Several factors have contributed to the continuous health threat of TB globally. HIV-infected patients are 19 times more likely to develop TB than HIV-negative subjects 3, 4. In 2019, TB resulted in nearly 1.4 million deaths, including 208,000 deaths among human immunodeficiency virus (HIV) positive patients 2. According to the World Health Organisation (WHO), TB is considered as one of the top 10 causes of death worldwide, and the leading cause of death from a single infectious agent 1. It is caused by the opportunistic bacillus Mycobacterium tuberculosis (MTB) which primarily attacks the lungs (pulmonary) but may later affect other parts (extra-pulmonary) of the body 1. Tuberculosis (TB) is a communicable infectious disease and a major cause of illness, particularly in low-income countries.
Thus, the indolizines warrant further development and may represent a novel promising class of InhA inhibitors and multi-targeting agents to combat drug-sensitive and drug-resistant MTB strains.
Further, a safety study ( in silico and in vitro) demonstrated no toxicity for these compounds. The X-ray diffraction analysis of the compound 4b was also carried out. In silico docking study revealed the enoyl-acyl carrier protein reductase (InhA) and anthranilate phosphoribosyltransferase as potential molecular targets for the indolizines. Compounds 2b–2d, 3a–3d, and 4a–4c were active against the H37Rv-MTB strain with minimum inhibitory concentration (MIC) ranging from 4 to 32 µg/mL, whereas the indolizines 4a–4c, with ethyl ester group at the 4-position of the benzoyl ring also exhibited anti-MDR-MTB activity (MIC = 16–64 µg/mL).
#Bruker apex ii duo ccd diffractometer series#
#Bruker apex ii duo ccd diffractometer generator#
It is equipped with a Copper MicroMax 003f X-ray generator and PILATUS R200K Hybrid Pixel Array Detector as well as an Oxford Cryosystems Cobra for variable temperature data collection from 90-400 K. Instrument is currently located on the BioSide of campus. Instrument is equipped with a Moly sealed tube and an Apex-II CCD detector as well as an Oxford Cryosystems Cryostream for variable temperature data collection from 90-400 K.ĭual source instrument equipped with a TRIUMPH monochromated Moly sealed tube and a Copper IµS. System features a Kappa goniometer and a Photon II detector as well as an Oxford Cryosystems Cryostream for variable temperature data collection from 90-400 K.
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