Synthesis, SAR and docking studies of substituted aryl phenylthiazolyl phenylcarboxamide as potential protein tyrosine phosphatase 1B (PTP1B) inhibitors
In our continued effort to discover novel PTP1B inhibitor with improved in vivo activity, we attempted to optimize our previously discovered lead compound by replacing the sulfonyl group with benzoyl group to yield compound II. Additional structural modif
Varshney, Kanika,Gupta, Amit K.,Rawat, Arun,Srivastava, Rohit,Mishra, Akansha,Saxena, Mridula,Srivastava, Arvind K.,Jain, Sudha,Saxena, Anil K.
SUBSTITUTED 4-ARYLTHIAZOLES AND PROCESS OF PREPARATION THEREOF
The present invention relates to novel substituted 4-arylthiazoles, their preparation, and to their use as therapeutic agents, particularly in the prevention or treatment of tuberculosis. The resent invention articularl relates to com ounds of formula A:
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Page/Page column 33-34
(2013/02/28)
Synthesis and biological evaluation of substituted 4-arylthiazol-2-amino derivatives as potent growth inhibitors of replicating Mycobacterium tuberculosis H37RV
In search of potential therapeutics for tuberculosis, we describe herein synthesis and biological evaluation of some substituted 4-arylthiazol-2-amino derivatives as modified analogues of the antiprotozoal drug Nitazoxanide (NTZ), which has recently been reported as potent inhibitor of Mtb H37Rv (Mtb MIC = 52.12 μM) with an excellent ability to evade resistance. Among the synthesized derivatives, the two compounds 7a (MIC = 15.28 μM) and 7c (MIC = 17.03 μM) have exhibited about three times better Mtb growth inhibitory activity over NTZ and are free from any cytotoxicity (Vero CC50 of 244 and 300 μM respectively). These two compounds represent promising leads for further optimization.
Roy, Kuldeep K.,Singh, Supriya,Sharma, Sandeep K.,Srivastava, Ranjana,Chaturvedi, Vinita,Saxena, Anil K.
p. 5589 - 5593
(2011/10/12)
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