Analytical quality by design-based stability-indicating high performance liquid chromatography method for the estimation of evogliptin tartrate in bulk and tablet dosage form.

The present study utilized Analytical Quality by Design (AQbD) approach to develop a stability-indicating high-performance liquid chromatography (HPLC) method for estimating evogliptin tartrate using design expert software. The key parameters were methodically optimized, contours were plotted, and stability was evaluated using various forced degradation conditions. Using an Agilent HPLC system with a photo diode array (PDA) detector along with Fortis C18 column (250 × 4.

Stability-Indicating Densitometric Analysis of Evogliptin Tartrate in Bulk and Tablet Dosage Form.

Background: Evogliptin tartrate is a novel dipeptidyl peptidase (DPP-4) inhibitor very recently introduced into the market as an oral hypoglycemic drug.

Objective: The literature review has revealed no reports of stability-indicating analytical methods so far for evogliptin tartrate. Thus, the goal of this study was to develop and validate a stability-indicating high-performance thin-layer chromatography (HPTLC) method for evogliptin tartrate in bulk and tablet dosage form.

DprE1 Inhibitors: Enduring Aspirations for Future Antituberculosis Drug Discovery.

DprE1 is a crucial enzyme involved in the cell wall synthesis of Mycobacterium tuberculosis and a promising target for antituberculosis drug development. However, its unique structural characteristics for ligand binding and association with DprE2 make developing new clinical compounds challenging. This review provides an in-depth analysis of the structural requirements for both covalent and non-covalent inhibitors, their 2D and 3D binding patterns, as well as their biological activity data in vitro and in vivo, including pharmacokinetic information.

Dibenzylideneacetone analogues as novel Plasmodium falciparum inhibitors.

A series of dibenzylideneacetones (A1-A12) and some of their pyrazolines (B1-B4) were synthesized and evaluated in vitro for blood stage antiplasmodial properties in Plasmodium falciparum culture using SYBR-green-I fluorescence assay. The compound (1E, 4E)-1,5-bis(3,4-dimethoxyphenyl)penta-1,4-dien-3-one (A9) was found to be the most active with IC(50) of 1.97 μM against chloroquine-sensitive strain (3D7) and 1.

Synthesis of novel alpha-pyranochalcones and pyrazoline derivatives as Plasmodium falciparum growth inhibitors.

Both the lack of a credible malaria vaccine and the emergence and spread of parasites resistant to most of the clinically used antimalarial drugs and drug combination have aroused an imperative need to develop new drugs against malaria. In present work, alpha-pyranochalcones and pyrazoline analogs were synthesized to discover chemically diverse antimalarial leads. Compounds were tested for antimalarial activity by evaluation of the growth of malaria parasite in culture using the microtiter plate based SYBR-Green-I assay.