Sriram, Dharmarajan’s team published research in Chemical Biology & Drug Design in 75 | CAS: 76283-09-5

Chemical Biology & Drug Design published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C16H20N2, COA of Formula: C7H5Br2F.

Sriram, Dharmarajan published the artcileSynthesis and antimycobacterial evaluation of novel phthalazin-4-ylacetamides against log- and starved phase cultures, COA of Formula: C7H5Br2F, the publication is Chemical Biology & Drug Design (2010), 75(4), 381-391, database is CAplus and MEDLINE.

Twenty four novel 2-[3-(4-bromo-2-fluorobenzyl)-4-oxo-3,4-dihydro-1-phthalazinyl]acetic acid amides were synthesized from phthalic anhydride and were subjected to in vitro and in vivo evaluation against log- and starved phase of mycobacterial species and Mycobacterium tuberculosis isocitrate lyase enzyme inhibition studies. Among the compounds screened, 2-(2-(4-bromo-2-fluorobenzyl)-1,2-dihydro-1-oxophthalazin-4-yl)-N-(2,6- dimethylphenyl)acetamide (I) inhibited all eight mycobacterial species with MIC’s ranging from 0.08 to 5.05 μM and was non-toxic to Vero cells till 126.43 μM. Four compounds were tested against starved culture of Mycobacterium tuberculosis and they inhibited with MIC’s ranging from 3.78 to 23.2 μM. Some compounds showed 40-66% inhibition against Mycobacterium tuberculosis isocitrate lyase enzyme at 10 μM. The docking studies also confirmed the binding potential of the compounds at the isocitrate lyase active site. In the in vivo animal model, I reduced the mycobacterial load in lung and spleen tissues with 1.38 and 2.9-log10 protections, resp., at 25 mg/kg body weight dose.

Chemical Biology & Drug Design published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C16H20N2, COA of Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary