scholarly journals Synthesis of Some New Folic Acid-Based Heterocycles of Anticipated Biological Activity

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 368
Author(s):  
Ola A. Abu Ali ◽  
Hosam A. Saad ◽  
Bodor M. A. Al Malki
Keyword(s):  
Biological Activity ◽  
Folic Acid ◽  
Ethyl Pyruvate ◽  
Ethyl Cyanoacetate ◽  
Acid Hydrazide ◽  
Ethyl Chloroformate ◽  
Urea Derivatives ◽  
Fused Heterocycles ◽  
Amino Derivatives ◽  
Derivatives Of

To date, no fused heterocycles have been formed on folic acid molecules; for this reason, and others, our target is to synthesize new derivatives of folic acid as isolated or fused systems. Folic acid 1 reacted with ethyl pyruvate, triethyl orthoformate, ethyl chloroformate, thioformic acid hydrazide, and aldehydes to give new derivatives of folic acid 2–6a,b. Moreover, It reacted with benzylidene malononitrile, acetylacetone, ninhydrin, ethyl acetoacetate, ethyl cyanoacetate, and ethyl chloroacetate to give the pteridine fused systems 10–15, respectively. Ethoxycarbonylamino derivate 5 reacted with some nucleophiles containing the NH2 group, such as aminoguanidinium hydrocarbonate, hydrazine hydrate, glycine, thioformic acid hydrazide, and sulfa drugs in different conditions to give the urea derivatives 16–20a,b. Compound 4 reacted with the same nucleophiles to give the methylidene amino derivatives 21–24a,b. The fused compound 10 reacted with thioglycolic acid carbon disulfide, malononitrile, and formamide to give the four cyclic fused systems 25–30, respectively. The biological activity of some synthesized showed moderate effect against bacteria, but no effect shown towards fungi.

Synthesis and Properties of Methyl-, Formyl- and Amino-Diazaphenanthrene

1994 ◽  
Vol 47 (11) ◽  
pp. 2129 ◽  
Author(s):  
L Chrzastek ◽  
B Mianowska ◽  
W Sliwa
Keyword(s):  
Biological Activity ◽  
Activity Data ◽  
Amino Derivatives ◽  
Derivatives Of

Methyl, formyl and amino derivatives of the isomeric benzo [c][1,5] naphthyridine and benzo [f][1,7] naphthyridine have been obtained, and their structures confirmed by 1H n.m.r. spectroscopy. Biological activity data (MIC) for some methyl and formyl derivatives are presented.

ChemInform Abstract: SYNTHESIS AND BIOLOGICAL ACTIVITY OF DERIVATIVES OF 2-ARYLAMINONICOTINIC ACID HYDRAZIDE

1981 ◽  
Vol 12 (25) ◽  
Author(s):  
A. I. MIKHALEV ◽  
L. B. FALALEEVA ◽  
N. I. SHRAMM ◽  
L. M. POLUKHINA ◽  
V. S. ZALESOV ◽  
...  
Keyword(s):  
Biological Activity ◽  
Acid Hydrazide ◽  
Derivatives Of

Synthesis and biological activity of certain amino-derivatives of 5α-steroids

2006 ◽  
Vol 42 (3) ◽  
pp. 322-324 ◽  
Author(s):  
M. I. Merlani ◽  
L. Sh. Amiranashvili ◽  
K. G. Mulkidzhanyan ◽  
E. P. Kemertelidze
Keyword(s):  
Biological Activity ◽  
Amino Derivatives ◽  
Derivatives Of

scholarly journals FLAVONOID COMPOUNDS FROM ARTEMISIA GLABELLA KAR. ET. KIR., SYNTHESIS ON THEIR BASIS AND BIOLOGICAL ACTIVITY

2018 ◽  
pp. 215-222
Author(s):  
Габиден (Gabiden) Маратович (Maratovich) Байсаров (Baysarov) ◽  
Айдана (Аjdana) Рахманиякызы (Rakhmaniyakyzy) Жуматаева (Zhumatayeva) ◽  
Гулим (Gulim) Кенесбековна (Kenesbekovna) Мукушева (Mukusheva) ◽  
Эльвира (El'vira) Эдуардовна (Eduardovna) Шульц (Shul'ts) ◽  
Роза (Roza) Батталовна (Battalovna) Сейдахметова (Seydakhmetova) ◽  
...  
Keyword(s):  
Biological Activity ◽  
Raw Materials ◽  
Hepatoprotective Activity ◽  
Biologically Active ◽  
Secondary Amines ◽  
Moderate Activity ◽  
Amino Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

As a result of complex chemical processing of medicinal raw materials of Artemisia glabella Kar. et Kir., including CO2 extraction and lactones isolation, we have investigated the chemical composition of flavonoids to select the biologically active ones and carry out modifications on their basis. Two flavonoids pectolinaringenin and cirsilineol have been isolated by partition chromatography from the secondary raw materials of Artemisia glabella Kar. et. Kir. and identified. To obtain new biologically active compounds, we have synthesized new amino derivatives of cirsilineol by the Mannich reaction with secondary amines (piperidine and N-methylpiperazine) in isopropanol with the presence of dimethylaminopyridine. In proton NMR spectrum of the synthesized compounds there are proton signals of the initial cirsilineol fragment; however, there is no N-8 proton signal, besides other signals typical for amines’ benzene ring have been observed at 1.53–3.90 ppm. It means that reaction occurred at the C-8 position of carbon in ring A. The synthesized compounds have been studied for various types of biological activity typical for this class, including hepatoprotective and anti-inflammatory activities. Amino derivatives of cirsilineol exhibit a moderate activity against HepG2 cell line, while cirsilineol at a dose of 5 mg/ml expresses a pronounced hepatoprotective activity. Moreover, all samples at a dose of 25 mg/kg show poor anti-inflammatory effects on the model of acute exudative reaction in vivo.

scholarly journals Synthesis and Antimicrobial Studies of New [Tetrakis (1, 2, 4-Triazole / 1, 3, 4-Oxadiazole / 1, 3, 4-Thiadiazole] [Bis-(Benzene-1, 3, 5-Triyl)] Dioxymethylene Compounds

2020 ◽  
pp. 234-245
Author(s):  
Ahmed Neamah Ayyash
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Chemical Structure ◽  
Acid Hydrazide ◽  
Basic Medium ◽  
Tosyl Chloride ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Concentrated Sulfuric Acid ◽  
Derivatives Of

     Synthesis of new heterocyclic compounds containing four five-membered rings together was the main goal of this work. The new derivatives of [tetrakis (1,2,4-triazole /1,3,4-thiadiazole /1,3,4-oxadiazole][bis-(benzene-1,3,5-triyl)] dioxymethylene A7-A18 were synthesized by the reaction of [bis-(dimethyl 5-yl-isophthalate)] dioxymethylene compound A1 which was previously prepared from the reaction of 1,2-dibromomethan and dimethyl 5-hydroxyisophthalate, then treated with hydrazine hydrate to yield the corresponding acid hydrazide A2. In the next step, compound A2 was refluxed with 4-substituted isothiocyanate to give substituted thiosemicarbazides A3-A6. The treatment of the latter compounds in basic medium of 2M of NaOH afforded 1,2,4-Triazole derivatives A7-A10. Whereas the reaction of the same compounds with concentrated sulfuric acid gave 1,3,4-thiadiazoles  A11-A14. Furthermore, the new derivatives of 1,3,4-oxadiazole A15-A18 were obtained by the reaction of thiosemicarbazides and tosyl chloride in presence of pyridine. (C. H. N.) elemental analysis, FT-IR, and 1HNMR techniques were used to characterize the chemical structure of some of the new synthesized compounds which also exhibited an important biological activity.

scholarly journals Amino- and polyaminophthalazin-1(2H)-ones: synthesis, coordination properties, and biological activity

2021 ◽  
Vol 17 ◽  
pp. 558-568
Author(s):  
Zbigniew Malinowski ◽  
Emilia Fornal ◽  
Agata Sumara ◽  
Renata Kontek ◽  
Karol Bukowski ◽  
...  
Keyword(s):  
Biological Activity ◽  
Metal Ion ◽  
Spectroscopic Data ◽  
Anticancer Activities ◽  
Biological Screening ◽  
Biological Assays ◽  
Palladium Catalyzed ◽  
Amino Derivatives ◽  
Derivatives Of ◽  
Ht 29

Amino- and polyaminophthalazinones were synthesized by the palladium‐catalyzed amination (alkyl- and arylamines, polyamines) of 4-bromophthalazinones in good yields. The coordinating properties of selected aminophthalazinones towards Cu(II) ions were investigated and the participation of the nitrogen atoms in the complexation of the metal ion was shown. A biological screening of the potential cytotoxicity of selected synthesized compounds on HT-29 and PC-3 cell lines, as well as on the L-929 cell line, proved that some amino derivatives of phthalazinone show interesting anticancer activities. The detailed synthesis, spectroscopic data, and biological assays are reported.

Synthesis and Biological Activity of 3- and 5-Amino Derivatives of Pyridine-2-carboxaldehyde Thiosemicarbazone

1996 ◽  
Vol 39 (13) ◽  
pp. 2586-2593 ◽  
Author(s):  
Mao-Chin Liu ◽  
Tai-Shun Lin ◽  
Joseph G. Cory ◽  
Ann H. Cory ◽  
Alan C. Sartorelli
Keyword(s):  
Biological Activity ◽  
Amino Derivatives ◽  
Derivatives Of

scholarly journals Biological Activity of Analogues of YM022. Novel (3-Amino Substituted Phenyl)urea Derivatives of 1,4-Benzodiazepin-2-one as Gastrin/Cholecystokinin-B Receptor Antagonists.

1996 ◽  
Vol 44 (7) ◽  
pp. 1412-1414 ◽  
Author(s):  
Masato SATOH ◽  
Yoshinori OKAMOTO ◽  
Hiroyuki KOSHIO ◽  
Mitsuaki OHTA ◽  
Akito NISHIDA ◽  
...  
Keyword(s):  
Biological Activity ◽  
Receptor Antagonists ◽  
Urea Derivatives ◽  
Derivatives Of

scholarly journals Antibiotics Aminosidin. II. Some Amino Derivatives of Aminosidin and Their Biological Activity

1973 ◽  
Vol 21 (3) ◽  
pp. 609-615 ◽  
Author(s):  
HYOZO TANIYAMA ◽  
YOSUKE SAWADA ◽  
SHIGEO TANAKA
Keyword(s):  
Biological Activity ◽  
Amino Derivatives ◽  
Derivatives Of
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