Child presenting with ocular ecchymosis

Singh, Sweta; Kumar, Jaidrath; Abhishek, Ankit

doi:10.4103/ojo.ojo_181_2018

Cited by 7 publications

(1 citation statement)

References 4 publications

(3 reference statements)

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“…TB primarily affects the lungs through the airborne transmission of bacteria when infected individuals cough, sneeze, or spit [ 4 , 5 , 6 , 7 ]. Upon entering the bloodstream, the bacteria can attack other organs and tissues, including the brain, kidneys, bones, spine, skin, peripheral lymph nodes, heart, pancreas, thyroid, spleen, eye, and skeletal muscles [ 8 , 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 ].…”

Section: Introductionmentioning

confidence: 99%

Benzothiadiazinone-1,1-Dioxide Carbonic Anhydrase Inhibitors Suppress the Growth of Drug-Resistant Mycobacterium tuberculosis Strains

Bua,

Bonardi,

Mük

et al. 2024

IJMS

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2H-Benzo[e][1,2,4]thiadiazin-3(4H)-one 1,1-dioxide (BTD) based carbonic anhydrase (CA) inhibitors are here explored as new anti-mycobacterial agents. The chemical features of BTD derivatives meet the criteria for a potent inhibition of β-class CA isozymes. BTD derivatives show chemical features meeting the criteria for a potent inhibition of β-class CA isozymes. Specifically, three β-CAs (MtCA1, MtCA2, and MtCA3) were identified in Mycobacterium tuberculosis and their inhibition was shown to exert an antitubercular action. BTDs derivatives 2a-q effectively inhibited the mycobacterial CAs, especially MtCA2 and MtCA3, with Ki values up to a low nanomolar range (MtCA3, Ki = 15.1–2250 nM; MtCA2, Ki = 38.1–4480 nM) and with a significant selectivity ratio over the off-target human CAs I and II. A computational study was conducted to elucidate the compound structure-activity relationship. Importantly, the most potent MtCA inhibitors demonstrated efficacy in inhibiting the growth of M. tuberculosis strains resistant to both rifampicin and isoniazid—standard reference drugs for Tuberculosis treatment.

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