Results 61 to 70 of about 2,349 (173)
Chiral (Stereoselective) Drugs, Asymmetric Synthesis, and Racemic Resolution Methods
Chirality is crucial in drug development since both biological targets in the organism and the majority of pharmaceutical compounds are chiral. The synthesis and resolution of chiral compounds are critical steps while developing chiral drugs. Asymmetric synthesis and racemic resolution are the two most common methods for obtaining enantiopure drugs ...
Burcu Karayavuz +1 more
wiley +1 more source
We developed new derivatives of the cancer drug ponatinib, significantly reducing and altering its spectrum of target kinases. Compound 5 retained the efficacy in inhibiting the colony formation of MDA‐MB‐231 cells and acted primarily on B‐Raf and Flt‐1 as its main targets in a kinase panel.
Tobias Betzholz +7 more
wiley +1 more source
Cocristais farmacêuticos de furosemida: obtenção, caracterização e estudos de estabilidade [PDF]
Dissertação (mestrado) - Universidade Federal de Santa Catarina, Centro de Ciências da Saúde, Programa de Pós-Graduação em Farmácia, Florianópolis, 2013A Furosemida é um potente diurético de alça indicado para o tratamento de edema associado à ...
Rauber, Gabriela Schneider
core
A Review on Pharmaceutical Cocrystals
Pharmaceutical cocrystals are crystalline materials composed of two or more different molecules, at least one being an active pharmaceutical ingredient (API), in a fixed stoichiometric ratio, held together by non-covalent interactions.Cocrystal can be prepared by cocrystallization method.
Samina Sameer +3 more
openaire +1 more source
Abstract The intrinsic dynamic asymmetry between homologous PDZ domains in multidomain scaffold proteins offers insight into how they achieve multivalent partner recognition. Through a systematic x‐ray crystallographic analysis of tandem PDZ1–PDZ2 domains in human syntenin‐1 (SDCBP/MDA‐9), we solved nine high‐resolution structures and uncovered ...
Natsuno Ando +8 more
wiley +1 more source
Water activity (aw) was measured in eight DESs (10–90 wt% water). Strong DES–water interactions persist to ∼50 wt%, after which structure collapses toward aqueous‐like behavior. Redlich–Kister, Wilson, and COSMO‐RS models showed limited performance, whereas QSAR modeling using COSMOtherm‐derived σ‐profile descriptors significantly improved aw ...
Marko Rogošić +6 more
wiley +1 more source
Considering its low occurrence in the Cambridge Structural Database, is the amide–pyridyl synthon easy to form, and what structural factors affects its interaction energy and its subsequent formation?Nicotinamide (Nico) and derivatives of pyridine are important materials in both the pharmaceutical and agrochemical industries.
Oluwatoyin Akerele, Andreas Lemmerer
wiley +1 more source
This review describes how an integrated structural biology platform at Merck Sharp & Dohme LLC, Rahway, New Jersey, USA, combining X‐ray crystallography, cryo‐EM, MicroED and cryo‐ET, enables seamless three‐dimensional insights from molecular to cellular length scales.
Jill E. Chrencik +44 more
wiley +1 more source
Dissolution Advantage of Nitazoxanide Cocrystals in the Presence of Cellulosic Polymers
The effect of hydroxypropyl methylcellulose (HPMC) and methylcellulose (Methocel® 60 HG) on the dissolution behavior of two cocrystals derived from nitazoxanide (NTZ), viz., nitazoxanide-glutaric acid (NTZ-GLU, 1:1) and nitazoxanide-succinic acid ...
Reynaldo Salas-Zúñiga +6 more
doaj +1 more source
Pharmaceutical Cocrystals: An Overview
Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are the major constraints during the development of new product. Various approaches have been used for enhancement of solubility of poorly aqueous soluble drugs, but success of these approaches depends on physical and chemical nature of molecules being developed.
null Jagdish Kumar Rawal +1 more
openaire +1 more source

