Current insights into the chemistry and antitubercular potential of benzimidazole and imidazole derivatives

2020 ◽  
Vol 20 ◽  
Author(s):  
Deepa Parwani ◽  
Sushanta Bhattacharya ◽  
Akash Rathore ◽  
Chaitali Mallick ◽  
Vivek Asati ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Multi Drug Resistance ◽  
Benzimidazole Derivatives ◽  
Duration Of Treatment ◽  
Structure Activity ◽  
Mdr Tb ◽  
Low Toxicity ◽  
Extensively Drug Resistance ◽  
Improved Characteristics

: Tuberculosis is a disease caused by Mycobacterium tuberculosis (Mtb), affecting millions of people worldwide. The emergence of drug resistance is a major problem in the successful treatment of tuberculosis. Due to the commencement of MDR-TB (multi-drug resistance) and XDR-TB (extensively drug resistance), there is a crucial need for the development of novel anti-tubercular agents with improved characteristics such as low toxicity, enhanced inhibitory activity and short duration of treatment. In this direction, various heterocyclic compounds have been synthesized and screened against Mycobacterium tuberculosis. Among them, benzimidazole and imidazole containing derivatives found to have potential anti-tubercular activity. The present review focuses on various imidazole and benzimidazole derivatives (from 2015-2019) with their structure activity relationships in the treatment of tuberculosis.

Anti-mycobacterial activity of 22 Iranian endemic or rare plant extracts against multi-drug and extensively drug resistant Mycobacterium tuberculosis

2021 ◽  
Vol 24 ◽  
Author(s):  
Sina Dehestani ◽  
Javid Davoodi ◽  
Seyed Ahmad Emami ◽  
Fereshteh Sadat Seddighinia ◽  
Amirhossein Sahebkar ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Ethyl Acetate ◽  
Plant Extracts ◽  
Inhibitory Effect ◽  
Multi Drug Resistance ◽  
Rare Plant ◽  
Plant Metabolites ◽  
Linum Album ◽  
Mdr Tb

Background: Due to side-effects and lost efficacy of common drugs on new resistance strains of Mycobacterium tuberculosis (Mtb), investigation on novel drugs and natural compounds from rich source of endemic plants is required. Thus, in the present study, the anti-mycobacterial effect of 22 Iranian endemic or rare plant extracts on multi-drug resistance (MDR) and extensively-drug resistance (XDR) Mtb isolates was evaluated. Methods: 22 Iranian endemic and rare plant species from 9 families were collected and extracted by methanol. Their inhibitory-effects were then evaluated against Mtb H37Rv strain, seven clinical MDR-TB and two XDR-TB isolates using resazurin microtiter assay (REMA) method. Best of them were then fractionalized by five different polar solvents (Petroleum-Ether, Dichloromethane, Ethyl-Acetate, n-butanol and water). To find anti-mycobacterial fractions, inhibitory effect of isolated fractions were tested on Mtb H37Rv. Results: Out of the 22 plants, 14 plant extracts demonstrated anti-mycobacterial activity with minimum inhibitory concentration (MIC) ranging from 4 to 30µg/mL against Mtb H37Rv. Eight plant extracts also exhibited anti-mycobacterial activity against MDR and XDR clinical strains of Mtb by MICs, 15-60μg/ml. Crinitaria grimmii and Linum album were the best anti-mycobacterial plants. Among fractions of Crinitaria grimmii, dichloromethane and n-butanol and for Linum album, dichloromethane and Ethyl-Acetate fractions displayed more anti-mycobacterial effect comparing to crude extract on Mtb. Conclusion: The present study confirms the potential role of some plants to treat respiratory diseases as our results have demonstrated that these plants exhibit anti-mycobacterial activity in the acceptable range against Mtb. Thus, these plants could be good sources and alternatives of plant metabolites for anti-TB-drug development.

scholarly journals Molecular Detection of Drug-Resistant Mycobacterium tuberculosis in Sputum Specimens from the New and Previously Treated Tuberculosis Cases at the National Reference Chest Diseases Laboratory in Lusaka, Zambia

2021 ◽  
Vol 2 (4) ◽  
pp. 232-243
Author(s):  
DK Mumena ◽  
G Kwenda ◽  
CW Ngugi ◽  
AK Nyerere
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Polymerase Chain Reaction Amplification ◽  
Multi Drug Resistance ◽  
Drug Resistant ◽  
Health Issues ◽  
Resistant Tuberculosis ◽  
Mdr Tb ◽  
Reaction Amplification ◽  
Previously Treated

Background: Drug-Resistant Tuberculosis (DR-TB) is one of the major public health issues globally. Zambia is highly burdened by TB and multi-drug resistant TB. In this study, sputum samples obtained from the new and previously treated cases of TB were examined for drug-resistant Mycobacterium tuberculosis (MTB). Methods: Sputum specimens were processed using the N-acetyl-L-cysteine-sodium hydroxide method, stained and examined using fluorescent technique and microscopy respectively. Mycobacterial DNA was extracted using the Genolyse kit, then subjected to multiplex polymerase chain reaction amplification and reverse hybridization. Drug-resistance and mutations in MTB genes were detected using the Genotype MTBDRplus VER 2.0 and MTBDRsl VER 2.0 assays. Results: A total of 329 MTB-positive sputum specimens, 102 from the new TB cases and 227 from previously treated TB cases, were analysed for drug-resistance. Among the new TB cases, 3.9% had Rifampicin (RIF) mono-resistance, 12.8% Isoniazid (INH) mono-resistance, and 17.7% had Multi-Drug Resistance (MDR). For the previously treated TB cases, 10.1% had RIF mono-resistance, 6.6% INH mono-resistance, 33.0% MDR, 1.8% poly-drug resistance, and 0.8% had pre-Extensively Drug-Resistance (pre-XDR). Mutations identified were rpoB (Ser531Leu, His526Asp, Asp516Val, His526Tyr, and Glu510His), katG (Ser315Thr 1 and Ser315Thr 2), InhA (Cys15Thr), gyrA (Ala90Val and Asp94Gly), and eis (Cys14Thr), each with a varying frequency. Conclusion: DR-TB is prevalent, especially MDR-TB, which is currently the most worrisome form of DR-TB and an emerging threat hampering efforts in the control of TB in Zambia. The early detection and effective treatment of TB cases are key in the control of DR-TB.

scholarly journals A study on multi drug resistant tuberculosis at Sree Mookambika Institute of Medical Sciences

2017 ◽  
Vol 4 (9) ◽  
pp. 3234
Author(s):  
Prashant V. Solanke ◽  
Preeti Pawde ◽  
Ajin R. M.
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Sputum Culture ◽  
Multi Drug Resistance ◽  
Drug Resistant ◽  
Medical Sciences ◽  
Drug Resistant Tuberculosis ◽  
Resistant Tuberculosis ◽  
Multi Drug Resistant Tuberculosis ◽  
Mdr Tb

Background: Tuberculosis (TB) is one of the major causes of morbidity and mortality worldwide. Resistance to antitubercular drugs has been noted since the drugs were first introduced, and occasionally outbreaks of drug-resistant tuberculosis have been reported worldwide. WHO emphasizes that good TB control prevents the emergence of drug resistance in the first place and that the proper treatment of multi-drug resistant tuberculosis prevents the emergence of XDR-TB. The objectives of the study were to examine the sputum samples regarding MDR-TB, to study the grading regarding sputum positive and to study the multi-drug resistance tuberculosis in Sree Mookambika Institute of Medical sciences.Methods: Study design was cross-sectional, Study duration was January 2016-March 2017. Study place was Sree Mookambika Institute of Medical Sciences Hospital, Kulasekharam. Sample size was 400. Data entered in MS-Office Word- 2016. Institutional ethical committee clearance was obtained. Results: In present study 54.86% patient had sputum AFB positive, 45.13% had sputum AFB negative smears. 75% of the sputum AFB positive pulmonary TB came under the age group between 20-60 and 25% above 60 yrs. 78.24% males, 21.75% females had sputum AFB smear positive pulmonary tuberculosis and 43.73% patients had positive sputum culture, 56.26% patients had negative sputum culture and the most common strain found was Mycobacterium tuberculosis. Conclusions: So from our study we found that Mycobacterium tuberculosis is the major strain isolated from sputum samples. The resistance is more to Isoniazid and Rifampicin and is more in the rural parts of India. Early screening and drug susceptibility test of culture positive and MTB cases will help in initiating treatment of MDR-TB. 

scholarly journals Determination of drug resistance of Mycobacterium tuberculosis in the operating material

2021 ◽  
Vol 69 (1) ◽  
Author(s):  
Maria Uraksina ◽  
◽  
Petr Rogozhkin ◽  
Ekaterina Eremenko ◽  
◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Drug Sensitivity ◽  
Molecular Genetic ◽  
Multi Drug Resistance ◽  
Sensitivity Testing ◽  
Number Of Patients ◽  
Primary Drug Resistance ◽  
Extensively Drug Resistance

Currently, with the improvement of epidemic indicators for tuberculosis, the number of patients with drug-resistant forms of tuberculosis is increasing, which complicates and prolongs the treatment of such patients. The aim of the work is to study the drug resistance of Mycobacterium tuberculosis obtained from surgical material. Materials and methods: the study included 74 patients with medical and diagnostic operations on the chest organs. All patients were examined by standard methods: sputum and BAL microscopy with bronchoscopy (during the procedure), molecular genetic methods, culture on dense and liquid nutrient media. The diagnosis of tuberculosis was confirmed morphologically in all patients by histological examination of surgical material. When analyzing the results of drug resistance, it was found that among the newly identified patients, more than half (59.3%) had multiple (44.6%) p<0.005 and extensively drug resistance (14.7%) p= 0.003. At the same time, 74.5% (n= 35/47) of patients had no MBT in sputum before surgery. The frequency of development of drug resistance to first-and reserve-line antibacterial drugs, the structure of drug resistance depending on the group of dispensary registration is presented. A comparative analysis of drug sensitivity testing of MBT isolated from sputum before surgery and from surgical material was performed. The results of the study showed a high percentage of MBT drug resistance obtained in the operating material in patients with negative MBT tests. More than half of the patients who did not receive antibacterial therapy before surgery have multi drug resistance and extensively drug resistance, which suggests a high regional primary drug resistance of Mycobacterium tuberculosis.

Recent Development of Sulfonyl or Sulfonamide Hybrids as Potential Anticancer Agents: A Key Review

2018 ◽  
Vol 18 (4) ◽  
pp. 488-505 ◽  
Author(s):  
K. P. Rakesh ◽  
Shi-Meng Wang ◽  
Jing Leng ◽  
L. Ravindar ◽  
Abdullah M. Asiri ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Anticancer Agents ◽  
Side Effect ◽  
Docking Studies ◽  
Multi Drug Resistance ◽  
Anticancer Activities ◽  
Pharmacological Activities ◽  
Synthetic Compounds ◽  
Structure Activity ◽  
Anticancer Drug Discovery

Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, a large number of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Sulfonyl or sulfonamide hybrids became one of the most attractive subjects due to their broad spectrum of pharmacological activities. Sulfonyl hybrids were broadly explored for their anticancer activities and it was found that they possess minimum side effect along with multi-drug resistance activity. This review describes the most recent applications of sulfonyl hybrid analogues in anticancer drug discovery and further discusses the mechanistic insights, structure-activity relationships and molecular docking studies for the potent derivatives.

scholarly journals Analysis of drug resistance and mutation profiles in Mycobacterium tuberculosis isolates in a surveillance site in Beijing, China

2021 ◽  
Vol 49 (1) ◽  
pp. 030006052098493
Author(s):  
Jie Zhang ◽  
Yixuan Ren ◽  
Liping Pan ◽  
Junli Yi ◽  
Tong Guan ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Drug Testing ◽  
Multidrug Resistant ◽  
High Rate ◽  
Drug Resistant ◽  
Surveillance Site ◽  
Mdr Tb ◽  
Previously Treated Patients ◽  
Beijing China

Objective This study analyzed drug resistance and mutations profiles in Mycobacterium tuberculosis isolates in a surveillance site in Huairou District, Beijing, China. Methods The proportion method was used to assess drug resistance profiles for four first-line and seven second-line anti-tuberculosis (TB) drugs. Molecular line probe assays were used for the rapid detection of resistance to rifampicin (RIF) and isoniazid (INH). Results Among 235 strains of M. tuberculosis, 79 (33.6%) isolates were resistant to one or more drugs. The isolates included 18 monoresistant (7.7%), 19 polyresistant (8.1%), 28 RIF-resistant (11.9%), 24 multidrug-resistant (MDR) (10.2%), 7 pre-extensively drug-resistant (XDR, 3.0%), and 2 XDR strains (0.9%). A higher rate of MDR-TB was detected among previously treated patients than among patients with newly diagnosed TB (34.5% vs. 6.8%). The majority (62.5%) of RIF-resistant isolates exhibited a mutation at S531L in the DNA-dependent RNA polymerase gene. Meanwhile, 62.9% of INH-resistant isolates carried a mutation at S315T1 in the katG gene. Conclusion Our results confirmed the high rate of drug-resistant TB, especially MDR-TB, in Huairou District, Beijing, China. Therefore, detailed drug testing is crucial in the evaluation of MDR-TB treatment.

scholarly journals Increasing prevalence of resistance to second-line drugs among multidrug-resistant Mycobacterium tuberculosis isolates in Kuwait

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Noura M. Al-Mutairi ◽  
Suhail Ahmad ◽  
Eiman Mokaddas
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Mutation Detection ◽  
Susceptibility Testing ◽  
Multidrug Resistant ◽  
Genetic Mutations ◽  
Second Line ◽  
Injectable Drugs ◽  
Mdr Tb ◽  
Phenotypic Susceptibility

AbstractMolecular methods detect genetic mutations associated with drug resistance. This study detected resistance-conferring mutations in gyrA/gyrB for fluoroquinolones and rrs/eis genes for second-line injectable drugs (SLIDs) among multidrug-resistant Mycobacterium tuberculosis (MDR-TB) isolates in Kuwait. Fifty pansusceptible M. tuberculosis and 102 MDR-TB strains were tested. Phenotypic susceptibility testing was performed by MGIT 960 system using SIRE drug kit. GenoType MTBDRsl version 1 (gMTBDRslv1) and GenoType MTBDRsl version 2 (gMTBDRslv2) tests were used for mutation detection. Results were validated by PCR-sequencing of respective genes. Fingerprinting was performed by spoligotyping. No mutations were detected in pansusceptible isolates. gMTBDRslv1 detected gyrA mutations in 12 and rrs mutations in 8 MDR-TB isolates. gMTBDRsl2 additionally detected gyrB mutations in 2 and eis mutation in 1 isolate. Mutations in both gyrA/gyrB and rrs/eis were not detected. gMTBDRslv1 also detected ethambutol resistance-conferring embB mutations in 59 isolates. Although XDR-TB was not detected, frequency of resistance-conferring mutations for fluoroquinolones or SLIDs was significantly higher among isolates collected during 2013–2019 versus 2006–2012. Application of both tests is warranted for proper management of MDR-TB patients in Kuwait as gMTBDRslv2 detected resistance to fluoroquinolones and/or SLIDs in 3 additional isolates while gMTBDRslv1 additionally detected resistance to ethambutol in 58% of MDR-TB isolates.

scholarly journals Prevalence and Determinant of Depression among Multi-Drug Resistance Tuberculosis: Study in Dr. Kariadi General Hospital

2020 ◽  
Vol 40 (2) ◽  
pp. 88-96
Author(s):  
Mahalul Azam ◽  
Arulita Ika Fibriana ◽  
Fitri Indrawati ◽  
Indah Septiani
Keyword(s):  
Drug Resistance ◽  
General Hospital ◽  
Secondary Data ◽  
Cross Sectional Study ◽  
Multi Drug Resistance ◽  
P Value ◽  
Cross Sectional ◽  
Depression Status ◽  
Prevalence Of Depression ◽  
Mdr Tb

Backgrouds: Multi-drug resistance tuberculosis (MDR-TB) adds the burden of tuberculosis (TB). Depression is a common comorbidity in TB patients. Prevalence of depression among MDR-TB patients was higher, i.e. 11-70%. Prevalence of depression among TB patients in Dr. Kariadi General Hospital was 51.9%. Previous study reported the determinants related to the depression in MDR-TB patients. This study explored the prevalence of depression in MDR-TB patients and its determinants. Methods: This study was a cross-sectional study conducted from July-August 2019. Data consisted of primary and secondary data from Dr. Kariadi General Hospital patients. Sample in this study involved 72 respondents, over 16 years old from 151 registered MDR-TB patients. Depression status was determined using Depression Anxiety Stress Scales obtained from the medical record. Subjects’ characteristics and determinants were collected from primary as well as secondary data. Descriptive data were presented in proportion. Chi-square test continued by Binary logistic regression was performed to determine the association between depression status and its determinants. A P-value

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