Volume-6, Issue-7, July 2020

Abstract

Zika Virus Disease (ZVD) is an emerging disease in India. Symptoms are generally mild but it's infection during pregnancy can cause other congenital malformations in infants. Because of its complications in pregnancy it becomes of public health importance. There was an epidemic in Jaipur in year 2018. This study was conducted to describe the epidemiologic curve and effects containment measures initiated by department of health to control it. Public health response initiated within three kilometer radius area from index case in the form of tracing & isolation of positive cases, tracking of fever cases & pregnant females in affected area. Vector control measures were taken and effect of control measures were assessed by difference in entomlogical indexes like Breateau Index (BI) and House index (HI). Total 159 Zika positive cases detected in 38 days, out of that 6 were from routine surveillance and 153 were from active surveillance. No mortality was reported. Timely containment measures were taken. Effect of these containment measures were significant (p<001) in the form of reduction in number of cases, Breauteau Index (BI) and House Index (HI). Number of cases became zero whereas mean BI and mean HI became less than 2 which was initially 35.01 and 21.72 respectively. It is concluded that with prompt public health response and intersectoral coordination resulted in containment of the outbreak.

Keywords: Zika Virus Disease (ZVD), Epidemic Curve, Containment Measures, Breateau Index, House Index.

References

Keywords: Zika Virus Disease (ZVD), Epidemic Curve, Containment Measures, Breateau Index, House Index.

Abstract

In the present designed work, we have synthesized imidazo[2,1-b][1,3,4]thiadiazole derivatives (6a1-a6 to 6d1-d6) by reaction of compound 3 with appropriate α-haloaryl ketones produce substituted imidazo thiadiazole derivatives (4a-d). In the next step, these compounds (4a–d) undergoes the Vilsmeier reaction to introduce formyl group on the substituted arylimidazo[2,1-b][1,3,4]thiadiazole derivatives to form carbaldehyde derivatives (5a–d) and finally in the last step of the reaction for the synthesis of designed molecules, a one-pot synthetic procedure was used. For this, the one-pot reaction of 5a–d, thiosemicarbazide and substituted α-haloaryl ketones were reacted together in different reaction condition in ethanol solvent at an optimum temperature around 80°C produces a corresponding derivatives (6a1-a6 to 6d1-d6) with a better yield. The IR, 1H-NMR, and mass spectroscopy techniques were used to confirm the structure of final products and all synthesized molecules were tested for antiTB and anti-fungal activity. The compounds 6a1, 6a2, 6a3, 6c1, 6c6 and 6d1 with MIC 1.6-6.25 µgm/ml displayed very good antitubercular and 6a1, 6a4, 6a5, and 6d1 displayed very good antifungal activity with MIC 5 µgm/ml due to electron withdrawing groups at 4th position to both phenyl rings which are attached to the thiazole of the imidazo thiadiazole and imidazo thiadiazole ring.

Keywords: Anti-fungal, Anti-tubercular, Imidazo[2,1-b][1,3,4], thiadiazole-5-carbaldehyde, One-pot synthesis, Vilsmeier reaction.

References

Keywords: Anti-fungal, Anti-tubercular, Imidazo[2,1-b][1,3,4], thiadiazole-5-carbaldehyde, One-pot synthesis, Vilsmeier reaction.

Abstract

The 2,4-diaminoquinazoline class of compounds has previously been identified as an effective inhibitor of Mycobacterium tuberculosis growth. We conducted an extensive evaluation of the series for its potential as a lead candidate for tuberculosis drug discovery. Three segments of the representative molecule N-(4-fluorobenzyl)-2-(piperidin-1-yl) quinazolin-4-amine were examined systematically to explore structure–activity relationships influencing potency. We determined that the benzylic amine at the 4-position, the piperidine at 2-position and the N-1 (but not N-3) are key activity determinants. The 3-deaza analog retained similar activity to the parent molecule. Biological activity was not dependent on iron or carbon source availability. We demonstrated through pharmacokinetic studies in rats that good in vivo compound exposure is achievable. A representative compound demonstrated bactericidal activity against both replicating and non-replicating M. tuberculosis. We isolated and sequenced M. tuberculosis mutants resistant to this compound and observed mutations in Rv3161c, a gene predicted to encode a dioxygenase, suggesting that the compound may act as a pro-drug.

Keywords: Tuberculosis Mycobacterium tuberculosis Antibacterial activity, 2,4-Diaminoquinazoline Dioxygenase.

References

Keywords: Tuberculosis Mycobacterium tuberculosis Antibacterial activity, 2,4-Diaminoquinazoline Dioxygenase.