Molecular Conformations and Biological Activity of N-Hetaryl(aryl)alkyl-4-methyl-2,2-dioxo-1H-2λ^sup 6^, 1-benzothiazine-3-carboxamides

• Published in: Scientia pharmaceutica 2018-10, Vol.86 (4), p.1
• Main Authors: Ukrainets, Igor V, Hamza, Ganna M, Burian, Anna A, Voloshchuk, Natali I, Malchenko, Oxana V, Shishkina, Svitlana V, Grinevich, Lina A, Grynenko, Vasyl V, Sim, Galina
• Format: Article
• Language: English
• Subjects: Acids; Analgesics; Narcotics; Natural products; NMR; Nuclear magnetic resonance; Pain; Pharmaceuticals; Polymorphism
• ISSN: 0036-8709; 2218-0532
• DOI: 10.3390/scipharm86040050

According to the results of the pharmacological tests carried out on the model of carrageenan inflammation it has been found that all without exception N-hetaryl(aryl)alkyl-4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamides demonstrate the statistically significant analgesic and anti-inflammatory properties. [...]having decided сп the lhad compounp we did not stop searching for new analgesics. Unfortunately, factors causing changes in the phase composition are still unclear. [...]study of amide VI as an analgesic is considered inappropriate, at least, until the conditions, which would allow obtaining exceptionally high active crystalline modifications of the substance in pharmacological respect, are found, and they will be able to guarantee their stability during storage. Highly, moderately and low active analgeeics may well turri out to bl Idolh powarful antiphlogistics and completely inactive substances regardlets of (he spatial structure (see, for example N-thiophen-2-ylmethylamide 2g, N-3-methyl-benzylamide 3f and N -furan-2-ylmethylamide 2d, respectively). [...]thrs tesult is not surprising; and even quite natural rince the ability to suppress tire inflammxtory reaction is implemented through tire impact on completely different biological targets.