Synthesis of Novel Benzothiazole-Profen Hybrid Amides as Potential NSAID Candidates.

Herein, we report the synthesis of a series of new compounds by combining 2-aminobenzothiazole with various profens. The compounds were characterized using techniques such as H- and C-NMR, FT-IR spectrometry, and high-resolution mass spectrometry (HRMS), with detailed HRMS analysis conducted for each molecule. Their biological activities were tested in vitro, revealing significant anti-inflammatory and antioxidant effects, comparable to those of standard reference compounds.

Concise Synthesis of Pseudane IX, Its -Oxide, and Novel Carboxamide Analogs with Antibacterial Activity.

A four-step synthesis of the natural product pseudane IX, starting from 3-oxododecanoic acid phenylamide and including only one chromatographic purification, was accomplished with an overall yield of 52%. The same synthetic sequence, but with a controlled partial reduction of a nitro group in the penultimate intermediate, led to the -oxide of pseudane IX (NQNO). A shortened three-step variation of the synthesis allowed for the preparation of novel carboxamide analogs of the natural product.

L.: Insights into Its Polyphenolic Constituents and Biological Activity.

In this study, UHPLC-HRMS analysis of the defatted methanol extract obtained from L. led to the identification of 58 compounds-hydroxycinnamic and hydroxybenzoic acids and their glycosides, acylquinic and caffeoylhexaric acids, and flavonoids and their glycosides. In addition, a new natural compound, N-(8-methylnepetin)-3-hydroxypiperidin-2-one was isolated and its structure was elucidated by NMR spectroscopy.

2-Amino--Phenethylbenzamides for Irritable Bowel Syndrome Treatment.

Irritable bowel syndrome (IBS) is a common gastrointestinal (GI) disorder characterized by abdominal pain or discomfort. Mebeverine is an antispasmodic that has been widely used in clinical practice to relieve the symptoms of IBS. However, its systemic use usually leads to side effects.

Metabolomic Profiling and DNA-Fingerprinting of Newly Recorded White-Flowered Populations of Salvia lanigera Poir. in Egypt.

Salvia lanigera Poir. is a small herbaceous perennial species with violet flowers that grows in low-altitude deserts, and sandy loam. During the collection of S.

In Silico and Chromatographic Methods for Analysis of Biotransformation of Prospective Neuroprotective Pyrrole-Based Hydrazone in Isolated Rat Hepatocytes.

In the current study, chromatographic and in silico techniques were applied to investigate the biotransformation of ethyl 5-(4-bromophenyl)-1-(2-(2-(2-hydroxybenzylidene) hydrazinyl)-2-oxoethyl)-2-methyl-1-pyrrole-3-carboxylate () in hepatocytic media. The initial chromatographic procedure was based on the employment of the conventional octadecyl stationary phase method for estimation of the chemical stability. Subsequently, a novel and rapid chromatographic approach based on a phenyl-hexyl column was developed, aiming to separate the possible metabolites.

Novel Flurbiprofen Derivatives as Antioxidant and Anti-Inflammatory Agents: Synthesis, In Silico, and In Vitro Biological Evaluation.

In this study, we present the synthesis of five novel compounds by combining flurbiprofen with various substituted 2-phenethylamines. The synthesized derivatives underwent comprehensive characterization using techniques such as H- and C-NMR spectroscopy, UV-Vis spectroscopy, and high-resolution mass spectrometry (HRMS). Detailed HRMS analysis was performed for each of these newly created molecules.

Novel Anthranilic Acid Hybrids-An Alternative Weapon against Inflammatory Diseases.

Anti-inflammatory drugs are used to relieve pain, fever, and inflammation while protecting the cardiovascular system. However, the side effects of currently available medications have limited their usage. Due to these adverse effects, there is a significant need for new drugs.

Synthesis, Molecular Docking, and Biological Evaluation of Novel Anthranilic Acid Hybrid and Its Diamides as Antispasmodics.

The present article focuses on the synthesis and biological evaluation of a novel anthranilic acid hybrid and its diamides as antispasmodics. Methods: Due to the predicted in silico methods spasmolytic activity, we synthesized a hybrid molecule of anthranilic acid and 2-(3-chlorophenyl)ethylamine. The obtained hybrid was then applied in acylation with different acyl chlorides.

HPLC Analysis and In Vitro and In Silico Evaluation of the Biological Activity of Polyphenolic Components Separated with Solvents of Various Polarities from .

has piqued the interest of many researchers in recent years, mostly for its essential oil, but increasingly for its polyphenolic content as well. In the current study, we examine the polyphenolic composition of grown in Bulgaria. The polyphenolic complex was fractionated with solvents of various polarities, including hexane, chloroform, ethyl acetate, and butanol, in order to assess the biological impact of the components.

Development of Hyphenated Techniques and Network Identification Approaches for Biotransformational Evaluation of Promising Antitubercular N-pyrrolyl hydrazide-hydrazone in Isolated Rat Hepatocytes.

Novel, rapid and precise RP-HPLC-DAD method was developed, validated and successfully applied for determination of metabolic changes of ethyl 5-(4-bromophenyl)-1-(3-(2-(2-hydroxybenzylidene)hydrazinyl)-3-oxopropyl)-2-methyl-1-pyrrole-3-carboxylate () in isolated rat hepatocytes. The analytes were detected by a simple DAD detector at 279 nm wavelength. A single-step extraction method was implemented to enable fast purification and extraction from cellular culture, resulting in a complete recovery.

Novel hybrids of sclareol and 1,2,4-triazolo[1,5-a]pyrimidine show collateral sensitivity in multidrug-resistant glioblastoma cells.

The synthesis of 24 hybrid molecules, consisting of naturally occurring sclareol (SCL) and synthetic 1,2,4-triazolo[1,5-a]pyrimidines (TPs), is described. New compounds were designed with the aim of improving the cytotoxic properties, activity, and selectivity of the parent compounds. Six analogs (12a-f) contained 4-benzylpiperazine linkage, while 4-benzyldiamine linkage was present in eighteen derivatives (12g-r and 13a-f).

Anticancer Podophyllotoxin Recovery from Juniper Leaves at Atmospheric and High Pressure Using Eco-Friendly Solvents.

Podophyllotoxin (PPT) is a precursor for the synthesis of drugs against cancer and other diseases. The present sources of PPT ( and ) are endangered species, with PPT production highly dependent on their growing conditions. In connection with the identification of new sources of PPT, the present study aimed to recover PPT from leaves via atmospheric or high pressure extraction methods with a focus on using eco-friendly solvents.

Cytotoxic and Antibacterial Prenylated Acylphloroglucinols from L.

Two new bicyclo[3.3.1]nonane type bicyclic polyprenylated acylphloroglucinol derivatives (BPAPs), olympiforin A and B as well as three known prenylated phloroglucinols, were isolated from the aerial parts of L.

Outstanding Antibacterial Activity of -Comparison of the Antimicrobial Effects of Extracts and Fractions from Four Species Growing in Bulgaria with a Focus on Prenylated Phloroglucinols.

Microbial infections are by no means a health problem from a past era due to the increasing antimicrobial resistance of infectious strains. Medicine is in constant need of new drugs and, recently, plant products have had a deserved renaissance and garnered scientific recognition. The aim of this work was to assess the antimicrobial activity of ten active ingredients from four species growing in Bulgaria, as well as to obtain preliminary data on the phytochemical composition of the most promising samples.

Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives.

Herein, we report the obtaining of new hybrid molecules of amphetamine with different profens (amfens). The obtained amfens are characterized by their melting points, UV, H-, C-NMR, and HRMS spectra. A complete and detailed mass spectral analysis of the newly obtained derivatives of amphetamine with ibuprofen, flurbiprofen, ketoprofen, naproxen, and carprofen was performed.

Beyond Traditional Use of : Genoprotective and Antitumor Activity In Vitro.

L. (lady's mantle) was used for centuries in Europe and Balkan countries for treatments of numerous conditions and diseases of the reproductive system, yet some of the biological activities of lady's mantle have been poorly studied and neglected. The present study aimed to estimate the potential of ethanolic extract from Southeast Serbia to prevent and suppress tumor development in vitro, validated by antioxidant, genoprotective, and cytotoxic properties.

In Vitro Study of the Biological Potential of Wastewater Obtained after the Distillation of Four Bulgarian Oil-Bearing Roses.

The wastewater after rose oil distillation is usually discharged into the drainage systems and it represents a serious environmental problem. While being rich in polyphenols, which have beneficial biological activity and application in the pharmaceutical industry, limited research has been carried out about the biological activity of the specific wastewaters per se. Wastewaters after distillation of the four Bulgarian oil-bearing roses Mill.

Innovative Biochemometric Approach to the Metabolite and Biological Profiling of the Balkan Thistle ( Griseb.), Asteraceae.

The widespread genus Mill. (Asteraceae) is renowned in traditional medicine. In the present study, an innovative biochemometric-assisted metabolite profiling of the flower heads, aerial parts and roots of Griseb.

Redox-Modulating Capacity and Antineoplastic Activity of Wastewater Obtained from the Distillation of the Essential Oils of Four Bulgarian Oil-Bearing Roses.

The wastewater from the distillation of rose oils is discharged directly into the soil because it has a limited potential for future applications. The aim of the present study was to determine in vitro the chromatographic profile, redox-modulating capacity, and antineoplastic activity of wastewater obtained by distillation of essential oils from the Bulgarian L., Mill.

UHPLC-Orbitrap-MS Tentative Identification of 51 Oleraceins (Cyclo-Dopa Amides) in L. Cluster Analysis and MS Filtering by Mass Difference.

Oleraceins are a class of indoline amide glycosides found in L. (Portulacaceae), or purslane. These compounds are characterized by 5,6-dihydroxyindoline-2-carboxylic acid -acylated with cinnamic acid derivatives, and many are glucosylated.

Junipers of Various Origins as Potential Sources of the Anticancer Drug Precursor Podophyllotoxin.

Juniper representatives are natural sources of plenty of bioactive metabolites and have been used since ancient times as folk remedies against tapeworms, warts, cancer, etc. The antiproliferative activities of junipers are attributed to podophyllotoxin (PPT), which is a precursor for the synthesis of efficient anticancer drugs. However, the natural sources of PPT, (Royle) T.

Ultra-high-performance liquid chromatography - high-resolution mass spectrometry profiling and hepatoprotective activity of purified saponin and flavonoid fractions from the aerial parts of wild spinach ( L.).

An ultra-high-performance liquid chromatography - high-resolution mass spectrometry profiling method was used for a comprehensive study of flavonoid and saponin-rich fractions from the aerial parts of wild spinach ( L.). Thirty-six compounds, respectively, saponins of eight sapogenins (phytolaccagenin, bayogenin, medicagenic acid, 2-hydroxygypsogenin, 2-hydroxyoleanoic acid, 2-hydroxy-30-nor-gypsogenin, 2-hydroxyakebonic acid, and akebonic acid) together with  flavonoid glycosides of 6-methoxykaempferol, isorhamnetin, patuletin, spinacetin as well as two ecdysteroids (20-hydroxyecdysone and polypodine B) were detected.

Neuroprotective, anti--glucosidase and prolipase active flavonoids from Good King Henry ( L.).

Nine glycosides of patuletin, 6-methoxykaempferol and spinacetin from Good King Henry ( L.) were investigated for neuroprotective, anti--glucosidase and lipase activities. All tested flavonoids (100 µM) showed statistically significant neuroprotective activities on isolated rat brain synaptosomes using 6-hydroxydopamine model.