1222831-64-2Relevant academic research and scientific papers
Distinctive inhibition of alkaline phosphatase isozymes by thiazol-2-ylidene-benzamide derivatives: Functional insights into their anticancer role
Ejaz, Syeda Abida,Saeed, Aamer,Shah, Syed Jawad Ali,Hameed, Abdul,Lecka, Joanna,Sévigny, Jean,Iqbal, Jamshed
, p. 6501 - 6513 (2018/04/30)
In the recent years, the role of alkaline phosphatase (AP) isozymes in the cause of neoplastic diseases such as breast, liver, renal, and bone cancer has been confirmed and, thus they represent a novel target for the discovery of anticancer drugs. In this
New substituted thiazol-2-ylidene-benzamides and their reaction with 1-Aza-2-azoniaallene salts. Synthesis and anti-HIV activity
Saeed, Aamer,Al-Masoudi, Najim A.,Ahmed, Amjed A.,Pannecouque, Christophe
experimental part, p. 512 - 520 (2011/07/08)
Aseries of N-(3-(substituted-aikyl- or halophenyl)-4-methylthiazol-2(3H)- ylidene)-substituted alkyl- or halo-benzamides 21-40 were prepared by base-catalyzed cyclization of the corresponding 1-(substituted-alkyl- or halo-benzoyl)-3-(substituted-halophenyl)thioureas 1-20. Substituted pyrazolo[4,3-d]thiazol-5(6aH)-ylidene)benzamides 45a-d were synthesized by cycloaddition of compound 45 with the reactive cumulene intermediates 42a -d. All compounds were evaluated for their antiviral activity against the replication of HIV-1 and HIV-2 in MT-4. Compounds 35 and 39 showed an IC 50 of 2.02 μgmL-1 and 0.40 μgmL-1 against the HIV-2 strain ROD with CC50 of ≥ 104.00 μgmL-1 and > 125.00 μgmL-1, respectively, resulting in a selectivity index of ≥ 52 and > 313. Based on the chemical structure of compounds 35 and 39, these molecules can be proposed to act as NNRTIs. However, it is exceptional to observe an antiretroviral activity that is limited to HIV-2.
Synthesis and antimicrobial activity of some novel 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines
Saeed, Aamer,Shaheen, Uzma,Hameed, Abdul,Kazmi, Faiza
experimental part, p. 333 - 339 (2010/04/30)
The synthesis of several 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines (2a-t) was carried out by base-catalyzed cyclization of corresponding 1-(fluorobenzoyl)-3-(fluorophenyl)thioureas (1a-t) with 2-bromoacetone in aqueous medium. The structures of the synthesized compounds were confirmed by spectral and elemental analysis. All synthesized compounds were evaluated for in vitro antibacterial activity using Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa). The minimum inhibitory concentration (MIC) was determined for the most active compounds. In vitro antifungal activity was also determined against the five fungal species (Rhizopus oryzae, Fusarium oxysporum, Aspergillus terreus, A. niger and A. fumigatus).
