717-37-3Relevant articles and documents
Synthesis and antibacterial activity of novel 4″-O-benzimidazolyl clarithromycin derivatives
Cong, Chao,Wang, Haiyang,Hu, Yue,Liu, Chen,Ma, Siti,Li, Xin,Cao, Jichao,Ma, Shutao
, p. 3105 - 3111 (2011/07/08)
Novel 4″-O-benzimidazolyl clarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. These benzimidazolyl derivatives exhibited excellent activity against erythromycin-susceptible strains better than the references, and some of them showed greatly improved activity against erythromycin-resistant strains. Compounds 16 and 17, which have the terminal 2-(4-methylphenyl)benzimidazolyl and 2-(2-methoxyphenyl)benzimidazolyl groups on the C-4″ bishydrazide side chains, were the most active against erythromycin-resistant Staphylococcus pneumoniae expressing the erm gene and the mef gene. In addition, compound 17 exhibited the highest activity against erythromycin-susceptible S. pneumoniae ATCC49619 and Staphylococcus aureus ATCC25923 as well. It is worth noting that the 4″-O-(2-aryl)benzimidazolyl derivatives show higher activity against erythromycin-susceptible and erythromycin-resistant strains than the 4″-O-(2-alkyl)benzimidazolyl derivatives.
Benzimidazole compounds
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Page column 80-81, (2010/02/05)
A benzimidazole compound represented by the formula (I): wherein R3is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.
Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates
Cui, Jingrong Jean,Araldi, Gian-Luca,Reiner, John E.,Reddy, Komandla Malla,Kemp, Scott J.,Ho, Jonathan Z.,Siev, Daniel V.,Mamedova, Lala,Gibson, Tony S.,Gaudette, John A.,Minami, Nathaniel K.,Anderson, Susanne M.,Bradbury, Annette E.,Nolan, Thomas G.,Semple
, p. 2925 - 2930 (2007/10/03)
Novel, potent, and highly selective classes of thrombin inhibitors were identified, which resulted from judicious combination of P4-aromatics and P2-P3-heterocyclic dipeptide surrogates with weakly basic (calcd pKa ～non-basic - 8.6) bicyclic P1-arginine mimics. The design, synthesis, and biological activity of achiral, non-covalent, orally bioavailable inhibitors NC1-NC44 featuring P1-indazoles, benzimidazoles, indoles, benzotriazoles, and aminobenzisoxazoles is disclosed.
