Factor Xa (FXa) plays a significant role in the blood coagulation cascade and it has become a promising target for anticoagulation drugs. Three oral direct FXa inhibitors have been approved by the FDA for treating thrombotic diseases. By structure-activity relationship (SAR) analysis upon these FXa inhibitors, a series of novel anthranilamide-based FXa inhibitors were designed and synthesized. ...

2-Phenyl-6,7-difluoro and 2-(4-fluorophenyl)quinazoline derivatives bearing salicylidenhydrazino fragments at position 4 were prepared based on 4,5-difluoroantranilic acid or anthranilamide. Molecular docking to casein kinase 2 was performed; compounds with high in silico activity CK2 revealed. Cytotoxic of the synthesized studied cancer cell line MDA-MB-231 normal WI26 VA4.

Factor Xa (FXa) plays a significant role in the blood coagulation cascade and is a promising target for anticoagulation drugs. Three oral FXa inhibitors have been approved by FDA for treating thrombotic diseases. In this study, 43 novel compounds were synthesized anthranilamide-based FXa inhibitors aiming to ameliorate the toxicity of traditional FXa inhibitors in clinic. The data indicated tha...

2-[Methyl-(3-phenylpropionyl)amino]-benzoic acid (1e) was isolated from a culture of marine Streptomyces sp. strain B7747. Analogous compounds have potential importance as phytotoxic substances, hence compound 1e and the analogues 1a approximately 1d and 1f approximately 3a were synthesised. Antimicroalgal activity of the anthranilamide analogues showed that esters 1b, 1f and 2b were more activ...

QSAR studies were performed to understand the structure activity relationship (SAR) and to build the computational model to predict newer inhibitors with improved potency. In this study, a library of thiophene-anthranilamide based inhibitors of factor Xa was used to develop QSAR model. The library was divided into two sets: Training and Test sets. QSAR Model consists of four descriptors with R-...

A new, facile, cost effective, and eco-friendly protocol is reported for the synthesis of 2,3-dihydroquinazoline-4-(1H)-ones exploring tannic acid as a novel, inexpensive, andbiodegradable catalyst. A variety of dihydroquinazolins were prepared from aromatic aldehydesand anthranilamide using catalytic amount of tannic acid under solvent free conditions.Operational simplicity, high yield, and hi...

UltraPerformance LC (UPLC) in hydrophilic interaction chromatography (HILIC) separation mode is becoming a routine and widely recognized technique for rapid, efficient, sensitive, and reproducible analysis of 2-aminobenzamide (2-AB) labeled glycans. Even though 2-AB is now the most common glycan labeling reagent, its use is limited by low MS sensitivity. Recent reports on LC/FLR/MS of glycans t...

Abstract This study focused on characterization of Volatile Organic Compounds (VOCs) as contaminants and non-volatile additives in Italian PET bottles, also suggesting potential functional aldehydes scavengers. Several VOCs, such acetic aldehyde (AA), butanal, 3-methyl 1,3-dioxolane, pentanal, hexanal, octanal, 5-hepten-2-one, nonanal, decanal, were identified by Head Space-Gas Chromatography/M...

Polygalacturonate 4-alpha-galacturonosyltransferase (GalA T) activity was detected in the microsomal fraction isolated from pumpkin (Cucurbia moschata Duchesne, cv. Tokyou-Kabocha) seedlings using UDP-GalA and 2-aminobenzamide (2AB)-labeled oligogalacturonides. A 2AB-labeled undecagalacturonide was elongated by the attachment of galacturonic acid (GalA) residues to give 2AB-labeled oligogalactu...