Benzothiazinone-piperazine derivatives as efficient Mycobacterium tuberculosis DNA gyrase inhibitors

Chandran, Manoj; Renuka, Janupally; Sridevi, Jonnalagadda Padma; Pedgaonkar, Ganesh S.; Vanaparthi, Asmitha; Yogeeswari, Perumal; Sriram, Dharmarajan

doi:10.1016/j.ijmyco.2015.02.002

Cited by 28 publications

(15 citation statements)

References 15 publications

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“…The IPT adherence rate in this study was much higher than that reported from southern India and that reported from another study in southern Ethiopia [ 24 ]. In Pakistan, of 184 under-five children enrolled in IPT, 60 (32.6%) completed six months of IPT [ 25 ]. But, in the South African report [ 18 ], only 15% achieved four months of therapy.…”

Section: Discussionmentioning

confidence: 99%

Adherence to Isoniazid Preventive Therapy among Under-Five Children in Contact with Adult Bacteriologically Confirmed Pulmonary Tuberculosis Patients: A Mixed-Method Study

Seid

Tsedalu

Ayele

2020

International Journal of Microbiology

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Background. The World Health Organization recommends that all children below the age of five who have household contact with an infectious tuberculosis case should receive isoniazid preventive treatment for at least six months after the active tuberculosis disease has been ruled out. This research aims to determine the adherence of children, eligible for isoniazid preventive treatment, to the treatment who had contact with pulmonary tuberculosis patients. Methods. A mixed study design was used to prospectively assess the adherence to IPT among children under the age of 5 in contact with pulmonary TB patients through the quantitative study design and barriers of adherence in view of health care professionals and the family of children through a descriptive qualitative study. The study was conducted from July 2019 to December 2019 in Addis Ababa. Data were collected by a structured datasheet from the selected health center registration book. Data were entered into Epi Data software and analyzed by using SPSS version 20. Descriptive statistical methods were used to summarize the sociodemographic characteristics of the study participants. Result. The ratio of the total number of pulmonary tuberculosis index cases recruited into the study to the number of child contacts aged less than 5 years was 1 : 1.32. The total isoniazid preventive treatment uptake in this study was 75.2%; one-fifth (21.3%) of the children who started IPT did not complete the full course of six-month isoniazid preventive treatment. Except for HIV not to be tested ( P < 0.001 ), there was no significant association of the listed risk factors in default to complete the full six months of preventive treatment. Conclusion. Enrolment of eligible children for isoniazid preventive treatment in the urban city Addis Ababa was still below the target of the World Health Organization End tuberculosis strategy by 2030. The treatment adherence rate also needs a great deal of effort to achieve the strategy. Child default after the first visit indicates a lack of understanding about the benefit and safety of preventive therapy in young children among families of TB patients, and awareness-creating efforts by health extension workers will help to improve the outcomes.

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Section: Discussionmentioning

confidence: 99%

Adherence to Isoniazid Preventive Therapy among Under-Five Children in Contact with Adult Bacteriologically Confirmed Pulmonary Tuberculosis Patients: A Mixed-Method Study

Seid

Tsedalu

Ayele

2020

International Journal of Microbiology

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“…The IPT completion rate of 80% in this study was much higher than the 23% reported from southern India, 24% reported among HIV-infected patients [ 18 ] and 12% reported from another study in southern Ethiopia [21. In Pakistan, of 184 under-five children enrolled in IPT, 60 (32.6%) completed six months of IPT [ 22 ]. But in the South African report [ 18 ], only 15% achieved four months of therapy.…”

Section: Discussionmentioning

confidence: 99%

Uptake of Isoniazid Preventive Therapy among Under-Five Children: TB Contact Investigation as an Entry Point

et al. 2016

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A child’s risk of developing tuberculosis (TB) can be reduced by nearly 60% with administration of 6 months course of isoniazid preventive therapy (IPT). However, uptake of IPT by national TB programs is low, and IPT delivery is a challenge in many resource-limited high TB-burden settings. Routinely collected program data was analyzed to determine the coverage and outcome of implementation of IPT for eligible under-five year old children in 28 health facilities in two regions of Ethiopia. A total of 504 index smear-positive pulmonary TB (SS+) cases were reported between October 2013 and June 2014 in the 28 health facilities. There were 282 under-five children registered as household contacts of these SS+ TB index cases, accounting for 17.9% of all household contacts. Of these, 237 (84%) were screened for TB symptoms, and presumptive TB was identified in 16 (6.8%) children. TB was confirmed in 5 children, producing an overall yield of 2.11% (95% confidence interval, 0.76–4.08%). Of 221 children eligible for IPT, 64.3% (142) received IPT, 80.3% (114) of whom successfully completed six months of therapy. No child developed active TB while on IPT. Contact screening is a good entry point for delivery of IPT to at risk children and should be routine practice as recommended by the WHO despite the implementation challenges.

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“…al., reported several piperazine based active antitubercular agents of which 4-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1-(2H)-yl)ethyl)-N-(4-nitrophenyl)piperazine-1-carboxamide 21 and N-(4-chlorophenyl)-4-(6-nitro-4-oxo-4H-benzo[e] [1,3]thiazin-2-yl)piperazine-1-carbothioamide 18 were the most active compounds with IC 50 0.29 mM and 0.51 mM in the DNA supercoiling assay and MTB MIC 3.45 mM and 4.41 mM respectively. 21,22 In our previous work, we linked a piperazine moiety to the pyridine nucleus of phenanthridine and these compounds were shown to exhibit good to excellent anti-TB activity with MICs ranging from 1.56 mg mL À1 to 50 mg mL À1 . Compounds 6-(4-((1-(phenylsulfonyl)-1H-1,2,3-triazol-4-yl) methyl)piperazin-1-yl)phenanthridine (G) and 6-(4-(pyridin-2yl)piperazin-1-yl)phenanthridine (H) were the most active compounds with MTB MIC 1.56 mg mL À1 against H37Rv.…”

Section: Introductionmentioning

confidence: 99%

Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents

et al. 2020

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Benzothiazinone-piperazine derivatives as efficient Mycobacterium tuberculosis DNA gyrase inhibitors

Cited by 28 publications

References 15 publications

Adherence to Isoniazid Preventive Therapy among Under-Five Children in Contact with Adult Bacteriologically Confirmed Pulmonary Tuberculosis Patients: A Mixed-Method Study

Adherence to Isoniazid Preventive Therapy among Under-Five Children in Contact with Adult Bacteriologically Confirmed Pulmonary Tuberculosis Patients: A Mixed-Method Study

Uptake of Isoniazid Preventive Therapy among Under-Five Children: TB Contact Investigation as an Entry Point

Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents

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