2065-75-0Relevant articles and documents
Honeybourne
, p. 49 (1978)
BSA binding and antibacterial studies of newly synthesized 5,6-Dihydroimidazo[2,1-b]thiazole-2-carbaldehyde
Yallur, Basappa Chanabasappa,Katrahalli, Umesha,Krishna, Panchangam Murali,Hadagali, Manjunatha Devagondahalli
, (2019)
A new heterocyclic compound, 5,6-Dihydroimidazo[2,1-b]thiazole-2-carbaldehyde (ITC) was synthesized and its antibacterial activity and also its interaction with bovine serum albumin (BSA) were studied. The structure of the synthesized compound was confirmed by 1H NMR, 13C NMR and IR spectroscopic techniques. The antibacterial activity was carried out by minimum inhibitory concentration (MIC) method. The compound showed a good antibacterial activity. The mechanism of interaction between the BSA and ITC under physiological conditions was investigated by various molecular spectroscopic techniques like, fluorescence, circular dichroism (CD), UV absorption and FT-IR. The interaction between ITC and BSA was followed by studying the quenching of intrinsic fluorescence of BSA upon the addition of ITC at three different temperatures. The binding constant (K), Stern-Volmer quenching constant (Ksv) and number of binding sites were determined. The separation distance between BSA and ITC was evaluated based on the fluorescence resonance energy transfer theory. The conformational changes in BSA upon binding of ITC were also confirmed. The interference of some metal ions on interaction was studies. The displacement studies with site specific markers confirm that the site III was the binding site for ITC on BSA.
Method for synthesizing 5-bromo-7-azaindole
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Paragraph 0019; 0027-0028, (2019/06/07)
The invention provides a method for synthesizing 5-bromo-7-azaindole, and belongs to the field of medicinal chemical synthesis. The method comprises the following steps: reacting a raw material 1,1,3,3-tetramethoxypropane 2 with bromine to obtain an intermediate 3, preparing an intermediate 4 from an intermediate 3 under the action of an alkali, and reacting the intermediate 4 with 2-aminopyrroleto obtain the 5-bromo-7-azaindole 1. The method has the advantages of few reaction steps, easily available raw materials, high yield, small pollution, and easiness in amplified production.
Synthesis and SAR study of new thiazole derivatives as vascular adhesion protein-1 (VAP-1) inhibitors for the treatment of diabetic macular edema
Inoue, Takayuki,Morita, Masataka,Tojo, Takashi,Yoshihara, Kousei,Nagashima, Akira,Moritomo, Ayako,Ohkubo, Mitsuru,Miyake, Hiroshi
, p. 1219 - 1233 (2013/03/28)
Vascular adhesion protein-1 (VAP-1), an amine oxidase that is also known as a semicarbazide-sensitive amine oxidase (SSAO), is present in particularly high levels in human plasma, and is considered a potential therapeutic target for various inflammatory diseases, including diabetes complications such as macular edema. In our VAP-1 inhibitor program, structural modifications following high-throughput screening (HTS) of our compound library resulted in the discovery that thiazole derivative 10, which includes a guanidine group, shows potent human VAP-1 inhibitory activity (IC50 of 230 nM; rat IC 50 of 14 nM). Moreover, compound 10 exhibited significant inhibitory effects on ocular permeability in STZ-induced diabetic rats.