- Design, synthesis and evaluation of novel N-phenylbutanamide derivatives as KCNQ openers for the treatment of epilepsy
-
KCNQ (Kv7) has emerged as a validated target for the development of novel anti-epileptic drugs. In this paper, a series of novel N-phenylbutanamide derivatives were designed, synthesized and evaluated as KCNQ openers for the treatment of epilepsy. These compounds were evaluated for their KCNQ opening activity in vitro and in vivo. Several compounds were found to be potent KCNQ openers. Compound 1 with favorable in vitro activity was submitted to evaluation in vivo. Results showed that compound 1 owned significant anti-convulsant activity with no adverse effects. It was also found to posses favorable pharmacokinetic profiles in rat. This research may provide novel potent compounds for the discovery of KCNQ openers in treating epilepsy.
- Yang, Shaoning,Lu, Dingqiang,Ouyang, Pingkai
-
p. 3004 - 3008
(2018/07/31)
-
- Synthesis and characterization of impurity B of S-(+)-clopidogrel bisulfate: An antiplatelet
-
S-(+)-Clopidogrel bisulfate [(S-(+)-methyl 2-(2-chlorophenyl)-2-(6, 7-dihydrothieno[3, 2-c]pyridin-5(4H)-yl)acetate bisulfate)] is a platelet aggregation inhibitor drug. S-(+)-Clopidogrel bisulfate is prepared by different synthetic approaches in the literature. In almost all the approaches the major impurities known in the literature (A, B, and C) are also listed in the U.S. pharmacopoeia. The control of these pharmaceutical impurities is currently a critical issue to the pharmaceutical industry. In this article, a description of these impurities and their origins in the S-(+)-clopidogrel bisulfate process are presented along with the preparation of impurity B.
- Reddy, K. Tatendra,Kumar, K. Suneel,Omprakash,Dubey
-
p. 1387 - 1396
(2013/05/22)
-