation of new S-glycosides including thiouracil derivatives as heterobase. The main step of this work is the formation of thiouracil derivatives [1-3] by the condensation reaction of ethyl cyanoacetate, aromatic aldehydes and thiourea to form target compounds [1-3], after protection of the hydroxyl groups in sugar (D-fructose, L- sorbose, and D-galactose), react with hydrobromic acid 45% in glacial acetic acid give different Bromo sugars [a-c], which coupled with prepares thiouracil derivatives [1-3] and propylthiouracil [4] in the presence of K2CO3 to afford the corresponding product S-glycoside analogs [1-4a, 1-4b, 1-4c]. deprotection of the S-glycoside analogs in acid and base medium, led to the free S-glycoside derivatives [1-4d,1-4e,1-4f]. The obtained compounds were tested for their antibacterial and antifungal actives.

Fingertip Necrosis due to Chemical Burn from Glacial Acetic Acid: A Case Report

Glacial acetic acid is a high-purity acetic acid that is mainly used as a solvent in chemical production and for various purposes in the food and pharmaceutical industries. It is safe enough to be used for chemical peeling when diluted, and has been used in folk remedies for warts, athlete’s foot, and eczema. Indeed, such conditions are the most common reason for exposure to glacial acetic acid. In the present report, we describe the case of a 10-year-old girl who presented with pain and necrosis of the distal phalanx of her left index finger. Two days prior, her fingers had been wrapped overnight with a paste of flour mixed with glacial acetic acid to treat warts. We irrigated the affected area with normal saline, applied a mupirocin ointment, and administered prostaglandin E1. However, the necrosis progressed rapidly. After 10 days, the girl’s fingertip was amputated, and a hypothenar free flap was performed. The case represents a severe chemical burn resulting from the misuse of glacial acetic acid, requiring surgical treatment.

Simultaneous analysis of eprosartan and hydrochlorothiazide in tablet formulation by High- Performance thin layer chromatography with ultraviolet absorption densitometry

A new, simple, accurate, and precise high-performance thin-layer chromatographic method has been established for simultaneous analysis of Eprosartan and Hydrochlorothiazide from a tablet formulation. Standard and sample solutions of Eprosartan and Hydrochlorothiazide were applied to precoated 250 μm layer of silica gel G 60 F and the plates were developed with Chloroform: Acetonitrile: Glacial Acetic Acid (7:3:1,v/v/v) as mobile phase. Detection and evaluation of densitograms was performed densitometrically at 254 nm. The linear range was 200-700 ng/band with the retention factors of Eprosartan and Hydrochlorothiazide were 0.26± 0.02 and 0.44±0.02, respectively. The method was validated and successfully used for analysis of the drugs in tablets.