183244-16-8Relevant academic research and scientific papers
ARYLCARBOXAMIDES AND USES THEREOF
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Paragraph 0324, (2017/12/13)
The present disclosure is directed to compounds of formula (I): or a pharmaceutically acceptable salt, solvate or solvate of the salt thereof. Compounds of formula (I) are inhibitors of NOX4 and are useful in the treatment of fibrotic diseases such as scleroderma; lung disease, such as pulmonary fibrosis including idiopathic pulmonary fibrosis (IPF); heart disease, such as heart failure due to ischaemic heart disease, valvular heart disease and hypertensive heart disease, diabetic cardiomyopathy and hypertension; liver disease, such as cirrhosis of the liver; and kidney disease, such as progressive kidney disease glomerulonephritis and diabetic nephropathy; and eye disease such as diabetic retinopathy; skin or subcutaneous scarring, such as keloids, adhesions, hypertrophic scarring or cosmetic scarring; or as an adjuvant or anti-fibrotic in pancreatic cancer to increase chemotherapeutic drug penetration by reducing the density of the connective tissue stroma.
1,3,4-Thiadiazole derivatives as selective inhibitors of iNOS versus nNOS: Synthesis and structure-activity dependence
López-Cara, Luisa C.,Carrión, M. Dora,Entrena, Antonio,Gallo, Miguel A.,Espinosa, Antonio,López, Ana,Escames, Germaine,Acu?a-Castroviejo, Darío,Camacho, M. Encarnación
experimental part, p. 129 - 139 (2012/07/03)
The synthesis of new compounds with a 1,3,4-thiadiazole structure, and their in vitro biological evaluation as inhibitors of both neuronal and inducible Nitric Oxide Synthase (nNOS and iNOS) is described. These compounds have been designed by an isosteric
Synthesis, characterization and evaluation of some 5-substituted 1,3,4-oxadiazole-2-thioesters as antifungal agents
Hasan, Aurangzeb,Sheikh, Md Rezaul Karim,Gapil, Shelly
experimental part, p. 2573 - 2578 (2012/09/07)
A series of 5-substituted 1,3,4-oxadiazole-2-thioesters was synthesized by converting several substituted organic acids successively into the corresponding esters, hydrazides and 5-substituted 1,3,4-oxadiazole-2-thiols. Finally the target compounds: 5-substituted 1,3,4-oxadiazole-2-thioesters were obtained by refluxing 5-substituted 1,3,4-oxadiazole-2-thiols in the presence of acid chloride and potassium hydroxide. The structures of the synthesized compounds were established by physicochemical and spectroscopic methods. The synthesized compounds were evaluated for their in vitro antifungal activity. Some of the evaluated compounds possessed significant antifungal activity as compared to a terbinafine standard.
Synthesis, characterization and antifungal activity of some new 5-substituted 1,3,4-oxadiazole-2-thiols
Hasan, Aurangzeb,Gapil, Shelly,Khan, Izzat
experimental part, p. 2007 - 2010 (2012/02/14)
A series of 5-substituted 1,3,4-oxadiazol-2-thiols (3a-i) was synthesized by refluxing variably substituted organic acids (Ra-i) with methanol to the corresponding esters (1a-i). These esters were then converted to hydrazides (2a-i) by reaction with hydrazine hydrate in the presence of absolute ethanol which was followed by reaction with carbon disulfide and potassium hydroxide. Structure of the synthesized compounds was established by physicochemical and spectral data analysis. Synthesized compounds were subjected to antifungal activity. Antifungal activity was performed against Aspergillus flavus, Mucor species, Aspergillus niger and Aspergillus fumigates, with test compounds at a concentration of 200 μg/mL. Terbinafine was used as the standard drug.
Synthesis, characterization and antifungal activity of some 5-substituted 4-amino-1,2,4-triazole-3-thiols
Hasan, Aurangzeb,Akhtar, Mohammad Nadeem,Gapil, Shelly
scheme or table, p. 5471 - 5476 (2012/07/27)
A series of 5-substituted 4-amino-1,2,4-triazole-3-thiols (4a-i) was synthesized by refluxing substituted organic acids (a-i) with methanol to the corresponding esters (1a-i). These esters were then converted to hydrazides (2a-i) by reaction with hydrazine hydrate in the presence of absolute ethanol. The hydrazides were then converted to 5-substituted 1,3,4-oxadiazole-2-thiols (3a-i) by cyclization reaction with carbon disulfide and KOH which was followed by reaction with hydrazine hydrate in the presence of absolute ethanol. Structure of the synthesized compounds was established by physico-chemical and spectral data analysis. Synthesized compounds were subjected to antifungal activity. Antifungal activity analysis was performed against Aspergillus flavus, Mucor species, Aspergillus niger and Aspergillus fumigates, with test compounds at a concentration of 200 μg/mL. Terbinafine was used as the standard drug.
