Disease relevance of aminothiazole

• Pharmacokinetic studies on ceftazidime, an aminothiazole cephalosporin with a wide spectrum of antibacterial activity, including activity against Pseudomonas aeruginosa, were performed in patients with nosocomial pneumonia [1].
• The antibacterial activity of BMY-28142, a new aminothiazole cephalosporin, was measured by standardized broth microdilution and agar dilution methods against 450 gram-positive and gram-negative bacteria isolated from pediatric infections, including acute pulmonary exacerbations of cystic fibrosis [2].
• Ureas of 5-aminopyrazole and 2-aminothiazole inhibit growth of gram-positive bacteria [3].
• Ureas of 5-aminopyrazole and 2-aminothiazole emerged as lead compounds from a high-throughput screen assaying the growth of Staphylococcus aureus [3].
• A randomised double blind trial of 2-(2-Hydroxy-4-methylphenyl) Aminothiazole Hydrochloride 0.1% (CBS 113A) versus placebo was carried out in 43 eyes with episcleritis [4].

Psychiatry related information on aminothiazole

• Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease [5].

High impact information on aminothiazole

• In contrast, 4-ethylpyridine, 4-methylpyrimidine, acetylguanidine, ethylguanidine, 2-aminothiazole, 2amino-4,5-dimethylthiazole, L-histidine, and 7-nitroindazole resulted in high spin heme complexes of eNOS, similar to that observed with L-arginine [6].
• 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor [7].
• The enzyme kinetics associated with the VEGFR-2 inhibition of 14 (Ki=49+/-9 nM) confirmed that the aminothiazole-based analogues are competitive with ATP [8].
• Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities [9].
• When the crystal structures of aztreonam and related monobactams were studied and projected into an active-site model of the PC1 beta-lactamase, it became apparent that the two lysine residues might serve equivalent roles by interacting with the carboxylate of the aminothiazole oxime side chain [10].

Chemical compound and disease context of aminothiazole

• Role of an aminothiazole derivative on ethanol- and thermally oxidized sunflower oil-induced toxicity [11].
• A series of derivatives of 4-arylthiazole acetic acid and 2-aminothiazole were studied with respect of their antiinflammatory effect in rat carrageenin edema [12].

Biological context of aminothiazole

• Structure-based drug design to the discovery of new 2-aminothiazole CDK2 inhibitors [13].
• Cefodizime (HR 221), a parenteral aminothiazole cephalosporin, does not affect hemostasis [14].

Anatomical context of aminothiazole

• In contrast, an investigational aminothiazole cephem, CGP 31523A, produced a new combination of antibacterial effects: it was highly bactericidal without causing cell wall degradation or lysis [15].
• A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay [16].
• At therapeutic concentrations a pronounced stimulation of murine lymphocyte transformation was caused by carbapenems, aminothiazole cephalosporins and imidazoles [17].

Associations of aminothiazole with other chemical compounds

• Under acidic pH conditions of admixtures the aminothiazole moiety of aztreonam was diazotized by the nitrite ion contributed by metronidazole solutions [18].

Gene context of aminothiazole

• In this study, we evaluated the inhibitory activity of a series of 2-aminothiazole derivatives against both iNOS and neuronal NOS (nNOS) [19].
• Optimization of 2-aminothiazole derivatives as CCR4 antagonists [20].
• A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity, and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay [21].
• The most potent analogue identified to date, aminothiazole 8z, inhibits the dual specificity phosphatase Cdc25B with a Ki of 4.6+/-0.4 microM and a Hill coefficient of 2 [22].

Analytical, diagnostic and therapeutic context of aminothiazole

• In this study, we show by titration calorimetry that 2-aminothiazole binds to W191G with a Kd of 0.028 mM at pH 6 [23].

References