Molecular modeling of drug-pathophysiological Mtb protein targets: Synthesis of some 2-thioxo-1, 3-thiazolidin-4-one derivatives as anti-tubercular agents

Synthesis, <i>in-Vitro</i> Cytotoxicity and Antimicrobial Evaluations of Some Novel Thiazole Based Heterocycles

“…35,162.09, 168. 19,199 13.91 (1H, -NH, exchangeable with D 2 O, s). 13 General Procedure for Synthesis of Compounds (5a-d) Method A: A solution of compound (1) (0.01 mol, 1.33 g) and 2-arylmethylidenemalononitrile (4a-d) in absolute ethanol in presence of piperidine as a catalyst was stirred at room temperature for 3 h. The solid product obtained was filtered off, dried and recrystallized from ethanol to afford (5a-d).…”

“…1,2) They have shown a varied range of pharmacological activities such as antimicrobial, [3][4][5] anticonvulsant, 6,7) antibacterial, antifungal and insecticidal activities. [8][9][10][11][12][13] Furthermore, some of them were reported to possess antiviral, 14) antidiabetic, 15,16) antiinflammatory 17,18) and antimalarial 19) activities. Moreover, various substituted rhodanines were found to be anti-tubercular, 20,21) antiproliferative agent against human colon cancer, 22) anti-human immunodeficiency virus (HIV), [23][24][25][26][27] cyclooxygenase (COX-2) inhibitors, 28) potent PTP1B inhibitors, 29) antiglioma and cytotoxicity.…”

“…C-NMR (DMSO-d 6 ) δ:19.05, 34.89, 108.65, 119.70, 125.65, 126 17,. 126.55, 127.20, 127.69, 128.00, 132.30, 133.54, 134.85, 135.05, 152.25, 166.85, 191.75.…”

Synthesis of some 5‐arylidene‐2‐(4‐acetamidophenylimino)‐thiazolidin‐4‐one derivatives and exploring their breast anticancer activity

“…[1][2][3][4] Especially, thiazolidin-4-one-containing compounds have gained significant attention since they were promising scaffolds in the area of medicinal chemistry. [5,6] The literature survey of thiazolidin-4-ones demonstrated a wide range of pharmacological properties, including antimicrobial, [7,8] antiinflammatory, [9,10] antioxidant, [11,12] antitubercular, [13,14] antidiabetic, [15] human immunodeficiency virus (HIV) inhibitors, [16] antihypertensive, [17] anticonvulsant, [18] antihepatitis, [19] antiproliferative, [20] and anticancer activities. [21][22][23][24] Published data showed that anticancer activity of thiazolidin-4-ones may be correlated with their sensitivity to various targets including non-membrane protein tyrosine phosphatase (SHP-2), JNK-stimulating phosphatase-1 (JSP-1), tumor necrosis factor (TNF-α), antiapoptotic biocomplex Bcl-XL-BH3, and inregrin.…”

Uses of 2-(Thiophene-2-carbonylcarbamothioylthio)acetic Acid as a Good Synthon for Construction of Some New Thiazole and Annulated Thiazole Derivatives

“…1,3-Thiazolidine-4-one derivatives are a class of important heterocycles that have attracted considerable attention because of their biological properties such as antibacterial, antifungal, [12][13][14] antiinflammatory, 15,16) antiproliferative activity against human colon cancer, 17) anti-human immunodeficiency virus (HIV), [18][19][20][21][22] anti-tubercular, 23,24) cyclooxygenase (COX-2) inhibitors, 25) potent PTP1B inhibitors, 26) anticonvulsant, 27) antiglioma and cytotoxicity. 28) Based on these considerations, our interest was focused on synthesizing new fused heterocyclic compounds including thiazolidine moiety with suitable substituents.…”