65282-42-0Relevant academic research and scientific papers
Synthesis and in vitro anti-Mycobacterium activity of N-alkyl-1,2- dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation
Pagani, Giuseppe,Pregnolato, Massimo,Ubiali, Daniela,Terreni, Marco,Piersimoni, Claudio,Scaglione, Francesco,Fraschini, Franco,Gascón, Alicia Rodríguez,Mu?oz, José Luis Pedraz
, p. 199 - 204 (2000)
Disseminated infections with Mycobacterium tuberculosis (MT) and Mycobacterium avium complex (MAC) are increasingly opportunistic diseases in patients with advanced acquired human immunodeficiency syndrome (AIDS). A series of N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides has been synthesized, and MICs for MT and MAC strains, either standard or isolated from infected patients, have been determined. Preliminary tests show a good activity and a very low toxicity for some derivatives. Pharmacokinetic studies in the rat show a very rapid elimination from the body after intravenous administration and a poor absorption after oral administration.
Preparation method of benzodithiole skeleton compounds
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Paragraph 0029-0066; 0097-0101; 0103, (2020/04/17)
The invention discloses a preparation method of benzodithiole skeleton compounds. The preparation method comprises the following steps: adding a 2-bromothiobenzamide derivative and S8 into an organicsolvent, adding a ligand and an alkali, performing a reaction in an inert atmosphere under the action of a copper catalyst, and carrying out suction filtration and acidic hydrolysis treatment on the reaction system to obtain the benzodithiole skeleton compounds. The method has the advantages of simplicity in operation, easily available raw materials and reagents, mild conditions, green and environmentally-friendly reaction system, and easiness in separation and purification of the product, is suitable for synthesis of a plurality of benzodithiole skeleton compounds, is especially suitable forlarge-scale industrial production, can prepare high-purity benzodithiole skeleton compounds at high efficiency and high yield, and has a highest product yield of 91%.
1,2-Dithiolan-3-ones and derivatives structurally related to leinamycin. Synthesis and biological evaluation
Salvetti, Raul,Martinetti, Giovanni,Ubiali, Daniela,Pregnolato, Massimo,Pagani, Giuseppe
, p. 995 - 998 (2007/10/03)
Leinamycin, an antitumor antibiotic isolated from Streptomyces sp., shows a 1,2-dithiolan-3-one 1-oxide heterocycle that appears to be involved in the biological activity. Several derivatives related to 1,2-dithiolan-3-one 1-oxide have been prepared and their activity as antineoplastic agents have been investigated. The synthesized compounds did not display a significative antitumor or cytotoxic activity in vitro.
3H-[1,2]Dithiolo[3,4-b]pyridine-3-thione and its derivatives. Synthesis and antimicrobial activity
Pregnolato, Massimo,Terreni, Marco,Ubiali, Daniela,Pagani, Giuseppe,Borgna, Pietro,Pastoni, Fiorenzo,Zampollo, Fabrizio
, p. 669 - 679 (2007/10/03)
A series of 2-substituted isothiazolo[5,4-b]pyridine-3(2H)-thiones, isothiazolo[5,4-b]pyridin-3(2H)-ones, N-substituted 2-sulfanylnicotinamides and the corresponding carbothioamide derivatives were synthesized and evaluated for their antimicrobial activity against several strains of Gram+ and Gram-bacteria and fungi. Chemical syntheses were resumed into a comprehensive cyclic route that enables the reversible conversion for each derivative of the series considered. Among the tested compounds the N-(aralkyl)-2-sulfanylnicotinamides show the highest fungitoxicity (MIC=1.25-5 μg/ml). The best activity towards Gram-positive bacteria was in the range of 2.5-5 μg/ml. Activity against Gram-negative bacteria was generally very poor for all compounds. Copyright
NEW 5-SUBSTITUTED DERIVATIVES OF ETHYL 2,3-DIHYDRO-3-OXOISOTHIAZOLOPYRIDINE-2-ACETATE
Martinez-Merino, Victor,Gil, Maria J.,Gonzalez, Alberto,Zabalza, Jose M.,Navarro, Javier,Manu, Maria A.
, p. 333 - 344 (2007/10/02)
New series of ethyl 5-substituted 2,3-dihydro-3-oxoisothiazolopyridine-2-acetate was prepared either a) directly by reaction of 5-substituted 2-chlorothio-3-pyridinecarbonyl chlorides with ethyl glycinate or b) by oxidation of the correspondent 2-mercapto-3-pyridinecarboxamides.New 5-substituted 1,2-dihydro-2-thio-3-pyridinecarboxylic acids as starting materials are described.
Synthesis of 2-Substituted Isothiazolopyridin-3-ones
Baggaley, Keith H.,Jennings, L. John A.,Tyrrell, A. William R.
, p. 1393 - 1396 (2007/10/02)
The synthesis of some 2-substituted derivatives 1-4 of all four isomeric isothiazolopyridin-3-ones is described.Several novel 1,2-dithiolopyridin-3-ones and 3-thiones were prepared as intermediates.
