330978-94-4Relevant academic research and scientific papers
Synthesis, multiparametric structure assessment and biological evaluation of some new 1,3,4-oxadiazoles containing piperidine nucleus
Iqbal, Javed,Aziz-Ur-Rehman,Abbasi, Muhammad Athar,Siddiqui, Sabahat Zahra,Rasool, Shahid,Rehan, Muhammad,Shah, Syed Adnan Ali
, p. 1901 - 1906 (2017)
With an aim to introduce more biologically active compounds, S-substituted derivatives of 5-[1-(4-nitrophenylsulfonyl)piperidin-4-yl]-1,3,4-oxadiazole-2-thiol (3) were synthesized through four steps. In the first step, ethyl 1-(4-nitrophenylsulfonyl)piperidine-4-carboxylate (1)was synthesized by reacting 4-nitrobenzenesulfonyl chloride (a) and ethyl isonipacotate (b) in basic medium. In the second step, compound 1 and hydrazine monohydrate were converted to corresponding hydrazide (2). In third step, hydrazide (2), CS2 and KOH were refluxed in the presence of MeOH to acquire 5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazole-2-thiol (3). In the last step, alkyl/aralkylhalides (4a-o) and 3 were made to react in an aprotic polar solvent to get the final compounds, 2-(substitutedthio)-5-[1-(4-nitrophenylsulfonyl)piperidin-4-yl]-1,3,4-oxadiazole (5a-o). The synthesized compounds were structurally confirmed by spectroscopic techniques including 1H NMR, EIMS and IR. Finally the synthesized compounds were screened for antibacterial activity against five bacterial strains.
Structural basis of binding and justification for the urease inhibitory activity of acetamide hybrids of N-substituted 1,3,4-oxadiazoles and piperidines
Abbasi, Muhammad Athar,Afridi, Sahib Gul,Khan, Ajmal,Khan, Asifullah,Khan, Farman Ali,Lodhi, Muhammad Arif,Rehman, Aziz Ur
, (2020/09/18)
In present, we have performed the Michaelis–Menten kinetics studies of urease inhibitors (6a–o), having basic skeleton of acetamide hybrids of N-substituted 1,3,4-oxadiazoles and piperidines. From the Lineweaver-Burk plot, Dixon plot and their secondary replots, it has been confirmed that all the compounds have inhibited the enzyme competitively with Ki values of in range from 3.11 ± 0.2 to 5.20 ± 0.7 μM. Compound 6a was found to have lowest Ki among the series, while compounds 6d, 6e, 6gand 6i were found subsequently the excellent Ki values after 6a. Molecular docking has supported their types of inhibitions and structure activity-relationship. Most frequently, the nitro group oxygen atoms were found in contact with nickel ions of the active site. Moreover, all the compounds were subjected to toxicity tests and were found nontoxic against human neutrophils and plants, respectively.
Synthesis of acetamide derivatives of 1,2,4-triazole bearing azinane and their binding interactions with bovine serum albumin using spectroscopic techniques
Iqbal, Javed,Ur-Rehman, Aziz,Abbasi, Muhammad Athar,Siddiqui, Sabahat Zahra,Khalid, Hira,Laulloo, Sabina Jhaumeer,Joondan, Nausheen,Taupass, Aniisah Banu,Rasool, Shahid,Shah, Syed Adnan Ali
, p. 1459 - 1478 (2019/01/03)
A new series of acetamide derivatives containing 1,2,4-triazole and azinane moieties has been synthesized and characterized using1 H NMR,13 C NMR, IR, and EI-MS spectroscopic analysis. The intermediate triazole was synthesized through a sequential synthesis of carboxylate and carbohydrazide. The bovine serum albumin (BSA) binding of the newly synthesized 1,2,4-triazole derivatives was evaluated along with thermodynamics, site-selective binding, and synchronous study. The results obtained by BSA binding as well as thermodynamic studies justify that all the compounds show spontaneous interaction with BSA and could be effectively distributed and eliminated from the body. Therefore, the triazole-based analogs might be a useful strategy for designing new drug systems.
