16189-10-9Relevant articles and documents
COMPOUNDS AND COMPOSITIONS FOR OCULAR DELIVERY
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Page/Page column 108; 178-179, (2020/05/12)
The present invention provides new prodrags of Sunitinib, Brinzolamide, and Dorzolamide and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (TOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.
Synthesis of a series of benzothiazole amide derivatives and their biological evaluation as potent hemostatic agents
Nong, Wenqian,Zhao, Anran,Wei, Jinrui,Cheng, Hui,Luo, Xuan,Lin, Cuiwu
, p. 6231 - 6241 (2018/02/19)
A series of benzothiazole amide derivatives were synthesized through a facile and efficient method via a nucleophilic acyl substitution reaction between 2-aminobenzothiazole and various cinnamic acid compounds. The obtained products exhibited good thermal stabilities. All compounds were evaluated for their in vitro hemostatic activities using the commercially available standard drug etamsylate as a positive control. The results showed that compound Q2 had a significant partial coagulation activity, reduced capillary permeability at 5, 10 and 50 μmol L-1, activated thrombin activity, and a more potent platelet aggregation activity than the positive control group (etamsylate, up to 1283.9 times in the nanomole range). A molecular modeling study revealed that compound Q2 was a competitive thrombin activator. Therefore, Q2 may be a potential lead for further biological screening and for the generation of drug molecules. Moreover, the structure-activity relationship of the prepared compounds is also discussed herein.
Synthesis of novel 1,2,5-oxadiazoles and evaluation of action against Acinetobacter baumannii
Christoff, Rebecca M.,Murray, Gerald L.,Kostoulias, Xenia P.,Peleg, Anton Y.,Abbott, Belinda M.
supporting information, p. 6267 - 6272 (2017/10/13)
With multidrug resistant bacteria on the rise, novel antibiotics are becoming highly sought after. In 2008, eleven compounds were identified by high throughput screening as inhibitors of BasE, a key enzyme of the non-ribosomal peptide synthetase pathway found in Acinetobacter baumannii. Herein, we describe the preparation of four structurally similar heterocyclic lead compounds from that study, including one 1,2,5-oxadiazole. A further library of 30 analogues containing the oxadiazole moiety was then generated. All compounds were screened against Acinetobacter baumannii and their minimum inhibitory concentration data is reported, with (E)-3-(2-hydroxyphenyl)-N-(4-methyl-1,2,5-oxadiazol-3-yl)acrylamide 32 found to have an MIC of 0.5 mM. This work provides the foundation for further investigation of 1,2,5-oxadizoles as novel inhibitors of A. baumannii.
Synthesis and biological evaluation of a new series of cinnamic acid amide derivatives as potent haemostatic agents containing a 2-aminothiazole substructure
Nong, Wenqian,Zhao, Anran,Wei, Jinrui,Lin, Xiao,Wang, Lisheng,Lin, Cuiwu
supporting information, p. 4506 - 4511 (2017/09/12)
Ten new cinnamic acid derivatives containing a 2-aminothiazole substructure were designed and synthesized. This series of compounds exhibited good thermostabilities as demonstrated by thermogravimetric analysis. In coagulation assays (prothrombin time, activated partial thromboplastin time and thrombin time) in vitro, most compounds demonstrated excellent activities to promote blood coagulation. Among the studied series, compounds N1, N4, N5 and W5 exhibited a significant coagulation activity. Further studies indicated that compound N5 (IC50 = 1.87 μmol/L) displayed the most suitable efficacy of promoting platelet aggregation than the clinically used haemostatic drug etamsylate (IC50 = 46.22 μmol/L). Furthermore, the relationship between the functional groups of the compounds and the corresponding blood coagulant activity was explored in this study.
Novel enzymatic synthesis of 4-O-cinnamoyl quinic and shikimic acid derivatives
Armesto, Nuria,Ferrero, Miguel,Fernandez, Susana,Gotor, Vicente
, p. 5784 - 5787 (2007/10/03)
The first direct synthesis of 4-O-cinnamoyl derivatives of quinic and shikimic acids were accomplished by regioselective esterification with Candida antarctica lipase A. For hydrocinnamic esters, enzymatic transesterification with vinyl esters gave excell
Two new improved approaches to the synthesis of coumarin-based prodrugs
Zheng, Ailian,Wang, Wei,Zhang, Huijuan,Wang, Binghe
, p. 4237 - 4254 (2007/10/03)
Our laboratory has recently reported the development of a coumarin- based, esterase-sensitive prodrug system for the preparation of prodrugs of amines, peptides, and peptidomimetics. Biological evaluations including animal studies have demonstrated the cl
SIDE REACTIONS IN THE PHASE TRANSFER CATALYZED WITTIG-HORNER SYNTHESIS. A CONVENIENT METHOD OF PREPARATION OF HYDROXYCINNAMIC ACIDS.
Chenault, J.,Dupin, J. F. E.
, p. 1059 - 1066 (2007/10/02)
Reaction between triethylphosphonoacetate and acetylated hydroxy aromatic aldehydes gives hydroxycinnamic acids except for ortho acetylated componds where the Knoevenagel product is sometimes obtained.
