878671-94-4Relevant articles and documents
Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach
Li, Xiao,Huang, Boshi,Zhou, Zhongxia,Gao, Ping,Pannecouque, Christophe,Daelemans, Dirk,De Clercq, Erik,Zhan, Peng,Liu, Xinyong
, p. 241 - 253 (2016)
With the continuation of our unremitting efforts toward the discovery of potent HIV-1 NNRTIs, a series of novel imidazo[4,5-b]pyridin-2-ylthioacetanilides were designed, synthesized, and evaluated for their antiviral activities through combining bioisosteric replacement and structure-based drug design. Almost all of the title compounds displayed moderate to good activities against wild-type (wt) HIV-1 strain with EC50 values ranging from 0.059 to 1.41 μm in a cell-based antiviral assay. Thereinto, compounds 12 and 13 were the most active two analogues possessing an EC50 value of 0.059 and 0.073 μm against wt HIV-1, respectively, which was much more effective than the control drug nevirapine (EC50 = 0.26 μm) and comparable to delavirdine (EC50 = 0.038 μm). In addition, one selected compound showed a remarkable reverse transcriptase inhibitory activity compared to nevirapine and etravirine. In the end of this manuscript, preliminary structure–activity relationships (SARs) and molecular modeling studies were detailedly discussed, which may provide valuable insights for further optimization.
Thienopyrimidone acyl sulfonamide derivative as well as preparation method and application thereof
-
Paragraph 0032-0036, (2021/09/04)
The invention relates to a thienopyrimidone acyl sulfonamide derivative as well as a preparation method and application thereof. The thienopyrimidone acyl sulfonamide derivative has a structure as shown in a formula I. The invention also relates to a preparation method of the compound with the structure as shown in the general formula I and a pharmaceutical composition. The invention also provides application of the compound in preparation of anti-gout drugs.
Thienopyrimidinone mercaptoacetic acid derivative as well as preparation method and application thereof
-
Paragraph 0044; 0045; 0046; 0047, (2020/10/21)
The invention relates to an imidazopyridine mercaptoacetic acid derivative as well as a preparation method and application thereof. The compound has a structure shown as a formula I or a formula II which is described in the specification. The invention also relates to a preparation method and a pharmaceutical composition of the compound containing the structure shown in the formula I or II. The invention also provides application of the compound in preparation of anti-gout drugs.
Lesinurad analogue and its preparation method and medical use
-
, (2019/05/28)
The invention relates to a lesinurad analog as shown in the general formula (I), its preparation method, a pharmaceutical composition containing the derivative and an application of the pharmaceutical composition used as a therapeutic agent, especially as a medicine for treating hyperuricemia and gout, wherein definition of each substituent group in the general formula (I) is as the same as definition in the specification.