1. Diabetic chronic wounds, mainly foot ulcers, constitute one of the most common complications poorly managed diabetes mellitus. The typical reasons are insufficient glycemic management, latent neuropathy, peripheral vascular disease, and neglected care. In addition, it is a cause osteomyelitis amputation lower extremities. Patients admitted in larger numbers attributable to wounds compared any other diabetic disease. United States, currently non-traumatic amputations. Approximately five...

Lipophilicity is one of the key properties a potential drug that determines solubility, ability to penetrate through cell barriers, and transport molecular target. It affects pharmacokinetic processes such as adsorption, distribution, metabolism, excretion (ADME). The 10-substituted 1,9-diazaphenothiazines show promising if not impressive in vitro anticancer potential, which associated with activation mitochondrial apoptosis pathway connected induction BAX, forming channel MOMP releasing...

Lipophilicity is one of the principal parameters that describe pharmacokinetic behavior a drug, including its absorption, distribution, metabolism, elimination, and toxicity. In this study, lipophilicity other physicochemical, pharmacokinetic, toxicity properties affect bioavailability newly synthesized dialkylaminoalkyldiquinothiazine hybrids as potential drug candidates are presented. The lipophilicity, RM0, was determined experimentally by RP-TLC method using RP18 plates acetone–TRIS...

The quinoline molecule is a chemical motif showing highly promising pharmacological potential. Its numerous derivatives introduced into medicine revolutionized in the treatment of many entities disease. presence system structure phenothiazines made it possible to obtain new aza- and diazaphenothiazine that show anticancer aza-analogs are structurally modified by substitution one or both benzene rings phenothiazine ring with various azine rings. This approach strategy obtaining substances...

Albumin is one of the most important proteins in human blood. Among its multiple functions, drug binding crucial terms distribution body. This protein undergoes many modifications that are certain to influence activity and affect structure. One such reaction albumin oxidation. Chloramine T a strong oxidant. Solutions serum albumin, both non-modified modified by chloramine T, were examined with use fluorescence, absorption circular dichroism (CD) spectroscopy. 10H-3,6-diazaphenothiazine...

Human serum albumin (HSA) plays a fundamental role in the human body, including transport of exogenous and endogenous substances. HSA is also biopolymer with great medical pharmaceutical potential. Due to nontoxicity biocompatibility, this protein can be used as nanocarrier. 10-(2′-Pyrimidyl)-3,6-diazaphenothiazine (10-Pyr-3,6-DAPT) phenothiazine showing high anticancer potential vitro against glioma, melanoma breast cancer cells. Additionally, compound characterized by selectivity action...

Hyperlipidemia, marked by high levels of fats in the blood, is a major risk factor for non-communicable diseases such as type 2 diabetes, cardiovascular diseases, and cancer. It has been linked to action reactive oxygen species formation advanced glycation end products. Current treatments hyperlipidemia, like orlistat, simvastatin, atorvastatin, often present undesirable side effects, prompting need new therapeutic agents that are safer, more effective, cost-efficient, have fewer effects. In...

Abstract magnified image The review surveys the chemistry of diaza‐, triaza‐, and tetraazaphenothiazines their benzo dibenzo derivatives consisting over 30 different heterocyclic systems. J. Heterocyclic Chem., 46, 355 (2009).

Abstract In this study, we evaluated the activities of new types azaphenothiazines in following immunological assays: proliferative response human peripheral blood mononuclear cells induced by phytohemagglutin A or anti-CD3 antibodies; lipopolysaccharide-induced cytokine production PBMC; secondary, humoral immune mice to sheep erythrocytes (in vitro); and delayed-type hypersensitivity ovalbumin vivo). some tests, chlorpromazine served as a reference drug. The compounds exhibited differential...

Phenothiazine derivatives are widely studied in various fields such as biology, chemistry, and medicine research because of their pharmaceutical effects. The first reagent that was used suc-cessfully the treatment psychosis a phenthiazine derivative, chlorpromazine. Apart from activity neurons, chlorpromazine have also been reported to display anticancer antibacterial properties. In these studies, we present synthesis on activ-ity against A549, MDA, MiaPaCa, PC3 HCT116 cancer cell lines S....

Phenothiazine derivatives are widely studied in various fields such as biology, chemistry, and medicine research because of their pharmaceutical effects. The first compound used successfully the treatment psychosis was a phenthiazine derivative, chlorpromazine. Apart from its activity neurons, chlorpromazine has also been reported to display anticancer antibacterial properties. In this study, we present synthesis on A549, MDA, MiaPaCa, PC3, HCT116 cancer cell lines S. aureus, epidermidis, E....

A new type of tricyclic azaphenothiazines-1,8-diazaphenothiazines-was obtained in the reaction 2,3- and 3,4-disubstituted pyridines. The ran as Smiles rearrangement. 1,8-diazaphenothiazine system was determined using NOE experiment 2D NMR spectra (COSY, HSQC, HMBC). 10H-1,8-diazaphenothiazine transformed into 10-derivatives with alkyl, aminoalkyl, amidoalkyl, sulfonamidoalkyl, nitrogen half-mustard groups. compounds were tested for their effects on phytohemagglutinin A-induced proliferative...

New tetracyclic and pentacyclic azaphenothiazines containing one or two quinoline rings instead of benzene were obtained in the original reactions isomeric diquinodithiins, dichlorodiquinolinyl sulfides, disulfide with aromatic amines. The type ring fusion azaphenothiazine system was concluded from 1H NMR spectra. evaluated vitro for their antioxidant activity on rat hepatic microsomal membranes protection non-enzymatic lipid peroxidation promoted by Fe2+/ascorbic acid redox system. Most...

3,6-Diazaphenothiazines were obtained in cyclization of 3-amino-3'-nitro-2,4'-dipyridinyl sulfide and the reaction sodium 3-amino-2-pyridinethiolate with 4-chloro-3-nitropyridine followed by alkylation heteroarylation. The thiazine ring formation ran via Smiles rearrangement. structure elucidation was based on 2D NMR X-ray analysis N-methylated product. investigated for antitumor activity using glioblastoma SNB-19, melanoma C-32 breast cancer MCF-7 cells. 10H-3,6-diazaphenothiazine 10 times...

Angularly condensed diquinothiazines (MY1, MY2, and MY3) a phenothiazine derivative was evaluated for antioxidant, antiglycation, sugar hydrolysis enzyme inhibitory effect molecular in silico docking. Antioxidants were using DPPH, chelating ion, FRAP lipid peroxidation. Alpha glucosidase alpha amylase inhibition used activity antiglycation with BSA-Glucose BSA-MGO. In silco docking done AutoDock Vina ADMET properties pkCSM software. showed free radical scavenging, alpha-glucosidase...

An efficient synthesis of novel type dipyrido-1,4-thiazine (4) was elaborated in the reactions two pairs 3,4-disubstituted pyridines DMF.The proceeded through S→N Smiles rearrangement resulting 4,4'-dipyridinyl sulfide.In case formation 10-(3'-nitro-4'pyridinyl)-2,7-diazaphenothiazine (5) double observed.10H-2,7-diazaphenothiazine N-alkylated, N-arylated and N-heteroarylated to give 10-substituted (alkyl, arylalkyl, aryl, heteroaryl dialkylaminoalkyl) derivatives ( 5) (17-29).The NMR spectra...

New derivatives of two isomeric types azaphenothiazines, 1,8- and 2,7-diazaphenothiazine, containing the triple bond substituents additionally tertiary cyclic acyclic amine groups, were synthesized tested for their anticancer activity. The compounds exhibited differential inhibitory activities. Better results obtained when acetylenic group was transformed via Mannich reaction to dialkylaminobutynyl groups. most active 2,7-diazaphenothiazine with N-methylpiperazine-2-butynyl substituent...

Abstract: The asymptomatic properties and high treatment resistance of ovarian cancer result in poor outcomes mortality rates. Although the fundamental chemotherapy provides promising anticancer activities, it is associated with severe side effects. derivative phenothiazine, namely, 10 H -3,6-diazaphenothiazine (PTZ), was synthesized reported ideal effects a previous paper. In this study, detailed PTZ examined on A2780 cells by investigating cytotoxicity profiles, mechanism apoptosis, cell...

New phenothiazine derivatives as 10-substituted dipyridothiazines of the 1,6-diazaphenothiazine structure were obtained in cyclization reaction 3-amino-3'-nitro-2,2'-dipyridinyl sulfide and 3,3'-dinitro-2,2'-dipyridinyl disulfide, 2-chloro-3-ntropyridine with sodium 3-amino-2-pyridinethiolate followed by various alkylation arylation reactions. The thiazine ring formation ran via Smiles rearrangement S-N type. As reactions could proceed at thiazine, azine or both nitrogen atoms, product...