3098-67-7Relevant articles and documents
Microwave-assisted synthesis of bis(N-substituted thiazol-2-amine) derivatives and their biological activities
Baba, N.H. Kumar,Ashok,Rao, Boddu Ananda,Sarasija, Madderla,Murthy,Srinivasarao, Vankadari,Parthasarathy, Tigulla
, p. 405 - 409 (2017)
New 4,4′-(4,6-dimethoxy-1,3-phenylene)-bis(N-substituted thiazol-2-amine) derivatives 5a-j were synthesized from 1,1′-(4,6-dimethoxy-1,3-phenylene)-bis(2-bromoethanone) 3 and substituted thioureas 4a-j under conventional and microwave irradiation conditio
Microwave assisted synthesis of some novel bis-(2-substituted imidazole[2,1-b] [1,3,4] thiadiazole) derivatives and their biological activities
Kumar Baba,Ashok,Rao, Boddu Ananda,Sarasija, Madderla,Murthy
, p. 163 - 168 (2018/09/14)
A new series of 6,6'-(4,6-dimethoxy-1,3-phenylene)bis (2- substituted imidazo[2,1-b] [1,3,4]thiadiazole) derivatives (5a-5h) were synthesized from corresponding 1,1'-(4,6-dimethoxy-1,3-phenylene)bis(2-bromoethanone) and substituted 1,3,4-thiadiazol-2-amine under conventional and microwave irradiation conditions. The structures of all the synthesized compounds were characterized by Fourier transform infrared,1H nuclear magnetic resonance (NMR),13C NMR, mass, and elemental analysis. All products were subjected to in vitro antibacterial and antimycobacterial evaluation. Some of the compounds exhibit good activities against Staphylococcus aureus (+ve), Bacillus subtilis (+ve) strains, and Mycobacterium bovis strain.
Leukotriene B4 Receptor Antagonists: The LY255283 Series of Hydroxyacetophenones
Herron, David K.,Goodson, Theodore,Bollinger, Nancy G.,Swanson-Bean, Dorothy,Wright, Ian G.,et al.
, p. 1818 - 1828 (2007/10/02)
A series of hydroxyacetophenones was prepared for evaluation as leukotriene B4 (LTB4) receptor antagonists, culminating in 1-oxy>phenyl>ethanone (compound 35, LY255283).Using an assay for inhibition of specific LTB4 binding to human PMN, we found that substitution of a nonpolar substituent in the 5-position was required for activity.Best activity was realized with hydrogen in the 3-position, hydroxyl in the 2-position, short chain alkyl ketone in the 1-position, and a six- or eight-carbon chain linking the oxygen in the 4-position with an unsaturated terminal function.Compound 35, having an IC50 of 87 nM in the binding assay, was chosen for further preclinical evaluation.