• Bulletin of the Korean Chemical Society
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• 제32권8호
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• pp.2657-2660
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• 2011

1,2,4-Triazoles and quinoxalines were found to display various pharmacological activities. Hence a series of 1-aryl-4-methyl-1,2,4-triazolo[4,3-a]quinoxalines were synthesized. Due to various advantages of organic reactions under solvent-free conditions these compounds were developed using iodobenzene diacetate under solvent-free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, $^{13}C$ NMR and HRMS. All the synthesized compounds were investigated for their antitubercular activity and 5g was found to the most active compound.

• Clinical and Experimental Pediatrics
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• 제52권6호
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• pp.717-720
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• 2009

결핵 환자들에서 역설적반응이란 항결핵제 치료 중 초기에 병변의 호전 이후 방사선학적, 임상적으로 이전의 병변이 악화되거나 새로운 병변이 발생하는 경우로 정의될 수 있다. 전세계적으로 지금까지 다양한 종류의 역설적 반응이 보고되어 왔다. 그러나 국내 소아에서의 보고는 거의 드물다. 이에 저자들은 17세 남아에서 결핵성 흉막삼출로 진단되어 결핵약물에 좋은 반응을 보여 적절한 치료 후 흉수가 호전된 후에, 첫 치료 3주 후에 새로이 발생한 폐병변이 기존의 항결핵제를 계속하면서 결국에는 호전된 케이스를 경험하였기에 보고하는 바이다.

• 약학회지
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• 제15권3_4호
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• pp.83-86
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• 1971

Nine novel compounds, namely, 2-(p-aminobenzenesulfonamideo)-6-sulfamylbenzothiozle, 2-benzamido-6-sulfamylbenzothiazole, 2-(p-toluenesulfonamide)-6-sulfamylbenzothiazole, 2-(3,5-dinitrobenzamido)-6-sulfamylbenzothiazole, 2-benzamido-6-nitrobenzothiazole, 2-(p-toluene-sulfonamido)-6-nitrobenzothiazole, 2-(3,5-dinitrobenzamido)-6-nitrobenzothiazole, 2-(p-toluenesulfonamido)-6-chlorobenzothiazole, 2-(3,5-dinitrobenzamido)-6-chlorobenzothiazole were synthesized and evaluated for their in vitro antimicrobial activity against Staphylococcus aureus wood 46, $\betha$-Streptococcus S86, Escherichia coli and antitubercular activity against Mycobacterium tuberculosis H$_{37}$ /Rv. 2-(p-Toluenesulfonamido)-6-chlorobenzothiazole showed antimicrobial activity at 25 $\mu$g/ml against $\betha$-Streptococcus S/86, 2-(3,5-Dinitrobenzamido)-6-sulfamylbenzothiazole was active at 5 $\mu$g/ml and 2-(3,5-dinitrobenzamido)-6-nitrobenzothiazole was consderably active at 1$\mu$g/ml against Mycobacterium tuberculosis H$_{37}$Rv.

• 약학회지
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• 제10권2_3호
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• pp.8-11
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• 1966

항인결핵균성및 streptomycin, isoniazid및 para-aminosalicylic acid에 대한 내성인결핵균주에 현저한 항균작용 있는 dextro-2,2'-(ethylenediimino)-di-1- butanol(Ethambutol) 계열 및 thioureido(-NHCSNH-) 함유화 합물 계열인 2,2'-(ethylenediimino)-di-1-butyric acid및 2,2'-(thioureido)-di-1-butyric acid를 합성했으며 이들 약물의 구조와 작용간의 상호관계를 설명코저 이들 화합물과 류사한 구조인 2,2'-(thioureido)-di-acetic acid를 합성했기에 보고함.

• 약학회지
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• 제15권3_4호
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• pp.93-97
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• 1971

Seventeen novel compounds of thiosemicarbazone derivatives were synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H$_{37}$Rv and antibacterial activity against Staphylococcus aureus, Escherichia coli. It was found that 4-($\alpha$-naphthyl)-1-(2-furfuraldehyde)-3-thiosemicarbazone was active at 0.01$\mu$g/ml and 1, 1'-(p-phenylene)-4, 4'-bis(phenyl)-2, 2'-dithiosemicarbazide, at 0.01$\mu$g/ml against E. coli, respectively.

• 약학회지
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• 제15권3_4호
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• pp.87-92
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• 1971

Fourteen novel N,N'-disubstitued thiourea derivatives were synthesized by Hugershof reaction. Antitubercular activities of ten compounds against Mycobacterium tuberculosis H$_{37}$ Rv were tested and was found tat 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was considerably active at 1mg/ml and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea was slightly active at 1mg/ml. Antibacterial activity of the newly synthesized compounds against E. coli, Sta. aureus and Streptococcus hemolyticus were also tested. 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was makedly active against E. coli, Sta, aureus and Streptococcus hemolyticus; Phenol coefficients against E. coli, Sta, aureus and Streptococcus hemolyticus were 30,17.5 and 21.3, respectively. 1,1'-p-phenylene-3,3'bis[N-(2-thiazolyl)-sulfamylphenyl]-2,2'-dithiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were considerably active against E. coli: phenol coefficients, 18.8 and 37.5 respectively. 1-(4-ethoxyphenyl)3-(4-sulfamylphenyl)-2-thiourea was active against Streptococcus hemolyticus: phenol coefficients, 22.5. 1-$\alpha$-naphthyl-3-(4-sulfamylphenyl)-2-thiourea, 1-$\betha$-naphthyl-3-[4-N-(2-thiazolyl)-sulfamylphenyl]-2-thiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were active against Sta. aureus: phenol coefficients, 17.5, 20.0 and 18.8 respectively.

• Tuberculosis and Respiratory Diseases
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• 제72권6호
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• pp.475-480
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• 2012

Background: Pyrazinamide (PZA) is an effective antitubercular drug that becomes toxic to Mycobacterium tuberculosis when converted to pyrazinoic acid by pyrazinamidase (PZase), encoded by mycobacterial pncA. A strong association was noted between the loss of PZase activity and PZA resistance. The causative organisms in extrapulmonary tuberculosis are rarely cultured and isolated. To detect pncA mutations in specimens from extrapulmonary tuberculosis as confirmative diagnosis of mycobacterial infection and alternative susceptibility test to PZA. Methods: Specimens were collected from clinically proven extrapulmonary tuberculosis. pncA was sequenced and compared with wild-type pncA. Results: pncA from 30 specimens from 23 donors were successfully amplified (56.6% in specimens, 59% in donors). Six mutations in pncA were detected (20.0% in amplified specimens, 26.1% in specimen donors) at nucleotide positions of 169, 248 and 419. The mutation at position 169 results in substitution of aspartic acid for histidine, a possible allelic variation of M. bovis that have intrinsic PZA resistance. The mutation at position 248 changes proline into arginine and that at position 419, arginine into histidine. Conclusion: DNA-based diagnosis using pncA may be simultaneously useful for the early diagnosis of mycobacterial infection and the rapid susceptibility to PZA in extrapulmonary tuberculosis. A potential implication of pncA allelic variation at 169 might be suggested as a rapid diagnostic test for M. bovis infection or Bacille Calmette-Gu$\acute{e}$rin (BCG) reactivation.

• Tuberculosis and Respiratory Diseases
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• 제78권3호
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• pp.161-167
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• 2015

Tuberculosis (TB) remains a major global health problem, and the incidence of TB cases has not significantly decreased over the past decade in Korea. The standard short course regimen is highly effective against TB, but requires multiple TB-specific drugs and a long treatment duration. Recent studies using late-generation fluoroquinolones and/or high-dose rifapentine-containing regimens to shorten the duration of TB treatment showed negative results. Extending the treatment duration may be considered in patients with cavitation on the initial chest radiograph and positivity in sputum culture at 2 months of treatment for preventing TB relapse. Current evidence does not support the use of fixed-dose combinations compared to separate drugs for the purpose of improving treatment outcomes. All patients receiving TB treatment should be monitored regularly for response to therapy, facilitation of treatment completion, and management of adverse drug reactions. Mild adverse effects can be managed with symptomatic therapy and changing the timing of the drug administration, but severe adverse effects require a discontinuation of the offending drugs.

• Tuberculosis and Respiratory Diseases
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• 제77권4호
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• pp.161-166
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• 2014

Since tuberculosis (TB) remains a major global health concern and the incidence of multi-drug resistant (MDR)-TB is increasing globally, new modalities for the detection of TB and drug resistant TB are needed to improve TB control. The Xpert MTB/RIF test can be a valuable new tool for early detection of TB and rifampicin resistance, with a high sensitivity and specificity. Late-generation fluoroquinolones, levofloxacin, and moxifloxacin, which are the principal drugs for the treatment of MDR-TB, show equally high efficacy and safety. Systemic steroids may reduce the overall TB mortality attributable to all forms of TB across all organ systems, although inhaled corticosteroids can increase the risk of TB development. Although fixed dose combinations were expected to reduce the risk of drug resistance and increase drug compliance, a recent meta-analysis found that they might actually increase the risk of relapse and treatment failure. Regarding treatment duration, patients with cavitation and culture positivity at 2 months of TB treatment may require more than 6 months of standard treatment. New anti-TB drugs, such as linezolid, bedaquiline, and delamanid, could improve the outcomes in drug-resistant TB. Nontuberculous mycobacterial lung disease has typical clinical and immunological phenotypes. Mycobacterial genotyping may predict disease progression, and whole genome sequencing may reveal the transmission of Mycobacterium abscessus. In refractory Mycobacterium avium complex lung disease, a moxifloxacin-containing regimen was expected to improve the treatment outcome.

• Journal of Preventive Medicine and Public Health
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• 제52권1호
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• pp.66-70
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• 2019

Objectives: In the Republic of Korea (ROK), the notified incidence of tuberculosis in foreign-born individuals (NITFBI) has increased recently, as has the rate of multidrug-resistant (MDR) and rifampicin-resistant (RR) tuberculosis in foreigners staying in the ROK. As Jeju Province in ROK has a no-visa entry policy, control programs for NITFBI should be consolidated. The aim was to evaluate the status of NITFBI, with a focus on the distribution of MDR/RR tuberculosis by nationality. Methods: Data on tuberculosis incidence in individuals born in Jeju Province and in foreign-born individuals were extracted from the Korean Statistical Information Service of Statistics Korea, and the Infectious Disease Surveillance Web Statistics of the Korea Centers for Disease Control and Prevention, respectively. Results: Among all notified incident cases of tuberculosis, the proportion of NITFBI increased from 1.46% in 2011 to 6.84% in 2017. China- and Vietnam-born individuals accounted for the greatest proportion of the 95 cases of NITFBI. Seven cases of MDR/RR tuberculosis were found, all involving patients born in China. Conclusions: In Jeju Province, ROK, NITFBI might become more common in the near future. Countermeasures for controlling active tuberculosis in immigrants born in high-risk nations for tuberculosis should be prepared in Jeju Province, since it is a popular tourist destination.