China 
Africa 
Explore chapters and articles related to this topic
Identification of New Diflunisal Derivatives as Potent In Vitro Transthyretin Fibril Inhibitors
Published in Gilles Grateau, Robert A. Kyle, Martha Skinner, Amyloid and Amyloidosis, 2004
T. Mairal, G. Arsequell, G. Valencia, I. Dolado, J. Nieto, A. Planas, J. Barluenga, A. Ballesteros, R. Almeida, M.J. Saraiva
It is known that certain classes of compounds such as salicylates, steroids, antibiotics (penicillin, triiodophenol), flavonoids, inotropic agents (milrinone) and PCBs bind with high affinity to transthyretin (TTR). More recently, some members of a number of these and other families of already known therapeutic compounds such as flavones, tetrahydroquinolines, dihydropyridines, benzodiazepines, NSAIDs, phenoxazines, stilbenes, benzoxazoles and natural products (resveratrol) have also been identified and characterized as in vitro TTR fibril inhibitors by limited screening studies (2).
HIV Integrase Inhibitors
Published in Satya Prakash Gupta, Cancer-Causing Viruses and Their Inhibitors, 2014
It was soon realized that polyhydroxylated aromatic compounds (catechol) are not selective inhibitors against IN 3′-processing or strand transfer reactions, show significant cytotoxicity, have low oral bioavailability, and are not metabolically stable. It could be because the cellular oxidation of catechol to semiquinone or orthoquinone results in reactive intermediate capable of interacting with other cellular targets. Attempts to improve the biological activity of catechol derivatives by substitution or removal of the hydroxyl group resulted in the complete loss of IN inhibitory activity. The National Cancer Institute (NCI) 3D database of pharmacophore-based searches and computational molecular modeling approaches identified several active structures devoid of catechol moiety (Neamati 2011). Among them, coumarins, hydrazides, quinones, sulfones, sulfonamides, diketo acids (DKAs), naphthyridines, and pyrimidinones were explored extensively. Raltegravir, the first FDA-approved IN inhibitor drug, was the result of research on pyrimidinone carboxamides, whereas elvitegravir, the second FDA-approved IN inhibitor drug, resulted from research on quinolinoyl carboxylic acids. Several other diverse compounds uniquely different from many examples mentioned earlier have been reported to inhibit IN. Some of them, such as thiazolothiazepines, chalcones, dihydropyridine carboxylic acids, benzoxazoles, tetrazoles, and benzene tricarboxamides, were extensively optimized in search of potent and selective IN inhibitors. Many QSAR studies on these inhibitors were reported and are discussed in this section.
Classifications
Published in Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani, Pharmacology in 7 Days for Medical Students, 2018
Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani
Centrally-acting muscle relaxantsBenzodiazepinesClorazepateDiazepamKetazolamMedazepamBenzoxazole derivativesBenzimidazoleChlorzoxazoneZoxazolamineGABA analogueBaclofenMiscellaneous compoundsCyclobenzaprineChlormezanoneChlorphensinMethocarbamolOrphenadrine HClOrphendrine citratePropanediol derivativesCarisoprodolMephenesinMeprobamateStyramate
Therapeutic potential of oxazole scaffold: a patent review (2006–2017)
Published in Expert Opinion on Therapeutic Patents, 2018
Ramandeep Kaur, Kezia Palta, Manoj Kumar, Meha Bhargava, Lalita Dahiya
Oxazole (1) is a well-known important heterocyclic motif characterized as 1,3-azole possessing oxygen and nitrogen atoms in 1,3 relationship of five membered ring. This was first reported by Hantzsch in 1887 and synthesized in 1947. Annuloline was the first demonstration of oxazole ring in nature. Benzo derivatives of oxazole are called as benzoxazole (2). Partially reduced oxazoles are called oxazolines and depending upon the position of the double bond are named as 2-oxazoline (3), 3-oxazoline (4), and 4-oxazoline (5), whereas, the fully saturated analog is called as oxazolidine (6). Oxazole is weakly basic liquid, miscible with water and organic solvents and has dipole moment of 1.5 D. Although the sextet of π-electrons is present in oxazole ring, its properties have demonstrated incomplete delocalization of π-electrons that attributes to its little aromaticity and greater dienic character. This lower aromaticity is not to be equated with instability [5–8].
Multi-targeted drug design strategies for the treatment of schizophrenia
Published in Expert Opinion on Drug Discovery, 2021
Piotr Stępnicki, Magda Kondej, Oliwia Koszła, Justyna Żuk, Agnieszka A. Kaczor
Huang et al. described new benzoxazole-piperidine derivatives with good dopamine D2 and also serotonin 5-HT1A and 5-HT2A receptor affinities. The most promising molecule (11) (Figure 3) displayed nanomolar affinity to D2 and serotonin 5-HT1A and 5-HT2A receptors (Ki = 10.6 ± 1.6; 21.3 ± 2.6; 27 ± 0.6), but low affinities to 5-HT2C and H1 receptors (Ki = 1987 ± 212; 3151 ± 388). In in vivo studies this substance decreased apomorphine-induced climbing and DOI-induced head twitching and did not cause any catalepsy [102].
2-Aminobenzoxazole-appended coumarins as potent and selective inhibitors of tumour-associated carbonic anhydrases
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Alma Fuentes-Aguilar, Penélope Merino-Montiel, Sara Montiel-Smith, Socorro Meza-Reyes, José Luis Vega-Báez, Adrián Puerta, Miguel X. Fernandes, José M. Padrón, Andrea Petreni, Alessio Nocentini, Claudiu T. Supuran, Óscar López, José G. Fernández-Bolaños
We envisioned the preparation of a small library of the hitherto unknown coumarin-benzoxazole hybrids depicted in Figure 1 to develop novel inhibitors of hCAs IX and XII. The numerous pharmacological properties associated with the benzoxazole skeleton, together with the reduced toxicities of its derivatives45, stimulated us to incorporate such scaffold and analyse the possibility of interactions with CAs.