Introduction: Tyrosinase, found in various organisms, including plants and mammals, is responsible for pigmentation as well the undesirable browning of fruits vegetables, a multi-copper enzyme involved synthesis melanin human. As it known, provides protection against harmful ultraviolet radiation, which can lead to serious conditions like skin cancers. However, excessive accumulation could result hyperpigmented spots, creating aesthetic concerns. Tyrosinase inhibitors potentially development...

A series of 38 new acylhydrazones [3-40], derived from (2$S)$-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl] amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV antimicrobial activity with the further aim to develop carrying an amino side chain. All tested compounds possess stronger against gram (+) bacteria. Compound 23 was found active methicillin-resistant Staphylococcus aureus (MRSA) a MIC value 3.9 $\mu $g/mL. The compound 30 Enterococcus faecalis,...

A series of novel diflunisal hydrazide-hydrazones has been reported together with their anti-hepatitis C virus and antiproliferative activities in a number human hepatoma cell lines. However, the mechanisms underlying efficacy these agents remain unclear. It was chosen to investigate lead hydrazide-hydrazone, 2',4'-difluoro-4-hydroxy-N'- [(pyridin-2-yl)methylidene]biphenyl-3-carbohydrazide (compound 3b), two cultured lines-HepG2 Hep3B-using metabolomic protocol aimed at uncovering any...

In our continuing search for new anticancer agents, herein we report the synthesis of 2-(4-chloro-3-methylphenoxy)-N'-[(aryl)methylidene]acetohydrazides 3a–j and evaluation their activities on cell viability, morphological changes caspase-3 activity in cancer lines including gastric (MKN45), cervical (HeLa) breast (MDA-MB-231) cells. 2-(4-chloro-3-methylphenoxy)-N'-[(4-phenylthiophen-2-yl)methylidene] acetohydrazide 3g presented strongest growth inhibition against MKN45 with IC50 value 1.471...

4-Thiazolidinones are sulphur analogues of oxazolidines. They heterocyclic ring systems which have been explored for their antimicrobial, anticancer, anti-HCV, antifungal, anticonvulsant, antituberculosis, and other activities. While some earlier reviews on the biological activities this system reported, present review describes more recent synthetic strategies medicinal aspects 4-thiazolidinones as anticancer agents reported during past few years (2010-2016). Keywords: 4-Thiazolidinone,...

Background: A series of novel N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene sulfonamides [SGK 318, 319, 320, 324, 327] and N-(3- substitutedaryl/alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1- yl]benzenesulfonamides[SGK 328, 329, 330, 334, 337] were synthesized tested for their quorum sensing inhibitor (QSI) capacity using selector 1 (QSIS1) bioassay. Keywords: Celecoxib,...

In this study, the synthesis and characterization of 2-(2-fluorobiphenyl-4-yl)-N´- [(substituted methylene]propanehydrazides (3a-s) 2-(2-fluoro-[1,1'-biphenyl]-4-yl)-N-(5-methyl-2-(substituted aryl)-4oxothiazolidin-3-yl)propanamides (4a-s) are described also antiproliferative effect compounds on HT-29, HeLa, A549 MCF-7 cancer cell lines is investigated.Additionally, mouse embryonic fibroblast cells NIH3T3 were evaluated to determine selectivity.The results showed that identified did not...

Background: Hydrazide-hydrazones constitute an important class of compounds for new drug development. In this study, a series 39 acylhydrazones (3-41), derived from (2S)-3-methyl- 2-[[(4-methylphenyl)sulfonyl]amino]butanoic acid hydrazide were synthesized with further aim to achieve biologically active carrying amino side chain. Methods: Compounds 3-41 by microwave-assisted method. All have been tested their anti-HIV activity compound 21 was subjected set 2DNMR analysis the characterization...

Some novel 1-(2-methyl-5-nitro-1H-imidazol-1-yl)-3-(substituted phenoxy)propan-2-ol derivatives (3a-g) were designed and synthesized.Compounds 3a-g obtained by refluxing ornidazole (1) with the corresponding phenolic compounds (2a-g) in presence of anhydrous K2CO3 acetonitrile.Following structure elucidation, vitro antimicrobial activity cytotoxic effects on K562 leukemia NIH/3T3 mouse embryonic fibroblast cells measured. As a part this study, compliance drug-likeness properties was...

In this work, twenty hydrazide-hydrazone and 4-thiazolidinone derivatives were synthesized starting from m-cresol. Antimicrobial evaluation was carried out by microdilution method against Enterococcus faecalis Staphylococcus aureus as Gram-positive bacteria Escherichia coli Pseudomonas aeruginosa Gram-negative bacteria, three pathogenic fungi Candida albicans, parapsilosis krusei. Some compounds possessed considerable antimicrobial properties the tested microorganisms, particularly E. coli....

Sedanur Ekreka , Sevil Şenkardeşa* Ömer Erdoğanb & Özge Çevikb a Department of Pharmaceutical Chemistry, Faculty Pharmacy, Marmara University, İstanbul, Turkeyb Biochemistry, School Medicine, Adnan Menderes Aydın, Turkey

The aim of the present study was to develop and validate a High-Performance Liquid Chromatography (HPLC) method for determination lisinopril gliclazide. developed on Zorbax C8 analytical column (4.6x250 mm; 5μm) by isocratic elution with flow rate 1.0 mL/min injection volume 25 μl. mobile phase composition methanol:water (65:35 v/v, pH adjusted 3.0 triethylamineorthophosphoric acid buffer) retention time found be 2.883 7.456 min gliclazide, respectively. linear in concentration range 5-20...

A series of thiosemicarbazides were synthesized and structurally characterized by spectroscopic techniques (NMR, FT-IR) besides elemental analysis. These compounds evaluated for their cytotoxicity against human breast cancer cell line MCF7 prostate PC3 nonmalignant fibroblast L929 MTT assay. Among the compounds, N-[2-(4-chlorophenyl)ethyl]-2-[(4-methylphenyl)sulfonyl]hydrazinecarbothioamide (3d) 2-[(4-methylphenyl)sulfonyl]-N-[4-(trifluoromethoxy)phenyl]hydrazinecarbothioamide (3f) found to...

By exploiting the wide biological potential of hydrazone scaffold, a series derivatives were synthesized, starting from N-(3-hydroxyphenyl)acetamide (metacetamol). The structures compounds determined using IR, 1 H and 13 C-NMR, mass spectroscopic methods. obtained molecules (3 a-j) evaluated for their anticancer against MDA-MB-231 MCF-7 breast cancer cell lines. According to CCK-8 assay, all tested showed moderate potent activity. Among them,...

The aim of the present study was to develop and validate a High-Performance Liquid Chromatography (HPLC) method for determination lisinopril gliclazide. developed on Zorbax C 8 analytical column (4,6x250 mm; 5µm) by isocratic elution with flow rate 1.0 ml/min injection volume 25 µl. mobile phase composition methanol:water (65:35 v/v, pH adjusted 3.0 triethylamine-orthophosphoric acid buffer) retention time found be 2.883 7.456 min gliclazide, respectively. linear in concentration range 5...

Abstract Review: 203 refs.

Objective: Today, the development of antibiotic resistance is increasing rapidly. This makes it necessary to discover new antibiotics; therefore, this research aims find antibacterial agents. 
 Materials and Methods: Structures newly synthesised compounds (4a-d, 5a-d) were elucidated by elemental analyses spectroscopic data. Their in vitro activities tested using a micro-dilution technique against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, methicillin-resistant...

Acyl hydrazone (R-CO-NH-N=CH-R) is a versatile scaffold for the synthesis of several molecules with huge potential as anti-viral, anti-bacterial and anti-fungal drugs [1].The stereochemistry this very interesting, infact it may present double bond configuration in imine part E/Z also be amide syn/anti periplanar which give place to at least four possible stable products synthesis.Herein we conducted NMR experiments intent clarify representative set obtained their 3D structure...

A series of novel 2-(substituted arylidene)-N-(5-(propylthio)-2,3-dihydro-1H-benzo[d]imidazol-2-yl)hydrazine-1-carboxamide derivatives 3a-i were synthesized via condensation N-(5-(propylthio)-1H-benzo[d]imidazol-2-yl) hydrazinecarboxamide (2), with the corresponding ketone or aldehydes. The chemical structures compounds prepared confirmed by analytical and spectral data. screened for their α-glucosidase inhibitory activity all them showed better inhibition than acarbose, except 3h. In...