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Journal articles on the topic 'Antitubercular activity'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

HUSAIN, Asif, Aftab AHMAD, Anil BHANDARI, and Veerma RAM. "ANTITUBERCULAR ACTIVITY OF SOME NEWER 6-PYRIDAZINONE DERIVATIVES." SOUTHERN BRAZILIAN JOURNAL OF CHEMISTRY 19, no. 19 (2011): 17–23. http://dx.doi.org/10.48141/sbjchem.v19.n19.2011.22_2011.pdf.

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Two series of 6-pyridazinone derivatives (17-30) were synthesized and evaluated for antitubercular activities against the Mycobacterium tuberculosis H37Rv strain. The results indicated that among the synthesized compounds, 5-( 4-hydroxy-3-methoxybenzyl}-3-phenyl-1,6-dihydro-6-pyridazinone (23) showed good antitubercular activity. Three more compounds, (18, 25 & 27) were significant in their antitubercular action. The present study reveals the antitubercular potential of 6-pyridazinones.

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2

Wächter, Gerald A., Susanne Valcic, Scott G. Franzblau, Enrique Suarez, and Barbara N. Timmermann. "Antitubercular Activity of Triterpenoids fromLippiaturbinata." Journal of Natural Products 64, no. 1 (2001): 37–41. http://dx.doi.org/10.1021/np000267b.

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3

Cardoso, Silvia H., Milena B. Barreto, Maria C. S. Lourenço, et al. "Antitubercular Activity of New Coumarins." Chemical Biology & Drug Design 77, no. 6 (2011): 489–93. http://dx.doi.org/10.1111/j.1747-0285.2011.01120.x.

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4

Kuneš, Jiřı́, Jaroslav Bažant, Milan Pour, Karel Waisser, Milan Šlosárek, and Jiřı́ Janota. "Quinazoline derivatives with antitubercular activity." Il Farmaco 55, no. 11-12 (2000): 725–29. http://dx.doi.org/10.1016/s0014-827x(00)00100-2.

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5

Gu, Jian-Qiao, Yuehong Wang, Scott G. Franzblau, Gloria Montenegro, and Barbara N. Timmermann. "Constituents ofSeneciochionophiluswith Potential Antitubercular Activity." Journal of Natural Products 67, no. 9 (2004): 1483–87. http://dx.doi.org/10.1021/np049831z.

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6

Tonelli, Michele, Federica Novelli, Bruno Tasso, et al. "Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines." Bioorganic & Medicinal Chemistry 22, no. 24 (2014): 6837–45. http://dx.doi.org/10.1016/j.bmc.2014.10.035.

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7

K, Ishwar Bhat, and Abhishek Kumar. "PYRAZOLINES AS POTENT ANTITUBERCULAR AND CYTOTOXIC AGENTS." Asian Journal of Pharmaceutical and Clinical Research 10, no. 6 (2017): 247. http://dx.doi.org/10.22159/ajpcr.2017.v10i6.17344.

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Objective: Pyrazolines are known to exhibit different biological and pharmacological properties such as anticancer, antibacterial, antifungal and antitubercular activities. Chalcones with an enone group between two aromatic rings exhibit remarkable pharmacological activities such as antiinflammatory, antibacterial, antitumor, antifungal, and antimalarial activity. A series of pyrazolines from chalcones have been synthesized and evaluated for antitubercular and cytotoxic activity studies.Methods: Chalcones [3-substituted phenyl-1-(p-tolyl)prop-2-en-1-one] were synthesized from various substitut

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8

Jadhav, S. G., and S. R. Pattan. "SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF NOVEL BENZIMIDAZOLE DERIVATIVES." INDIAN DRUGS 49, no. 06 (2012): 12–17. http://dx.doi.org/10.53879/id.49.06.p0012.

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A new series of substituted benzimidazole derivatives were synthesized by N-Mannich base reaction and the structures of these compounds have been established on the basis of spectral analysis. All the compounds have been screened for antitubercular activities. Some of these compounds have shown promising antitubercular activity.

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9

Anjani, Solankee, and Tailor Riki. "An efficient synthesis of some new chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5- triazine nucleus as potential antimicrobial and antitubercular agent." Chemistry International 2, no. 4 (2016): 189–200. https://doi.org/10.5281/zenodo.1471239.

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In an attempt to find a new class of antimicrobial and antitubercular agent, a new series of chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5- triazine nucleus were synthesized with appropriate chemical reagent. Chalcones (D1-D5) were synthesized by the classical Claisen-Schmidt condensation of substituted ketone (C) with variously substituted aldehydes via conventional method. Now treatment of chalcones with hydrazine hydrate/glacial acetic acid and guanidine hydrochloride/Alkali afforded the corresponding acetyl pyrazoline (E1-E5) and amino pyrimidine (F1-F5) derivatives respec

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10

Philip, Ifesinachi Anochie. "African Medicinal Plants that Can Control or Cure Tuberculosis." Int J Pharm Sci Dev Res 4, no. 1 (2018): 001–8. https://doi.org/10.17352/ijpsdr.000016.

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This review contains a compendium of medicinal plants in Africa that can control or cure tuberculosis. A good number of plant secondary metabolites are reported to have antitubercular activity comparable to the existing antitubercular drugs or sometimes even better. Information regarding the chemistry and pharmacology of plants leads to insight into their structure–activity relationship and potency. A well-defined strategy is required to exploit these phytomolecules as antitubercular drugs.

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11

A., N. SOLANKEE, M. KAPADIA K., and M. TUREL J. "Synthesis and Antitubercular Activity of 4-Thiazolidinones." Journal of Indian Chemical Society Vol. 72, Oct 1995 (1995): 739–40. https://doi.org/10.5281/zenodo.5909279.

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Chemistry Department, B. K. M. Science College, Valsad-396 001 <em>Manuscript received 14 August 1992, revised 16 February 1994, accepted 22 February 1994</em> Synthesis and Antitubercular Activity of 4-Thiazolidinones

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12

Yadav, Smriti, Bharath Kumar Inturi, Shrinidhi B.R, Pooja H.J, Neenu Ganesh, and Gurubasavaraj V. Pujar. "Design, Synthesis and Antitubercular Evaluation of New Benzimidazole Scaffolds." Anti-Infective Agents 18, no. 4 (2021): 375–83. http://dx.doi.org/10.2174/2211352518666200108091454.

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Background: To overcome one of the resistance mechanisms of Isoniazid (INH), there is a need for an antitubercular agent that can inhibit InhA enzyme by circumventing the formation of INH-NAD+ adduct. Objective: The objective of the study is the development of novel antitubercular agents that target Mycobacterium tuberculosis InhA (Enoyl Acyl Carrier Protein Reductase). Methods: A small-molecule chemical library was used for the identification of the novel InhA inhibitors using primary screening and molecular docking studies followed by the scaffold hopping approach. The designed molecules, 2-

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13

Ramachandran, S., M. Vijey Aanandhi, and Binoy Varghese Cheriyan. "Assessment of Antitubercular Activity-A Review." Research Journal of Pharmacy and Technology 12, no. 8 (2019): 3973. http://dx.doi.org/10.5958/0974-360x.2019.00684.x.

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14

Kartseva, T. V., O. N. Oleshko, L. I. Lazareva, G. S. Predvoditeleva, V. I. Shvedov, and L. N. Filitis. "Synthesis and antitubercular activity of styrylquinoxalines." Pharmaceutical Chemistry Journal 21, no. 12 (1987): 864–66. http://dx.doi.org/10.1007/bf00757962.

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15

Chandrasekera, N. Susantha, Torey Alling, Mai A. Bailey, et al. "Identification of Phenoxyalkylbenzimidazoles with Antitubercular Activity." Journal of Medicinal Chemistry 58, no. 18 (2015): 7273–85. http://dx.doi.org/10.1021/acs.jmedchem.5b00546.

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16

Narendhar, Bandi, Veerachamy Alagarsamy, and Chitra Krishnan. "Design and Synthesis of Novel 1-substituted-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-yl amino) Isothioureas for their Anti-HIV, Antibacterial Activities, Graph Theoretical Analysis, Insilico Modeling, Prediction of Toxicity and Metabolic Studies." Drug Research 70, no. 08 (2020): 348–55. http://dx.doi.org/10.1055/a-0991-7617.

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AbstractIn the present study, we have placed the substituted thiosemicarbazide moiety at the C-2 position and 3-nitrophenyl group at N-3 position of benzopyrimidines and studied their antitubercular, anti-HIV and antibacterial activities against selected gram positive and negative bacteria. The target compounds 1-substituted-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino) isothioureas (PTS1 – PTS15 ) were obtained by the reaction of 2-hydrazino-3-(3-nitrophenyl) benzopyrimidin-4(3 H)-one (5) with different alkyl/aryl isothiocyanates followed by methylation with dimethyl sulphat

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17

More, Uttam A., Joshi S.D, and V. H. Kulkarni. "Antitubercular Activity of Pyrrole Schiff bases and Computational Study of M. Tuberculosis InhA." International Journal of Drug Design and Discovery 4, no. 4 (2025): 1163–73. https://doi.org/10.37285/ijddd.4.4.1.

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Pursuing our search program for new antitubercular drugs we decided to explore the potentiality of pyrrole moiety by molecular modeling and synthesizing novel pyrrole Schiff bases analogues of phthivazid. Enoyl-acyl carrier protein reductase catalyzes the last rate-limiting step in the elongation cycle of the fatty-acid biosynthesis pathway and has been validated as a potential antitubercular drug target in Mycobacterium tuberculosis. The development of new antitubercular therapies is important both to combat potential drug-resistant bio weapons and to address the broader societal problem of i

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18

Bisht, Surendra Singh, Arya Ajay, Sudhir Kumar Sinha, Vinita Chaturvedi, and Rama P. Tripathi. "Synthesis and Antitubercular Activity of 5-benzyl-3-phenyl dihydroisoxazoles." International Journal of Drug Design and Discovery 1, no. 1 (2010): 11–18. https://doi.org/10.37285/ijddd.1.1.2.

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Hetero Diels-Alder reaction of aromatic aldoximes with different alkenes resulted in highly substituted dihydroisoxazoles (1-12) in good yields. All the compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis H37Ra and H37Rv. Compounds 2, 3, 6, and 10 exhibited antitubercular activity with minimum inhibitory concentration (MIC) ranging from 12.5 to 3.12 g/mL against the infectious strain M. tuberculosis H37Rv.

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19

Teixeira, Cátia, Cristina Ventura, José R. B. Gomes, Paula Gomes, and Filomena Martins. "Cinnamic Derivatives as Antitubercular Agents: Characterization by Quantitative Structure–Activity Relationship Studies." Molecules 25, no. 3 (2020): 456. http://dx.doi.org/10.3390/molecules25030456.

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Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), remains one of the top ten causes of death worldwide and the main cause of mortality from a single infectious agent. The upsurge of multi- and extensively-drug resistant tuberculosis cases calls for an urgent need to develop new and more effective antitubercular drugs. As the cinnamoyl scaffold is a privileged and important pharmacophore in medicinal chemistry, some studies were conducted to find novel cinnamic acid derivatives (CAD) potentially active against tuberculosis. In this context, we have engaged in the setting up of a quantit

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20

A., N. SOLANKEE, M. KAPADIA K., and M.DESAI C. "Synthesis and Antitubercular Activity of 4-Thiazolidinone Derivatives." Journal of Indian Chemical Society Vol. 69, Nov 1992 (1992): 783–84. https://doi.org/10.5281/zenodo.6044231.

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Chemistry Department. B. K. M.<em> </em>Science College. Valsad-396 001 <em>Manuscript received 30 May 1991. revised 22 July 1992, accepted 10 August 1992</em> Synthesis and Antitubercular Activity of 4-Thiazolidinone Derivatives.  

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21

Sellamuthu, Satheeshkumar, Mohammad F. Bhat, Ashok Kumar, Gopal Nath, and Sushil K. Singh. "Design, Synthesis and Biological Evaluation of Carbazole Derivatives as Antitubercular and Antibacterial Agents." Current Bioactive Compounds 15, no. 1 (2019): 83–97. http://dx.doi.org/10.2174/1573407214666180226125501.

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Background:The neuroleptic chlorpromazine has been reported for antitubercular activity but the associated antipsychotic activity restricted its clinical presentation.Objectives:Novel derivatives of carbazole having structural similarity with chlorpromazine were designed, in an attempt to reduce the associated side effects, while retaining the antitubercular activity.Materials and Methods:The designed molecules were synthesized and screened for antitubercular and antibacterial activities. The blood-brain barrier (BBB) permeability and mammalian cell (VERO) cytotoxicity (CC50) were examined to

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22

Neha Krishnarth, Santosh Kumar Verma, and Anurag. "Quinazolinone novel derivatives synthesis and their Biological Evaluation as Antimicrobial and Antitubercular agents." International Journal of Research in Pharmaceutical Sciences 10, no. 4 (2019): 3026–34. http://dx.doi.org/10.26452/ijrps.v10i4.1590.

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At a global level, tuberculosis (TB) is the disease of human values. It suffers from major health, social and economic burden in many countries. There is an inability of an effective vaccine or the use of vaccine were too long and expensive, have increased risk of spread of this disease. A series of quinazolinone derivatives prepared with the help of 2-Amino-3,4,5-trimethoxy benzoic acid and Vilsmeir reagent. Synthesized compounds were characterized by various spectral methods. Different activity like antimicrobial activity of the synthesised compounds were performed, and the most active compo

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23

Jaisamut, Sunan, Suriyan Thengyai, Supreeya Yuenyongsawad, Chatchanok Karalai, Anuchit Plubrukarn, and Khanit Suwanborirux. "Structure-activity relationships of antitubercular scalaranes: Heteronemin revisited." Pure and Applied Chemistry 81, no. 6 (2009): 1019–26. http://dx.doi.org/10.1351/pac-con-08-09-03.

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A series of heteronemin-related antitubercular scalaranes, both from natural products and from chemical derivatization, were subjected to structure-activity investigations. Based on the activity profile, three main regions; i.e., the substituted groups hovering over C-19/C-18 and furan moiety, the functionalities in the vicinity of C-16 and the right-hand side of ring D, and the substituted groups on C-12, were speculated as the areas influencing the antitubercular activity of the scalaranes. The results suggested the promising possibility for the further investigation towards the modes of act

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24

Shaik, Afzal B., Richie R. Bhandare, Srinath Nissankararao, et al. "Design, Facile Synthesis and Characterization of Dichloro Substituted Chalcones and Dihydropyrazole Derivatives for Their Antifungal, Antitubercular and Antiproliferative Activities." Molecules 25, no. 14 (2020): 3188. http://dx.doi.org/10.3390/molecules25143188.

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Infectious diseases caused by fungi and mycobacteria pose an important problem for humankind. Similarly, cancer is one of the leading causes of death globally. Therefore, there is an urgent need for the development of novel agents to combat the deadly problems of cancer, tuberculosis, and also fungal infections. Hence, in the present study, we designed, synthesized, and characterized 30 compounds including 15 chalcones (2–16) and 15 dihydropyrazoles (17–31) containing dichlorophenyl moiety and also screened these compounds for their antifungal, antitubercular, and antiproliferative activities.

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25

Higuchi, C. T., M. Sannomiya, F. R. Pavan, et al. "Byrsonima fagifoliaNiedenzu Apolar Compounds with Antitubercular Activity." Evidence-Based Complementary and Alternative Medicine 2011 (2011): 1–5. http://dx.doi.org/10.1093/ecam/nen077.

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Bioassay-guided fractionation of the chloroform extract ofByrsonima fagifolialeaves led to the isolation of active antitubercular compounds alkane dotriacontane (Minimal Inhibitory Concentration—MIC, 62.5 μg mL−1), triterpenoids as bassic acid (MIC = 2.5 μg mL−1),α-amyrin acetate (MIC = 62.5 μg mL−1), a mixture of lupeol,α- andβ-amyrin (MIC = 31.5 μg mL−1) and a mixture of lupeol, and acetates ofα- andβ-amyrin (MIC = 31.5 μg mL−1). The antimycobacterial activity was determined by the Microplate Alamar Blue Assay (MABA) and the structures of promising compounds were determined by spectroscopic

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26

Gopi, Chandravadivelu, Magharla Dasaratha Dhanaraju, Konatham Pranusha, Thiyagarajan Deepan, AR Magesh, and Dhanaraju Kavitha. "Design, Synthesis, Characterization and Antitubercular Activity of Novel Benzimidazole Mannich Base Derivatives." Asian Journal of Chemistry 36, no. 4 (2024): 969–73. http://dx.doi.org/10.14233/ajchem.2024.31314.

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In present work, the newly synthesized benzimidazole Mannich base derivatives were design, synthesized and evaluated the in silico and in vitro antitubercular activity. These compounds were synthesized by condensation reaction between 1-(1H-benzo[d]imidazol-1-yl)ethanone and aliphatic/aromatic amines. The synthesized compound structures were identified by FTIR, 13C NMR, 1H NMR and mass spectroscopies. The results indicated that these derivatives have significant antitubercular activity against Mycobacterium tuberculosis (M.tb) cell wall enzyme enoyl acyl carrier protein reductase (InhA), EthR

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27

Akula, Ravi K., Shanthan R. Pamulaparthy, Pranay K. Koochana, and Dharmarajan Sriram. "Synthesis and In vitro Antibacterial, Antitubercular Studies of Novel Fluoroquinolones Analogs Containing 4-substituted Sec Amine." Current Bioactive Compounds 15, no. 6 (2020): 656–64. http://dx.doi.org/10.2174/1573407214666180529124816.

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Background: Tuberculosis is a contagious, air borne disease and second leading cause of death among infectious diseases worldwide. Fluoroquinolones are well-known antibacterial agents and they were recommended as second-line of antitubercular drugs. Method: A series of novel fluoroquinolone analogs 6-24 was effectively synthesized. An attempt was made by tagging the substituted pyrazole on to fluoroquinolones for the first time at C-7 position. The newly synthesized compounds were characterized by FTIR, 1HNMR, ESI-MS, HR-MS and elemental analysis. The in vitro antibacterial activity of all the

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28

Sulthana, M. T., K. Chitra, and V. Alagarsamy. "Anti-HIV, Antitubercular and Antibacterial Activities of Novel 3-(Substituted Quinazolinylamino)-2-phenyl quinazolin-4(3H)ones." Asian Journal of Chemistry 32, no. 2 (2019): 281–86. http://dx.doi.org/10.14233/ajchem.2020.22280.

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In the present study, we have synthesized a series of novel 2-phenyl-3-(substituted quinazolinylamino)quinazolin-4(3H)-ones by the reaction of 3-(substituted)-2-hydrazinoquinazoline-4(3H)-ones with 2-phenyl-3,1-benzoxazin-4-one. The starting material 3-(substituted)-2-hydrazinoquinazolin-4(3H)-ones were synthesized from various primary amines. All the synthesized compounds were screened for their antitubercular, anti-HIV and antibacterial activity against different Grampositive and Gram-negative strains by agar dilution method. Among the test compounds, 3-(4-nitrophenyl)-2-(4-oxo-2-phenylquina

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29

Zhang, Gang, Li Sheng, Pooja Hegde, Yan Li, and Courtney C. Aldrich. "8-cyanobenzothiazinone analogs with potent antitubercular activity." Medicinal Chemistry Research 30, no. 2 (2021): 449–58. http://dx.doi.org/10.1007/s00044-020-02676-4.

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30

Nayak, Nishi, Balkishen Razdan, and Meenakshi Bajpai. "Plumbagin analogs-synthesis, characterization, and antitubercular activity." Journal of Advanced Pharmaceutical Technology & Research 5, no. 1 (2014): 28. http://dx.doi.org/10.4103/2231-4040.126984.

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31

Asif, Mohammad. "Antitubercular Activity of Some Substituted Phenothiazine Derivatives." Journal of Pharmaceutical and Applied Chemistry 4, no. 2 (2018): 81–89. http://dx.doi.org/10.18576/jpac/040202.

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32

HUSAIN, ASIF, AFTAB AHMAD, ANIL BHANDARI, and VEERMA RAM. "SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF PYRIDAZINONE DERIVATIVES." Journal of the Chilean Chemical Society 56, no. 3 (2011): 778–80. http://dx.doi.org/10.4067/s0717-97072011000300013.

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33

Higuchi, Celio Takashi, Fernando Rogério Pavan, Clarice Queico Fujimura Leite, et al. "Triterpenes and antitubercular activity of Byrsonima crassa." Química Nova 31, no. 7 (2008): 1719–21. http://dx.doi.org/10.1590/s0100-40422008000700023.

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34

Ratnakar, P., and P. Suryanarayana Murthy. "Antitubercular activity of trifluoperazine, a calmodulin antagonist." FEMS Microbiology Letters 97, no. 1-2 (1992): 73–76. http://dx.doi.org/10.1111/j.1574-6968.1992.tb05442.x.

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35

Akihisa, Toshihiro, Scott G. Franzblau, Motohiko Ukiya, et al. "Antitubercular Activity of Triterpenoids from Asteraceae Flowers." Biological & Pharmaceutical Bulletin 28, no. 1 (2005): 158–60. http://dx.doi.org/10.1248/bpb.28.158.

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36

Isaka, Masahiko, Panida Chinthanom, Malipan Sappan, et al. "Antitubercular Activity of Mycelium-Associated Ganoderma Lanostanoids." Journal of Natural Products 80, no. 5 (2017): 1361–69. http://dx.doi.org/10.1021/acs.jnatprod.6b00973.

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37

Mahapatra, Anita, Vijay Maheswari, Nitin Pal Kalia, Vikrant S. Rajput, and Inshad Ali Khan. "Synthesis and Antitubercular Activity of Berberine Derivatives." Chemistry of Natural Compounds 50, no. 2 (2014): 321–25. http://dx.doi.org/10.1007/s10600-014-0942-8.

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38

Victoria, A., N. Elangovan, T. Gobi, S. Sowrirajan, and T. Kolochi. "Antitubercular activity of some new Azomethine compounds." International Journal of Advanced Research in Biological Sciences (IJARBS) 4, no. 1 (2017): 44–52. http://dx.doi.org/10.22192/ijarbs.2017.04.01.005.

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39

Mativandlela, Sannah Patience Nkami, Jacobus Johannes Marion Meyer, Ahmed A. Hussein, and Namrita Lall. "Antitubercular Activity of Compounds Isolated fromPelargonium sidoides." Pharmaceutical Biology 45, no. 8 (2007): 645–50. http://dx.doi.org/10.1080/13880200701538716.

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40

Aguiar, Inara de, Aline Tavares, Antonio C. Roveda, et al. "Antitubercular activity of Ru (II) isoniazid complexes." European Journal of Pharmaceutical Sciences 70 (April 2015): 45–54. http://dx.doi.org/10.1016/j.ejps.2015.01.008.

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41

Kunes, Jiri, Jaroslav Bazant, Milan Pour, Karel Waisser, Milan Slosarek, and Jiri Janota. "ChemInform Abstract: Quinazoline Derivatives with Antitubercular Activity." ChemInform 32, no. 14 (2001): no. http://dx.doi.org/10.1002/chin.200114173.

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42

VAZZANA, I., F. NOVELLI, F. SPARATORE, A. SPARATORE, G. FADDA, and C. MANCA. "ChemInform Abstract: Quinolizidine Derivatives with Antitubercular Activity." ChemInform 25, no. 35 (2010): no. http://dx.doi.org/10.1002/chin.199435269.

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43

Thorat, B. R., S. N. Mali, Umang Shah, et al. "Hydrazide-Hydrazone Derivatives and Their Antitubercular Activity." Russian Journal of Bioorganic Chemistry 51, no. 1 (2025): 35–52. https://doi.org/10.1134/s1068162025010054.

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44

Triveni, S., C. Naresh Babu, E. Bhargav, and M. Vijaya Jyothi. "in silico Design, ADME Prediction, Molecular Docking, Synthesis of Novel Triazoles, Indazoles & Aminopyridines and in vitro Evaluation of Antitubercular Activity." Asian Journal of Chemistry 32, no. 11 (2020): 2713–21. http://dx.doi.org/10.14233/ajchem.2020.22790.

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To design and synthesize novel triazoles, indazoles and aminopyridines from various (thiophene-2-yl)prop-2-en-1-one derivatives as antitubercular leads by in silico and in vitro methods. in silco Drug design, ADME prediction and molecular docking studies were performed to assess drug likeliness and antitubercular potential of all 30 novel triazoles, indazoles and aminopyridines. in silico Drug design studies revealed that the synthetic routes applied were appropriate according to the calculations of Swiss-ADME that measure synthetic accessibility. Most of the synthesized compounds found to hav

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45

Phanumartwiwath, Anuchit, Chatchai Kesornpun, Sanya Sureram, et al. "Antitubercular and antibacterial activities of isoxazolines derived from natural products: Isoxazolines as inhibitors of Mycobacterium tuberculosis InhA." Journal of Chemical Research 45, no. 11-12 (2021): 1003–15. http://dx.doi.org/10.1177/17475198211047801.

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Isoxazoline derivatives of the natural products eugenol, 1’- S-acetoxychavicol acetate and sclareol are prepared through 1,3-dipolar cycloaddition reactions in an aqueous buffered system. The compounds are evaluated for their antitubercular and antibacterial activities. Compounds 2, 2a and 3f display strong antitubercular activity with minimum inhibitory concentration values of 26.68, 17.89 and 14.58 µM, respectively. Furthermore, derivative 3f exhibits antibacterial activity against Bacillus cereus (minimum inhibitory concentration value of 29.16 µM). Isoxazoline derivatives of 1’- S-acetoxyc

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BASAK, SUSMITA, and K. ISHWAR BHAT. "Design, Synthesis, Evaluation of Antitubercular and Antioxidant Activity of Isoxazoline Derivatives Derived from Novel Chalcone Intermediates." Asian Journal of Chemistry 35, no. 11 (2023): 2782–88. http://dx.doi.org/10.14233/ajchem.2023.30580.

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Tuberculosis (TB), a bacterial infection caused by Mycobacterium tuberculosis (M-TB) is a fatal disease associated with a high degree of mortality. Present work involved synthesis of a series of novel isoxazoline derivatives (ISOA1-ISOA8) the new antitubercular agents using newly synthesized chalcones (CHL1-CHL8). This was done by subjecting the chalcones to a reaction with hydroxylamine hydrochloride in presence of acetic acid and sodium acetate. The structure of the synthesized compounds was elucidated by IR, 1H NMR and mass spectra. In silico studies of isoxazoline were performed for antitu

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Boukthir, Mouna, Zribi Fethi, Iman Halloum, Laurent Kremer, and Fakher Chabchoub. "Synthesis and Antitubercular Evaluation of Some Novel 1,2,3,6-tetrahydropyrimidine-5-carbonitrile." JOURNAL OF ADVANCES IN CHEMISTRY 9, no. 3 (2013): 2072–77. http://dx.doi.org/10.24297/jac.v9i3.1014.

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In an attempt to find a new class of antitubercular agents, a series of 1,2,3,6-tetrahydropyrimidine-5-carbonitrile were prepared via the reaction of ethyl N-ethoxycarbonylbenzimidate 2a-b with cyanoacetanilide derivatives 1a-c. These compounds were screened for their antitubercular activity against M. tuberculosis. Several analogues, such as 2,6-dioxo-1-phenyl-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3a, 1-benzyl-2, 6-dioxo-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3c and 1-benzyl-2, 6-dioxo-4-phenyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3d exhibited a potent an

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Santoso, Mardi, Muhammad Riza Ghulam Fahmi, Yehezkiel Steven Kurniawan, et al. "Isoniazid-Isatin Hydrazone Derivatives: Synthesis, Antitubercular Activity and Molecular Docking Studies." Trends in Sciences 18, no. 21 (2021): 39. http://dx.doi.org/10.48048/tis.2021.39.

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This study examined the synthesis of isoniazid-isatin hydrazone derivatives 5-7, followed by an investigation on the in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv, and molecular docking. A yield of 81 - 92 % of these compounds was achieved, with structural characterization by spectroscopic methods (FTIR, NMR, HRMS). The in vitro antitubercular activity was evaluated against M. tuberculosis H37Rv, and the highest effect was observed in compound 7, with a minimum inhibitory concentration (MIC) of 0.017 mM, lower than rifampicin (MIC 0.048 mM), which served as the posi

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Saxena, Anil K., and Muneer Alam. "ATP Synthase Inhibitors as Anti-tubercular Agents: QSAR Studies in Novel Substituted Quinolines." Current Topics in Medicinal Chemistry 20, no. 29 (2020): 2723–34. http://dx.doi.org/10.2174/1568026620666200903163515.

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Background: Tuberculosis (TB) is a major infectious disease caused by Mycobacterium Tuberculosis. As per the World Health Organization (WHO) report of 2019, there were 1.5 million deaths in the year 2018, mainly because of multi- and extensively drug-resistant tuberculosis (MDR & XDR-TB). Among several antitubercular drugs in clinical trials, bedaquiline (TMC207) is a highly promising drug that was approved by the FDA in 2012 and marketed in 2016 for the treatment of multidrug resistant TB in combination with other drugs. Bedaquiline acts on mycobacterial ATP synthase and is highly effecti

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Md, Akram* Abdul Sayeed Syed Shah Abdus Salaam. "STUDIES ON THE DESIGN, SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF SOME NEW QUINAZOLINONE DERIVATIVES." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 03 (2018): 1915–25. https://doi.org/10.5281/zenodo.1211686.

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Quinazolinone derivatives are the versatile nitrogen containing heterocyclic compounds displaying a wide variety of biological and pharmacological activities like antibacterial, anthelmintic,neuroleptic,antitubercular,platelet,antiaggregating,antifungal,anticancer,anti-inflammatory,antiviral,CNSdepressant activity,antiparkinson,bronchodilator etc. Recently several scientists have elucidated that Quinazolinone system possesses variable sites like position 2 and 3 which can be suitably modified to yield new potent chemotherapeutic and pharmacotherapeutic agents. Further, Schiff bases are use as

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