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P. S. Murthy – One of the best experts on this subject based on the ideXlab platform.

  • Antitubercular Activity of garlic (allium sativum) extract on combination with conventional Antitubercular drugs in tubercular lymphadenitis
    Indian Journal of Clinical Biochemistry, 1999
    Co-Authors: R. L. Gupta, Sundeep Jain, V. Talwar, H. C. Gupta, P. S. Murthy

    Abstract:

    Based on our demonstration earlier that ethanol extract, water extract and a compound purified from garlic possessed in vitro Antitubercular Activity against drug resistant and susceptible Mycobacterium tuberculosis , we tried the effect of garlic extract in 30 patients of tubercular lymphadenitis. For ethical considerations, two groups of patients, 30 each, were given Antitubercular therapy (ATT) consisting of isoniazid, rifampicin, ethambutol and pyrazinamide for 30 days. For the next 15 days (31 to 45 days) group 1 patients received 3–6 garlic pearls per day in addition to ATT while group 2 patients received ATT only. From 46th day onwards both the groups received ATT only for 6–8 months. Antitubercular Activity of the serum samples collected on 45th day was assessed by its effect on the growth of M. tuberculois . The serum of group 1 patients showed significantly much higher Antitubercular Activity than that of group 2 patients. Further, there was relief of dyspeptic symptoms caused by ATT therapy in patients of group 1 with garlic plus ATT therapy but no change in group 2 patients with ATT only. Liver function and hematological tests were normal in both the groups after 6 months of therapy. Garlic extracts or compounds have a good potential as Antitubercular(s) drug if given as a supplement to ATT.

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  • Structure-Antitubercular Activity relationship of phenothiazine-type calmodulin antagonists.
    International Clinical Psychopharmacology, 1995
    Co-Authors: P. Ratnakar, Savita P. Rao, P. Sriramarao, P. S. Murthy

    Abstract:

    Six neuroleptic (antipsychotic) phenothiazine derivatives which are calmodulin antagonists were tested for their Activity against Mycobacterium tuberculosis H37Rv in order to understand their structure-Antitubercular Activity relationship. Out of the six derivatives tested (trifluoperazine, chlorpromazine, triflupromazine, thioridazine, acetopromazine and fluphenazine), trifluoperazine appears to be a more potent Antitubercular drug than others with a minimum inhibitory concentration (MIC) of 5 micrograms/ml. Chlorpromazine, triflupromazine and thioridazine are also active but less potent and have a higher MIC of 20 micrograms/ml. Acetopromazine and fluphenazine could not completely inhibit the growth even at a high concentration of 20 micrograms/ml. These results indicate that a methylpiperazinylpropyl group attached to the nitrogen (position 10) atom and trifluoromethyl group at the second carbon confer Antitubercular Activity to the phenothiazine molecule. It is suggested that trifluoperazine or one of its derivatives could be useful as one of the drugs in the multi-drug regimen for the treatment of tuberculosis with psychotic problems or vice versa.

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Dharmarajan Sriram – One of the best experts on this subject based on the ideXlab platform.

  • Design, Synthesis, and in vitro Antitubercular Activity of 1,2,3‐triazolyl‐dihydroquinoline derivatives
    Chemical biology & drug design, 2018
    Co-Authors: Saleha Banu, Rajitha Bollu, Lingaiah Nagarapu, Jagadeesh Babu Nanubolu, Perumal Yogeswari, Dharmarajan Sriram, Shravan Kumar Gunda, Divyasphoorthi Vardhan

    Abstract:

    In the quest for new active molecules against Mycobacterium tuberculosis, a series of dihydroquinoline derivatives possessing triazolo substituents were efficiently synthesized using click chemistry. The structure of 6l was evidenced by X-ray crystallographic study. The newly synthesized compounds were evaluated for their in vitro Antitubercular Activity against Mycobacterium tuberculosis H37Rv (ATCC27294). The compounds 6a, 6g, and 6j (MIC: 3.13 μg/ml) showed promising Activity when compared to the first-line drug such as ethambutol. In addition, the structure and Antitubercular Activity relationship were further supported by in silico molecular docking studies of the active compounds against 3IVX.PDB (crystal structure of pantothenate synthetase in complex with 2-(2-(benzofuran-2-ylsulfonylcarbamoyl)-5-methoxy-1H-indol-1-yl)acetic acid).

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  • synthesis and in vitro Antitubercular Activity of 4 aryl alkylsulfonylmethylcoumarins as inhibitors of mycobacterium tuberculosis
    Bioorganic & Medicinal Chemistry Letters, 2012
    Co-Authors: Malaichamy Jeyachandran, Dharmarajan Sriram, Penugonda Ramesh, Palaniappan Senthilkumar, Perumal Yogeeswari

    Abstract:

    Abstract A series of 4-aryl/alkylsulfonylmethylcoumarins have been synthesized and screened for in vitro Antitubercular Activity against Mycobacterium tuberculosis H 37 Rv (MTB). Four of the compounds showed MIC in the range of 0.78–3.13 μg/mL proving their potential Activity.

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  • Synthesis and in vitro Antitubercular Activity of 4-aryl/alkylsulfonylmethylcoumarins as inhibitors of Mycobacterium tuberculosis.
    Bioorganic & medicinal chemistry letters, 2012
    Co-Authors: Malaichamy Jeyachandran, Dharmarajan Sriram, Penugonda Ramesh, Palaniappan Senthilkumar, Perumal Yogeeswari

    Abstract:

    Abstract A series of 4-aryl/alkylsulfonylmethylcoumarins have been synthesized and screened for in vitro Antitubercular Activity against Mycobacterium tuberculosis H 37 Rv (MTB). Four of the compounds showed MIC in the range of 0.78–3.13 μg/mL proving their potential Activity.

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Ramrao A. Mane – One of the best experts on this subject based on the ideXlab platform.

  • synthesis and Antitubercular Activity of new 1 3 4 oxadiazoles bearing pyridyl and thiazolyl scaffolds
    Bioorganic & Medicinal Chemistry Letters, 2016
    Co-Authors: Sambhaji T. Dhumal, Amarsinh R. Deshmukh, Dhiman Sarkar, Vijay M. Khedkar, Laxman Nawale, Manisha R Bhosle, Ramrao A. Mane

    Abstract:

    Abstract In search of more potent and safe new Antitubercular agents, here new 2-pyridinyl substituted thiazolyl-5-aryl-1,3,4-oxadiazoles ( 6a – o ), have been designed and synthesized using thionicotinamide as a starting, following novel multistep synthetic route. An intermediate, pyridinyl substituted thiazolyl acid hydrazide ( 4 ) when condensed with benzoic acids/nicotinic acids ( 5a – o ) in the presence of silica supported POCl 3 yielded better to excellent yields of the title compounds. All the synthesized compounds ( 6a – o ) and intermediate acid hydrazide ( 4 ) have been screened for their in vitro Antitubercular Activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis BCG. Amongst them, 6f , 6j , 6l and 6o have revealed promising Activity against M. bovis BCG at concentrations less than 3 μg/mL. These compounds have shown low cytotoxicity (CC 50 : >100 μg/mL) towards four human cancer cell lines. Molecular docking study has also been performed against mycobacterial enoyl reductase (InhA) enzyme to gain an insight into the binding modes of these molecules and recorded good binding affinity. The ADME properties the title products have also been analyzed.

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  • Synthesis and Antitubercular Activity of New Thiazolidinones with Pyrazinyl and Thiazolyl scaffolds: New Thiazolidinones with Pyrazinyl and Thiazolyl scaffolds
    Journal of Heterocyclic Chemistry, 2015
    Co-Authors: Sambhaji T. Dhumal, Amarsinh R. Deshmukh, Lalit D. Khillare, Manisha Arkile, Dhiman Sarkar, Ramrao A. Mane

    Abstract:

    Emergence of multidrug resistant and extensively drug resistant tuberculosis has prompted to develop new molecular entities to treat the disease. A series of new 4-thiazolidinones with pyrazinyl and thiazolyl scaffolds has been synthesized, and their Antitubercular Activity is reported. The title 4-thiazolidinones, N-(pyrazinyl substituted thiazoloylamino)-2-aryl-4-thiazolidinones (6a, 6b, 6c, 6d, 6e, 6f, 6g, 6h, 6i, 6j) have been first time prepared using pyrazinamide as a starting material via five successive steps. The purity and the structures of the intermediates (carboethoxythiazole, acid hydrazide, and azomethines) and title thiazolidinones (6a, 6b, 6c, 6d, 6e, 6f, 6g, 6h, 6i, 6j) have been confirmed by TLC and spectral analyses, respectively. An Antitubercular screening of the new 4-thiazolidinones has been performed on bacterial strains, Mycobacterium tuberculosis H37Ra and Mycobacterium BCG using the solutions of different concentrations of the compounds (6a, 6b, 6c, 6d, 6e, 6f, 6g, 6h, 6i, 6j) and the screening results are presented. Compound 6a has displayed notable Antitubercular Activity.

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