Substituted 1H-pyrazolo[3,4-b]pyridine-4- and 1H-pyrazolo[3,4-b]pyridine-6-carboxamides have been synthetized through a Doebner–Ugi multicomponent reaction sequence in a convergent and versatile manner using diversity generation strategies: combination of two multicomponent reactions and conditions-based divergence strategy. The target products contain as pharmacophores pyrazolopyridine and peptidomimetic moieties with four points of diversity introduced from readily available starting materials including scaffold diversity. A small focused compound library of 23 Ugi products was created and screened for antibacterial activity.
An effective synthesis of (3H-quinazoline-4-ylidene)hydrazides of N-carboxyalkyl-(arylalkyl-,aryl-)isoindoline-1,3-diones, using activated N-protected aminoacids and 4-hydrazinoquinazoline was proposed in the framework methodology of directed search of hypoglycemic agents (fragment-oriented design, molecular docking). These hydrazides prepared via cyclocondensation under acid catalysis were converted to the corresponding 2-([1,2,4]triazolo[1,5-c]quinazoline-2-yl-) alkyl-(alkylaryl-,aryl-)-hydroisoindole-1,3(2H)-diones. The structure of synthesized compounds was established using IR, 1 H and 13 C NMR spectroscopy and LC-MS and the features of spectral pattern were discussed. The results of pharmacological screening revealed a series of compounds, that are short-acting hypoglycemic agents like prandial regulators of glucose (Mitiglinide). The SAR analysis showed, that the introduction of a hydrogenated 1,3-dioxoisoindole moiety bonded through linker groups with 4-hydrazinoquinazoline and triazolo[1,5-c]quinazoline cycles is reasonable in the context of searching for short-acting hypoglycemic agents and requires further research.
bc d eIUfMR gh jh c d eLMkOI lh mh c d nMoXRJTOM p h eq r d eLMkOI mq gq ;tu< :7 9999G 9996G 3614G 9/9.v . wxyz{|}~ y{ xy|y~ z~y~ y z~z } y x |}~ y{ xy|y~ y z~z } y 0 CFBFD 0 C 4 5 x x}~y | x }z y ¡¢ {}x~ £z¢ x¤ y ¤ yx y
A possibilidade do uso de um novo derivado de acridina, munido de um grupo doador de elétrons, como modificador de elétrons para a detecção do conteúdo total do ácido gálico em goma de alfarroba tem sido avaliada mediante uma análise teórica. O modelo matemático correspondente foi analisado mediante a teoria de estabilidade linear e análise de bifurcações. Foi mostrado que o derivado fosfazoico da acridina pode servir de modificador eficiente para a detecção eletroanalítica do conteúdo total do ácido gálico em alfarroba. As causas dos comportamentos oscilatório e monotônico também foram detectadas.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.