GLORIA

GEOMAR Library Ocean Research Information Access

X

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
  • 1
    Online Resource
    Online Resource
    Design, Synthesis and Antitubercular Evaluation of New Benzimidazole Scaffolds
    Bentham Science Publishers Ltd. ; 2021
    In:  Anti-Infective Agents Vol. 18, No. 4 ( 2021-01-04), p. 375-383
    Details
    In: Anti-Infective Agents, Bentham Science Publishers Ltd., Vol. 18, No. 4 ( 2021-01-04), p. 375-383
    Abstract: 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-(2-(hydroxymethyl)-1H- benzo[d] imidazole-1-yl)- N- substituted acetamides were synthesized by reacting (1H- benzo[d]imidazole -2-yl)methanol with appropriate 2-chloro-N-substituted acetamides / dialkylamino carbonyl chlorides respectively in good yields (42-65%). The antitubercular activity of synthesized compounds was determined by Microplate Alamar Blue Assay (MABA) against Mycobacterium tuberculosis H37Rv strain. The selected compounds were screened for cytotoxicity on normal cell lines. Results: The antitubercular activity data revealed that the 4-chlorophenyl substituted derivative (3b) showed good MIC value at 6.25 μg/mL and, dimethylacetamide substituted derivative (3i) showed MIC at 25 μg/mL among the tested compounds. The substitution of dimethylacetamide (3i) group on the 1st position of benzimidazole has good antitubercular activity (25μg/mL) in comparison to the diethyl acetamide group (3j, 100μg/mL). Conclusion: The antitubercular activity data indicated that the tested compounds exhibited well to moderate inhibition of the H37Rv strains. The compounds (3b) with electronegative substitution on the phenyl moiety exhibited better antitubercular activity than that of the other substitutions. The active compounds have displayed a good safety profile on normal cell lines.
    Type of Medium: Online Resource
    ISSN: 2211-3525
    URL: Article
    DOI: 10.2174/2211352518666200108091454
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
    Location Call Number Limitation Availability
    BibTip Others were also interested in ...
    Online Resource
  • 2
    Online Resource
    Online Resource
    Pus Somewhere, Pus Nowhere, Pus Around the Tube
    Elsevier BV ; 2023
    In:  Ophthalmology Glaucoma Vol. 6, No. 5 ( 2023-09), p. 465-
    Details
    In: Ophthalmology Glaucoma, Elsevier BV, Vol. 6, No. 5 ( 2023-09), p. 465-
    Type of Medium: Online Resource
    ISSN: 2589-4196
    URL: Article
    DOI: 10.1016/j.ogla.2023.05.007
    Language: English
    Publisher: Elsevier BV
    Publication Date: 2023
    Location Call Number Limitation Availability
    BibTip Others were also interested in ...
    Online Resource
  • 3
    Online Resource
    Online Resource
    Synthesis and Evaluation of New 5-methylisoxazole-3-carboxamide Derivatives as Antitubercular Agents
    Bentham Science Publishers Ltd. ; 2015
    In:  Anti-Infective Agents Vol. 13, No. 2 ( 2015-10-29), p. 114-122
    Details
    In: Anti-Infective Agents, Bentham Science Publishers Ltd., Vol. 13, No. 2 ( 2015-10-29), p. 114-122
    Type of Medium: Online Resource
    ISSN: 2211-3525
    URL: Article
    DOI: 10.2174/2211352513666150326004534
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2015
    Location Call Number Limitation Availability
    BibTip Others were also interested in ...
    Online Resource
  • 4
    Online Resource
    Online Resource
    Antitubercular Potential of Novel Isoxazole Encompassed 1, 2, 4- Triazoles: Design, Synthesis, Molecular Docking Study and Evaluation of Antitubercular Activity
    Bentham Science Publishers Ltd. ; 2021
    In:  Anti-Infective Agents Vol. 19, No. 2 ( 2021-04), p. 147-161
    Details
    In: Anti-Infective Agents, Bentham Science Publishers Ltd., Vol. 19, No. 2 ( 2021-04), p. 147-161
    Abstract: Decaprenylphosphoryl-β-D-ribose epimerase (DprE1), a flavoprotein enzyme engaged in the biosynthesis of decaprenylphosphoryl-β-D-arabinofuranose (DPA), is the only contributor of arabinose residues which is fundamental for the mycobacterium cell wall constituents. DprE1 is an interesting target for antitubercular agent and has been exploring to develop potential chemical entities as antitubercular agents. Objective: The objective of the study is the development of novel antitubercular agents targeting Mtb Decaprenylphosphoryl-β-D-ribose epimerase (DprE1). Methods: A series of isoxazole encompassed 1, 2, 4-triazoles were designed based on the antitubercular potential of triazoles and structural features of DprE1 inhibitors. Designed 1, 2, 4- triazoles were synthesized and characterized by spectral studies. The in vitro anti-TB activity of the compounds was screened against Mycobacterium tuberculosis H37Rv strain by Microplate Almar Blue Assay and in vitro cytotoxicity against normal cell lines by MTT assay. Molecular docking study was carried out on DprE1 enzyme to understand designed compounds interactions with amino acid residues at the active site. Results: Antitubercular activity data revealed that eight compounds (6d, 6e,7d, 7e, 10d, 10e, 11d and 11e) have shown promising antitubercular activity with minimum inhibitory concentration at 1.6μg/mL. Cytotoxicity data of anti-TB active compounds demonstrate good safety profile on normal cell lines. Conclusion: Eight compounds have shown promising antitubercular activity with good safety profile on normal cell lines. Molecular docking study revealed that the synthesized compounds have shown non-covalent interactions with amino acid residues of DprE1 enzyme.
    Type of Medium: Online Resource
    ISSN: 2211-3525
    URL: Article
    DOI: 10.2174/2211352518999200711163714
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
    Location Call Number Limitation Availability
    BibTip Others were also interested in ...
    Online Resource
  • 5
    Online Resource
    Online Resource
    QUALITY STANDARDS FOR MEDICAL DEVICES
    Society of Pharmaceutical Tecnocrats ; 2018
    In:  International Journal of Drug Regulatory Affairs Vol. 2, No. 4 ( 2018-02-13), p. 19-24
    Details
    In: International Journal of Drug Regulatory Affairs, Society of Pharmaceutical Tecnocrats, Vol. 2, No. 4 ( 2018-02-13), p. 19-24
    Abstract: Formerly with more augmented disabilities, Medical devices have become decisive device in many circumstances. As these are more perilous, the manufacturer should endow with an ideal medical device in aspects of safety & quality. To produce a homogeneous device globally, there should be some standards to be followed within an explicit country and standard throughout the globe, complying with the quality. In milieu of this resemblance of device globally, International Organization for Standard (ISO) has issued a standard, ISO 13485. This article is made to furnish the details about ISO 13485 and the Quality management system followed by United States manufacturer’s to market their devices within the country, i.e., 21 CFR Part 820.
    Type of Medium: Online Resource
    ISSN: 2321-6794 , 2321-7162
    URL: Article
    DOI: 10.22270/ijdra.v2i4.149
    Language: Unknown
    Publisher: Society of Pharmaceutical Tecnocrats
    Publication Date: 2018
    detail.hit.zdb_id: 2738279-5
    SSG: 15,3
    Location Call Number Limitation Availability
    BibTip Others were also interested in ...
    Online Resource
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...