当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Rational design, synthesis and antitubercular evaluation of novel 2-(trifluoromethyl)phenothiazine-[1,2,3]triazole hybrids.

Rational design, synthesis and antitubercular evaluation of novel 2-(trifluoromethyl)phenothiazine-[1,2,3]triazole hybrids.

Abstract：

:Molecular hybridization is an emerging structural modification tool to design molecules with better pharmacophoric properties. A series of novel 2-(trifluoromethyl)phenothiazine-1,2,3-triazoles 5a-v designed by hybridizing two antitubercular drugs trifluoperazine and I-A09 in a single molecular architecture, were synthesized in very good yields using click chemistry. Among the all '22' compounds screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (Mtb), three analogs 5c, 5l and 5o were found to be most potent (MIC: 6.25μg/mL) antitubercular agents with good selectivity index.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Addla D,Jallapally A,Gurram D,Yogeeswari P,Sriram D,Kantevari S

doi

10.1016/j.bmcl.2013.11.031

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

233-6

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01310-3

journal_volume

24

pub_type

杂志文章

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