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.
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.
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.
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.
