Authors Kartsev, V; Geronikaki, A; Petrou, A; Lichitsky, B; Kostic, M; Smiljkovic, M; Sokovic, M; Sirakanyan, S in BENTHAM SCIENCE PUBL LTD published article about INDOLE ALKALOIDS; ENDOPHYTIC FUNGUS; A-C; PENICILLIUM; BIOCHEMISTRY; PRODUCT; TUBULIN in [Kartsev, Victor] InterBioscreen, Moscow, Russia; [Geronikaki, Athina; Petrou, Anthi] Aristotle Univ Thessaloniki, Dept Pharm, Sch Hlth, Thessaloniki 54124, Greece; [Lichitsky, Boris] Zelinsky Inst Organ Chem, Moscow 119991, Russia; [Kostic, Marina; Smiljkovic, Marija; Sokovic, Marina] Univ Belgrade, Mycol Lab, Dept Plant Physiol, Inst Biol Res Sinisa Stankov, Bulevar Despota Stefana 142, Belgrade 11000, Serbia; [Sirakanyan, Samvel] Natl Acad Sci Republ Armenia, Sci Technol Ctr Organ & Pharmaceut Chem, Inst Fine Organ Chem AL Mnjoyan, Ave Azatutyan 26, Yerevan 0014, Armenia in 2019.0, Cited 48.0. Formula: C7H6O2. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4
Background: Griseofulvin – a mold metabolite produced by Penisilium griseofulvum is known as an antifungal drug. Objective: Thus, the goal of this paper is the design and synthesis of new griseofulvin derivatives and evaluation of their antifungal activity. Methods: Forty-two new compounds were synthesized using classical methods of organic synthesis and evaluated for their antimicrobial activity by microdilution method. Results: All forty-two new compounds exhibited very good activity against eight tested micromycetes with MIC ranging from 0.0075-0.055 mg/ml and MFC from 0.02-024 mg/ml. All compounds exhibited better activity than reference drugs ketoconazole (7-42 times) and bifonazole (3-16 fold). The most promising was compound 15. The most sensitive fungal was found to be T. viride, while the most resistant, as was expected, was A. fumigatus. It should be mentioned that most of compounds exhibited better activity than griseofulvin. The molecular docking studies revealed that the most active compound have the same hydrophobic and H-bonding interactions with Thr276 residue observed for griseofulvin forming 3 hydrogen bonds while griseofulvin only one. In general, the molecular docking results coincide with experimental. Conclusion: Forty-two giseofulvin derivatives were designed, synthesized and evaluated for antimicrobial activity. These derivatives revealed good antifungal activity, better than reference drugs ketoconazole, bifonazole, and griseofulvin as well.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles