mannich-bases and Candidiasis

mannich-bases has been researched along with Candidiasis* in 2 studies

Other Studies

2 other study(ies) available for mannich-bases and Candidiasis

Article	Year
Mannich base limits Candida albicans virulence by inactivating Ras-cAMP-PKA pathway. Scientific reports, 2018, 10-08, Volume: 8, Issue:1 Mannich bases and its derivatives are regarded as supreme pharmacophores in therapeutics. The study investigates the antimycotic potential of Mannich bases, 1-((1H-benzimidazol-1-yl) methyl) urea (C1) and 1-((3-hydroxynapthalen-2-yl) methyl) thiourea (C2), against Candida albicans. Biofilm and hyphal inhibitory activities of the Mannich bases were tested by crystal violet quantification, fluorescence imaging cAMP rescue, qRT PCR, and by molecular docking analysis. The compounds inhibited the biofilms of C. albicans and restrained the filamentation abilities of the pathogen. Structure-activity relationship studies revealed that the presence of urea or thiourea moiety in the tail section is essential for interacting with adenylate cyclase (AC). The Mannich bases seemed to block Ras-cAMP-PKA pathway by inhibiting second messenger activity required for hyphal induction and biofilm formation. In conclusion, the study warrants point-of-care testing of C1/C2 and provides a starting point for deriving several structurally modified Mannich bases which might plausibly replace the prevailing antimycotic drugs in future. Topics: Antifungal Agents; Biofilms; Candida albicans; Candidiasis; Cyclic AMP; Cyclic AMP-Dependent Protein Kinases; Fungal Proteins; Humans; Mannich Bases; Molecular Docking Simulation; ras Proteins; Signal Transduction; Thiourea	2018
Mannich reaction: an approach for the synthesis of water soluble mulundocandin analogues. Bioorganic & medicinal chemistry, 2004, Apr-01, Volume: 12, Issue:7 Semisynthetic modifications at Hydroxy tyrosine (Htyr) unit of mulundocandin (1) were carried out to improve its aqueous solubility. A single step introduction of substituted aminomethyl groups at the ortho position(s) of phenolic hydroxyl of HTyr unit of mulundocandin has been achieved in 7-85% yield. The in vitro screening of Mannich products against Candida albicans and Aspergillus fumigatus, retained the in vivo activity of parent by oral and intraperitoneal route. Compound 20, showed significant improvement in activity over mulundocandin (1) and activity compares well with that of fluconazole. Topics: Animals; Antifungal Agents; Candida albicans; Candidiasis; Disease Models, Animal; Drug Evaluation, Preclinical; Echinocandins; Mannich Bases; Mice; Microbial Sensitivity Tests; Models, Animal; Molecular Structure; Peptides, Cyclic; Solubility; Water	2004

Article

Year

Mannich base limits Candida albicans virulence by inactivating Ras-cAMP-PKA pathway.

Scientific reports, 2018, 10-08, Volume: 8, Issue:1

Mannich bases and its derivatives are regarded as supreme pharmacophores in therapeutics. The study investigates the antimycotic potential of Mannich bases, 1-((1H-benzimidazol-1-yl) methyl) urea (C1) and 1-((3-hydroxynapthalen-2-yl) methyl) thiourea (C2), against Candida albicans. Biofilm and hyphal inhibitory activities of the Mannich bases were tested by crystal violet quantification, fluorescence imaging cAMP rescue, qRT PCR, and by molecular docking analysis. The compounds inhibited the biofilms of C. albicans and restrained the filamentation abilities of the pathogen. Structure-activity relationship studies revealed that the presence of urea or thiourea moiety in the tail section is essential for interacting with adenylate cyclase (AC). The Mannich bases seemed to block Ras-cAMP-PKA pathway by inhibiting second messenger activity required for hyphal induction and biofilm formation. In conclusion, the study warrants point-of-care testing of C1/C2 and provides a starting point for deriving several structurally modified Mannich bases which might plausibly replace the prevailing antimycotic drugs in future.

Topics: Antifungal Agents; Biofilms; Candida albicans; Candidiasis; Cyclic AMP; Cyclic AMP-Dependent Protein Kinases; Fungal Proteins; Humans; Mannich Bases; Molecular Docking Simulation; ras Proteins; Signal Transduction; Thiourea

2018

Mannich reaction: an approach for the synthesis of water soluble mulundocandin analogues.

Bioorganic & medicinal chemistry, 2004, Apr-01, Volume: 12, Issue:7

Semisynthetic modifications at Hydroxy tyrosine (Htyr) unit of mulundocandin (1) were carried out to improve its aqueous solubility. A single step introduction of substituted aminomethyl groups at the ortho position(s) of phenolic hydroxyl of HTyr unit of mulundocandin has been achieved in 7-85% yield. The in vitro screening of Mannich products against Candida albicans and Aspergillus fumigatus, retained the in vivo activity of parent by oral and intraperitoneal route. Compound 20, showed significant improvement in activity over mulundocandin (1) and activity compares well with that of fluconazole.

Topics: Animals; Antifungal Agents; Candida albicans; Candidiasis; Disease Models, Animal; Drug Evaluation, Preclinical; Echinocandins; Mannich Bases; Mice; Microbial Sensitivity Tests; Models, Animal; Molecular Structure; Peptides, Cyclic; Solubility; Water

2004