52715-11-4Relevant academic research and scientific papers
Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase
Luci, Diane K.,Jameson, J. Brian,Yasgar, Adam,Diaz, Giovanni,Joshi, Netra,Kantz, Auric,Markham, Kate,Perry, Steve,Kuhn, Norine,Yeung, Jennifer,Kerns, Edward H.,Schultz, Lena,Holinstat, Michael,Nadler, Jerry L.,Taylor-Fishwick, David A.,Jadhav, Ajit,Simeonov, Anton,Holman, Theodore R.,Maloney, David J.
, p. 495 - 506 (2014/02/14)
Human lipoxygenases (LOXs) are a family of iron-containing enzymes which catalyze the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Our group has taken a particular interest in platelet-type 12-(S)-LOX (12-LOX) because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Herein, we report the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino) benzenesulfonamide-based scaffold. Top compounds, exemplified by 35 and 36, display nM potency against 12-LOX, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties. In addition, both compounds inhibit PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells.
Synthesis, antimicrobial and genotoxic properties of some benzoimidazole derivatives
Benvenuti,Severi,Sacchetti,Melegari,Vampa,Zani,Mazza,Antolini
, p. 231 - 235 (2007/10/03)
A number of 1H-benzoimidazol-2-ylamine and of 1-methyl-1H- benzoimidazol-2-ylamine derivatives were synthesized and the crystal and molecular structure of N-[4-(2-amino-benzoimidazole-1-sulfonyl)-phenyl] acetamide was determined by X-ray diffraction analysis. The compounds obtained were investigated for antimicrobial and genotoxic activities.
Functionalized azoles and triazolo[1,5-a]pyrimidines as latent leishmanicides
Ram, Vishnu Ji,Srivastava, Pratibha,Singh, Sunil K.,Kandpal, Mamta,Tekwani
, p. 1087 - 1090 (2007/10/03)
Triazolo[1,5-a]pyrimidine (3-6), benzoxazole (7a,b) and benzimidazole (7c) derivatives have been synthesized and evaluated for their in vitro leishmanicidal activity against L. donovani promastigotes.
Syhthesis of N4-substituted sulphanilamides and evaluation of their antibacterial efficacy
Seshadri, S,Sanghavi, N M,Tawate, S R,Naik, R V,Fruitwala, M A
, p. 748 - 752 (2007/10/02)
Pharmacologically active compounds belonging to the classes of p-thiocyano and p-aminobenzene sulphonamides have been synthesised and their antimicrobial activity evaluated against Gram + ve and Gram - ve bacteria.The compounds of both the classes show more inhibition of Gram -ve bacteria as compared to Gram + ve.
