A multicomponent synthesis was empolyed for the of ethyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate 1. An interesting cyclization obtained when amino-ester 1 reacted with isothiocyanate to give benzo[4,5]thieno[2,3-d][1,3]thiazin-4-one 3. Acylation chloroacetyl chloride in DCM and Et3N afforded acylated ester 4. The cyclized benzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one 8, which some alkylating agents leading alkylation at nitrogen 9–13. Hydrazide 14 utilized as a synthon...

Oxidative phenol coupling reactions are required to establish the cross-linked heptapeptide backbone of vancomycin. The first cross-linking reaction, catalyzed by P450 enzyme OxyB, is dramatically slower when a chlorine substituent present in hexapeptide-S-PCP substrate and abolished introduced into potential heptapeptide-S-PCP substrate.

Cancer is the most severe disease worldwide. Every year, tens of millions people are diagnosed with cancer, and over half those will ultimately die from disease. Hence, discovery new inhibitors for fighting cancer necessary. As a result, indolyl-triazole hybrids were synthesized to target breast liver cells. The synthetic strategy involves glycosylation 4-aryltriazolethiones 3a-b acetyl-protected α-halosugars in presence K2CO3 acetone give mixture β-S-glycosides 6a-b, 7a-b, β-N-glycosides...

Abstract Novel 2‐Amino‐4H‐1,3,4‐thiadiazine‐5‐(6H)‐one derivatives 3 – 6 were designed, synthesized, and assessed for their anticancer effects on MCF‐7 A549 cell lines. The cytotoxicity screening found several active compounds. Meanwhile, compound 5 b exhibited the strongest cytotoxic activity compared to Doxorubicin (DOX). Furthermore, DNA flow cytometry investigation over cells indicated that demonstrated arrest at G1/S stages of cycle induction apoptosis by rising pre‐G1 stage. In...

The present synthetic strategy involves the synthesis of indolyl-triazolo-thiadiazole heterocyclic ring systems 8–13 from condensation 4-amino-5-(1H-indol-2-yl)-3H-1,2,4-triazole-3-thione 1 with aromatic carboxylic acid derivatives 2–7 in presence POCl3 for h. All compounds were obtained very good yields and have been well-characterized using spectroscopic techniques. Exclusively, quality crystals target organic hybrid 8-(1H-indol-2-yl)-5-(p-tolyl)-[1,2,4]triazolo [3,4-b][1,3,4]thiadiazole 9...

2-((3-Cyano-4,6-dimethylpyridin-2-yl)oxy)acetohydrazide 1 was used as the precursor for synthesis of 5-thioxo-1,3,4-oxadiazol-2-yl)methoxy)nicotinonitrile 2. The latter alkylated with different alkylating agents to produce S-alkylated products 3–6. Galactosylation 2 produces a mixture S- and N-galactosides 8 9. hydrazide is converted azide 10, coupled glycine methyl ester hydrochloride set amines target amides 11–15. New compounds were assigned using NMR elemental analysis. Compound 12 had...

The present work describes an green and eco-friendly synthetic protocol, vitro anti-proliferative activity of a new series 3-arylidine imidazo[1,2-c]pyrimidines. target molecules 4a–p were synthesized via one-pot cyclization 6-amino-4-(4-chlorophenyl)-2-thioxo-1,2-dihydropyrimidine-5-carbonitrile(1) with chloroacetyl chloride followed by condensation aromatic heteroaromatic aldehydes in the presence K2CO3-NPs at room temperature. high yield (80–96%), mild reaction conditions (short time no...

A novel series of thiazolium ionic liquids (TILs) bound to chloride (2a-c), tetrafluoroborate (BF4) (3a-c), and bis-(trifluoromethanesulfonimide) (Tf2N) anions (4a-c) was synthesized their physicochemical characteristics were investigated using various microanalytical techniques. The pharmacological potential the new TILs assessed as chemotherapeutic agents for bacterial infections ovarian cancer (SKOV-3). Notably, ILs with same cations become more bactericidal upon binding strongest...

Oxidative Phenol-Kupplungen werden benötigt, um das makrocyclische Heptapeptid-Rückgrat von Vancomycin zu bilden. Die erste Cyclisierung, welche durch P450-Enzym OxyB katalysiert wird, ist stark verlangsamt, falls ein Chlor-Substituent im Hexapeptid-S-PCP-Substrat vorhanden ist, und findet gar nicht statt, wenn der in potenzielles Heptapeptid-S-PCP-Substrat eingeführt wird.

Background: diabetic nephropathy (DN) is a chronic main microvascular consequence of untreated hyperglycemia, affects significant portion the population. It's thought to be factor causing end-stage kidney disease. TNF-α involved in development and course disease DN. Aim: This study aimed evaluate plasma as new diagnostic marker for early Patients Methods: included 125 Egyptian subjects attending out Clinic Department Internal Medicine, 10Th Ramadan city Health Insurance Hospital divided...

Abstract Among the most typical reasons of end-stage renal disease (ESRD) is diabetic nephropathy (DN), which also rated as a major microvascular complication diabetes mellitus. The existent study looked at impact dapagliflozin, mulberry fruit and leaves extracts their combination on kidney rats. To induce nephropathy, experimental rats were supplied with 10% fructose (Fr) in drinking water for first two weeks. Each Fr-fed animal received an intraperitoneal injection low single dose STZ (40...

Background: Coumarin and thiazole derivatives have been used traditionally for many centuries. Because they anti-tumor, antioxidant activities, induced apoptosis.
 Aim: The present study aims to investigate the in vivo antitumor, activities of potassium salt 5-(4 -chlorophenyl)-2-[(7-hydroxy coumarin-3-ylethylidene) acetyl hydrazine]-1,3 (5a) -chlorophenyl)-2-[(8-hydroxy (5b). 
 Materials Methods: Toxicity has determined synthesized compound. Anti-cancer anti-oxidant were studied...

Dietary fibres are a type of carbohydrates that found in plant-based foods.They not absorbed or digested by the body but play an important role maintaining good health.Short-chain fatty acids (SCFAs), primarily acetate, propionate, and butyrate, metabolites formed gut microbiota from these complex dietary carbohydrates.The have secretion hormones such as glucagon-like peptide-1(GLP-1) glucose-dependent insulin tropic polypeptide (GIP) help to control diabetes.Diabetes mellitus is chronic...

The present work describes the synthesis and vitro anti-proliferative activity of a new series 3-arylidine imidazo[1,2-c]pyrimidines. target molecules were in 81-96% yield via one-pot cyclization 6-amino-4-(4-chlorophenyl)-2-thioxo-1,2-dihydropyrimidine-5-carbonitrile (1) with chloroacetyl chloride followed by condensation aromatic heteroaromatic aldehydes. Pyrimidines 5c, 5g 5i demonstrated significant against MCF-7 especially compound was found to be most effective among tested compounds...

hydrazine hydrate, hydroxylamine hydrochloride, and o-phenylenediamine to give different quinazolinones 4,5 benzoimidazoles 6, 7, respectively.Product 4 reacted with

The coronavirus disease 2019 (COVID-19) emerged as a worldwide challenge to researchers and scientists. All research communities are working relentlessly in their labs hoping find cure for the current COVID-19 pandemic. Developing new vaccine is not down on road, it long process that needs numerous clinical trials. Moving battle out of body requires personal protective equipment (PPE), particularly masks gloves. Together, they will limit spread virus, whether by reinforcing PPE developing...