1,5-Benzoxazepines as a unique and potent scaffold for activity drugs: A review.

Benzoxazepines constitute a huge number of organic compounds widely described in the literature. Many of them are distinguished by their biological properties. Among them, our attention was drawn to 1,5-benzoxazepine derivatives due to their interesting pharmacological properties. As is reported in the literature, these compounds are not only good building blocks in organic synthesis but also have interesting biological and pharmacological properties. This article is the first review publication to describe the synthesis methods and unique properties of 1,5-benzoxazepines. Literature reports widely describe the biological properties of 1,5-benzoxazepine, like anticancer, antibacterial, or antifungal activities. 1,5-Benzoxazepine derivatives can also interact with G-protein-coupled receptors and could be incorporated into new potential drugs, among others, in treating neuronal disorders like Alzheimer's and Parkinson's disease.

Structures 4-n-propyl Piperazines as Non-Imidazole Histamine H3 Antagonists.

Seven new low-temperature structures of 4-n-propylpiperazine derivatives, potential H3 receptor antagonists, have been determined by X-ray crystallography, with the following symmetry and unit cell parameters: 2-(4-propyl-piperazin-1-yl)oxazolo[4,5-c]pyridine (compound 1), P-1, 5.9496 Å, 12.4570 Å, 12.8656 Å, 112.445°, 95.687°, 103.040°; 2-(4-propyl-piperazin-1-yl)thia-zolo[4,5-c]pyridine (compound 2), I2/a, 22.2087 Å, 7.5519 Å, 19.9225 Å, ß = 92.368°; 2-(4-propyl-piperazin-1-yl)oxazolo[5,4-c]pyridine (compound 3), C2/c, 51.1351 Å, 9.36026 Å, 7.19352 Å, ß = 93.882°; 2-(4-propyl-piperazin-1-yl)thiazolo[5,4-c]pyridine (compound 4), Pbcn, 19.2189 Å, 20.6172 Å, 7.4439 Å; 2-(4-propylpiperazin-1-yl)[1,3]oxazolo[4,5-b]pyridine, hydrate (structure 5), Pbca, 7.4967 Å, 12.2531 Å, 36.9527 Å; 2-(4-propylpiperazin-1-yl)[1,3]oxazolo[4,5-b]pyridine, first polymorph (structure 6), P-1, 7.2634 Å, 11.1261 Å, 18.5460 Å, 80.561°, 80.848°, 76.840°; 2-(4-propylpiperazin-1-yl)[1,3]oxazolo[4,5-b]pyridine, second polymorph (structure 7), P21, 8.10852 Å, 7.06025 Å, 12.41650 Å, ß = 92.2991°. All the compounds crystallized out as hydrobromides. Oxazole structures show a much greater tendency to form twin crystals than thiazole structures. All the investigated structures display N-H···Br hydrogen bonding. (ADME) analysis, including the assessment of absorption, distribution, metabolism, and excretion, determined the physicochemical properties, pharmacokinetics, drug similarity, and bioavailability radar, and confirmed the usefulness of the compounds in question for pharmaceutical utility. This work is a continuation of the research searching for a new lead of non-imidazole histamine H3 receptor antagonists.