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Title: Design and Synthesis of Purine Contained Piperazine Chloropicoline and Sacubitril Analogs as New Inhibitors for Mycobacterium Tuberculosis
Researcher: Srihari Konduri
Guide(s): Koya Prabhakara Rao
Keywords: Engineering and Technology
Engineering Chemical
University: Vignans Foundation for Science Technology and Research
Completed Date: 2021
Abstract: Tuberculosis (TB) is a contagious infection that is caused by an active Mycobacterium tuberculosis (Mtb) bacterium. This can be transmitted from one person to another person, and it has symptoms. TB is active without symptoms it is called latent TB. TB causes more deaths when compared with HIV/AIDS. Treatment of TB, one needs to use antibiotics individually or in combination with other drugs. In the first part of this study, we focused on purines connected to heterocyclic scaffolds such as pyrimidine and imidazole rings were designed as new heterocyclic scaffold. The compounds having purine ring exhibits different medicinal and biological applications including anti-TB activity and the main purine structure with phenyl sulfonamide evaluates the great activity against anti-TB. In this study, a sequence of thirty purine connected piperazine analogs (7-36), were prepared to recognize as influential inhibitors against Mycobacterium tuberculosis. The analogs were prepared by reacting respective intermediate scaffold compound with various acid chlorides and isocyanate/isothiocyanate reagents. Later, all these analogs were screened for their anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv. However, among these compounds, a group of six compounds (11, 24, 27, 32, 33, and 34) had shown more efficient agents when compared with the present reference drug ethambutol. The compounds outlined aim the biosynthesis of the peptidoglycan of similar MurB and apply efforts of antiproliferative. The anti-TB activity study was well comparable to computational molecular docking values, models giving greater interactions with MurB inhibitors giving a piece of information for the next evaluation of early clinical reagents against Mycobacterium tuberculosis. In the second part of work, we were interested to develop a new heterocyclic scaffold by mimicking the above two moieties in a single moiety for better anti-TB activity. newline
Pagination: 196
Appears in Departments:Division of Chemistry

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