Synthesis, characterization, and antibacterial studies of pipemidic acid metal complexes

Background Pipemidic acid, like other quinolones, is susceptible against different organisms in vitro, and it was proved to be a preferred choice for certain indications. Previous studies reveal that concurrent administration of essential and trace elements with quinolones decreases gastrointestinal absorption, causing therapeutic failure. To study the probable interaction of pipemidic acid with essential and trace elements present in the human body, pipemidic acid has been reacted with magnesium, calcium, chromium, manganese, iron, cobalt, nickel, copper, zinc, and cadmium, the complexes formed. Results The compounds were characterized by the melting point, conductance studies, IR, UV, 1H-NMR, CHN, and atomic absorption analysis. Conclusion The results suggested oxygen atoms present at carbonyl and carboxylic group render the bidentate6 property to the pipemidic acid. The antimicrobial activity of the compounds was determined by the disk diffusion method, and both standard and complexes show no antibacterial activity against the clinical isolates.

Pola peresepan antibiotik pada pasien infeksi saluran kemih di instalasi rawat jalan RSUD Provinsi NTB tahun 2017

Urinary tract infection (UTI) is an infection due to the proliferation of microorganisms in the urinary tract. UTI is usually occur in the community at various ages. In 2014, Indonesian Ministry of Health showed that the number of people with UTIs reached 90-100 cases per 100,000 population per year. Antibiotics are the main therapy used in treating urinary tract infections. The purpose of this study was to determine the pattern of antibiotic prescribing in UTI patients and determine the suitability of therapy with guidelines for UTI at the Installation of NTB Provincial Hospital in 2017. The design of this study was descriptive by collecting data retrospectively. The study was conducted on 105 UTI patients at the Installation Hospital of NTB Province in 2017, then the data obtained from the medical record and prescription sections were processed using Microsoft Excel software. The results showed that therapy for UTI patients was antibiotics with the most use of ciprofloxacin (45.71%), then cefixime (40%), urinter (pipemidic acid) (11.43%), levofloxacin (1.90%), cefadroxil (0.95 %). Based on these results, the suitability of prescription was seen from the type of drug and the dosage in the main therapy (antibiotics) was 100% according to the treatment guidelines, but the frequency and duration of administration only reached 99.05% and 88.6%.

From pipemidic acid molecular salts to metal complexes and BioMOFs using mechanochemistry

Mechanochemistry has proven to be an excellent sustainable, efficient and fast tool for the discovery of new crystal forms of old drugs.

Inspiration for revival of old drug: Improving solubility and avoiding hygroscopicity of pipemidic acid by forming two pharmaceutical salts based on charge-assisted hydrogen bond recognitions

In order to improve the solubility of pipemidic acid (PPA) which belongs to quinolones and becomes an "old drug" due to it possesses low aqueous solubility which restricting its application,...

Evaluation of pipemidic acid derivatives for potential antimicrobial activity application: in silico studies on bioactivity

Background: Pipemidic acid is a broad-spectrum quinolone antibacterial agent for the treatment of chronic urinary tract infections against both gram-positive and gram-negative bacteria. Both quinolone and fluoroquinolone antibiotics have been useful in combating bacterial infections. However, patients suffer severe side effects when they stop taking the medication. The piperazinyl region of pipemidic acid is highly responsible for the side effects. Objective: Therefore, the objective of this study is to design new compounds in which the piperazinyl region is masked by way of conjugation to benzoic acid derivatives Methods: In silico studies were conducted using AutoDockTools software for ligand-protein docking. The docking scores were compared to the parent pipemidic acid docked to Bacterial DNA (deoxyribonucleic acid) gyrase and GABA (gamma- Aminobutyric acid) receptor from the PDB (Protein Data Bank) database. Sites of metabolism, biological activity, quantum chemical descriptors and ADME (absorption, distribution, metabolism, and excretion) property predictions for each designed ligand were also evaluated Results: The docking studies and biological activity predictions showed good anti-infective properties (ligand PAR03) whilst also suggesting a reduction in GABA receptor agonist activity. The performance of PAR03 correlates with its electronic properties showing electrophilic character (can generate reactive Electrophilic Species (RES)). Conclusion: The results from this study indicate that modification of the piperazinyl region of pipemidic acid can be an effective way to improve the drug potency whilst also ensuring reduction of the associated side effects

Bioactivity of Isostructural Hydrogen Bonding Frameworks Built from Pipemidic Acid Metal Complexes

We report herein three novel complexes whose design was based on the approach that consists of combining commercially available antibiotics with metals to attain different physicochemical properties and promote antimicrobial activity. Thus, new isostructural three-dimensional (3D) hydrogen bonding frameworks of pipemidic acid with manganese (II), zinc (II) and calcium (II) have been synthesised by mechanochemistry and are stable under shelf conditions. Notably, the antimicrobial activity of the compounds is maintained or even increased; in particular, the activity of the complexes is augmented against Escherichia coli, a representative of Gram-negative bacteria that have emerged as a major concern in drug resistance. Moreover, the synthesised compounds display similar general toxicity (Artemia salina model) levels to the original antibiotic, pipemidic acid. The increased antibacterial activity of the synthesised compounds, together with their appropriate toxicity levels, are promising outcomes.

Monitoring of Foreign Drug Safety Information

Analysis of administrative decisions of foreign regulatory authorities on the recoil of medicines and/or the need for changes in the instructions for their medical use due to changes in the safety profile, conducted by experts of the Scientific Centre for Expert Evaluation of Medicinal Products revealed 23 administrative decisions. These decisions contained information on the following medicines registered in Russia: аmitriptyline, duloxetine, quetiapine, lamotrigine, topiramate, phenytoin, articaine, epinephrine, bupivacaine, oxybutynin, dexlansoprazole, pantoprazole, esomeprazole, famotidine, ketoconazole, minocycline, quinolone and fluoroquinolone (cinoxacin, ciprofloxacin, flumequine, levofloxacin, lomefloxacin, moxifloxacin, nalidixic acid, norfloxacin, ofloxacin, pefloxacin, pipemidic acid, prulifloxacin and rufloxacin), antiretrovirals (abacavir, abacavir, dolutegravir, lamivudine, zidovudine, atazanavir, cobicistat, emtricitabine, tenofovir, darunavir, didanosine, rilpivirine, efavirenz, enfuvirtide, etravirine, fosamprenavir, indinavir, lopinavir, ritonavir, maraviroc, raltegravir, rilpivirine, nevirapine, saquinavir, tipranavir), direct-acting antiviral drugs (daclatasvir, dasabuvir, elbasvir, grazoprevir, glecaprevir, pibrentasvir, sofosbuvir, ombitasvir, ritonavir).