- BSA binding and antibacterial studies of newly synthesized 5,6-Dihydroimidazo[2,1-b]thiazole-2-carbaldehyde
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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.
- Yallur, Basappa Chanabasappa,Katrahalli, Umesha,Krishna, Panchangam Murali,Hadagali, Manjunatha Devagondahalli
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- Synthetic method 2- bromomalondialdehyde (by machine translation)
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The synthesis method is characterized by 2 - comprising the following steps, bromo - 1111, 3-propylene glycol as a raw material: water as a solvent 2 - under basic conditions to obtain, bromomalondialdehyde, with a catalyst 2, 2, 6, 6 - with sodium hypochlorite, to obtain the target, compound, with, purity more than, % of product, quality. 2 - The method, comprises the following steps of: refining sodium hypochlorite with sodium hypochlorite solution at a low temperature; and filtering 99%; with sodium hypochlorite by a, one-step method as a. catalyst body TEMPO to obtain an aldehyde, by a one-step method. (by machine translation)
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Paragraph 0020; 0022-0039
(2020/03/29)
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- Method for synthesizing 5-bromo-7-azaindole
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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.
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Paragraph 0019; 0027-0028
(2019/06/07)
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- Synthesis method of 3-bromoquinoline compound
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The invention provides a synthesis method of a 3-bromoquinoline compound. The invention belongs to the field of medical chemical synthesis. The synthesis method comprises the following steps: taking 1, 1, 3, 3-tetramethoxypropane 2 as a raw material to react with bromine to obtain an intermediate 3, obtaining an intermediate 4 from the intermediate 3 under the action of alkali, and reacting the intermediate 4 with a substituted aniline compound to obtain the 3-bromoquinoline compound 1, wherein R1 and R2 are selected from any one of hydrogen, alkyl, alkoxy, halogen, ester, nitro, trifluoromethyl, trifluoromethoxy, dimethylamino, acetyl and methylthio. The synthesis method of the 3-bromoquinoline compound has the advantages of few reaction steps, simplicity in operation, cheap and easily available raw materials, high yield, easiness in purification and easiness in amplified production.
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Paragraph 0025-0027
(2019/07/04)
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- Synthesis and SAR study of new thiazole derivatives as vascular adhesion protein-1 (VAP-1) inhibitors for the treatment of diabetic macular edema
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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.
- Inoue, Takayuki,Morita, Masataka,Tojo, Takashi,Yoshihara, Kousei,Nagashima, Akira,Moritomo, Ayako,Ohkubo, Mitsuru,Miyake, Hiroshi
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p. 1219 - 1233
(2013/03/28)
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- Stereoselective process for the synthesis of chiral garft compounds and intermediates
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The present invention describes a stereoselective preparation of derivatives and precursors of molecules having formula 1: Method of preparing the compounds, intermediates and derivatives are described. The methods described herein allow the preparation o
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Page/Page column 25
(2010/02/11)
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- Synthesis of (6R)- And (6S)-5,10-dideazatetrahydrofolate oligo-γ-glutamates: Kinetics of multiple glutamate ligations catalyzed by folylpoly-γ-glutamate synthetase
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Folylpoly-γ-glutamate synthetase (FPGS, EC 6.3.2.17) catalyzes the ATP-dependent ligation of glutamic acid to reduced folates including (6S)-5,6,7,8-tetrahydrofolate (H4PteGlu), as well as to anticancer drugs such as 5,10-dideaza-5,6,7,8-tetrahydrofolate ((6R)-DDAH 4PteGlu1, (6R)-DDATHF, Lometrexol(tm)). Synthesis of unlabeled mono- and polyglutamates, DDAH4PteGlu n (6R, n = 1-6; 6S, n = 1-2), as well as (6R)-DDAH 4Pte[14C]Glu1, was effected from (6R)- or (6S)-5,10-dideazatetrahydropteroyl azide and glutamic acid, H-Glu-γ- Glun-y-Glu-OH (n = 0-4), or [14C]glutamic acid, respectively. These compounds were evaluated as FPGS substrates to determine steady-state kinetic constants. Michaelis-Menten kinetics were observed for (6-R)-DDAH4PteGlu1, the isomer corresponding to H 4PteGlu, whereas marked substrate inhibition was observed for (6S)-DDAH4PteGlun (n = 1-2) and (6R)-DDAH 4PteGlun (n = 2-5), but not (6.R)-DDAH 4PteGlu6. Multiple ligation of glutamate renders a quantitative analysis of these data difficult. However, approximate values of KM = 0.65-1.6 μM and K1, = 144-417 μM for DDAH 4PteGln were obtained using a simple kinetic model. The Royal Society of Chemistry 2005.
- Tomsho, John W.,McGuire, John J.,Coward, James K.
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p. 3388 - 3398
(2007/10/03)
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- Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis
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Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and
- Francisco, Gerardo D.,Li, Zhong,Albright, J. Donald,Eudy, Nancy H.,Katz, Alan H.,Petersen, Peter J.,Labthavikul, Pornpen,Singh, Guy,Yang, Youjun,Rasmussen, Beth A.,Lin, Yang-I.,Mansour, Tarek S.
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p. 235 - 238
(2007/10/03)
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- THIAZOLE DERIVATIVES AND THEIR USE AS VAP-1 INHIBITORS
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A compound of the formula (I): R1-NH-X-Y-Z (I) wherein R1 is acyl; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond, lower alkylene or -COHN-; and Z is a groupe of the formulae (II) or (III) wherein R
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- 2-[[2-Methyl-1-[2-benzoyl(or benzyl)phenyl]-1H-imidazol-5-yl]methyl]-1H-isoindole-1,3(2H)-diones
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A multistep process is presented for the preparation of imidazobenzodiazepines of the formula STR1 wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl. Also presented are novel intermediates utilized in the process. The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants. The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
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