Synthesis, in vitro biological analysis and molecular docking studies of new thiadiazole-based thiourea derivatives as dual inhibitors of a-amylase and a-glucosidase by Imran Khan, Wajid Rehman, Fazal Rahim, Rafaqat Hussain, Shoaib Khan, Liaqat Rasheed, Ashwag S. Alanazi, Mohamed Hefnawy, Mohammed M. Alanazi, Syed A.A. Shah, Muhammad Taha

Subjects: Get full text

New Triazinoindole Bearing Benzimidazole/Benzoxazole Hybrids Analogs as Potent Inhibitors of Urease: Synthesis, In Vitro Analysis and Molecular Docking Studies by Sundas Mumtaz, Shahid Iqbal, Mazloom Shah, Rafaqat Hussain, Fazal Rahim, Wajid Rehman, Shoaib Khan, Obaid-ur-Rahman Abid, Liaqat Rasheed, Ayed A. Dera, Hanan A. Al-ghulikah, Sana Kehili, Eslam B. Elkaeed, Hamad Alrbyawi, Mohammed Issa Alahmdi

“…The synthesized analogs were tested against urease enzyme (in vitro) as compared to the standard thiourea drug. All triazinoindole-based benzimidazole/benzoxazole analogs (<b>1</b>–<b>25</b>) exhibited moderate to excellent inhibition profiles, having IC₅₀ values of 0.20 ± 0.01 to 36.20 ± 0.70 μM when evaluated under the positive control of thiourea as a standard drug. …”
Get full text

Synthetic transformation of 6-Fluoroimidazo[1,2-a]Pyridine-3-carbaldehyde into 6-Fluoroimidazo[1,2-a]Pyridine-Oxazole Derivatives: In vitro urease inhibition and in silico study by Rafaqat Hussain, Wajid Rehman, Fazal Rahim, Ayman M. Mahmoud, Mohammed M Alanazi, Shoaib Khan, Liaqat Rasheed, Imran Khan

“…Results: Particularly, the analogs 4i (IC50 = 5.68 ± 1.66 μM), 4o (IC50 = 7.11 ± 1.24 μM), 4 g (IC50 = 9.41 ± 1.19 μM) and 4 h (IC50 = 10.45 ± 2.57 μM) were identified to be more potent than standard thiourea drug (IC50 = 21.37 ± 1.76 μM). Additionally, the variety of spectroscopic tools such as 1H NMR, 13C NMR and HREI-MS analysis were employed to confirm the precise structures of all the newly afforded analogs. …”
Get full text

Novel benzoxazole-based thiosemicarbazide derivatives as new inhibitors of urease and β-Glucuronidase: Synthesis, in vivo anti-nematodal activity and ADMET prediction along with in... by Shoaib Khan, Fazal Rahim, Wajid Rehman, Mohammed M. Alanazi, Ashwag S. Alanazi, Rafaqat Hussain, Muhammad Taha, Farhan Ali, Muhammad Usman Khan, Syed Adnan Ali Shah

“…After spectral confirmation all the synthesized compounds were evaluated for urease and β-Glucuronidase inhibitory activity in order to explore their biological significances in the presence of standard drug thiourea (IC50 = 21.86 ± 0.40) and D-saccharic acid 1,4-lactone (IC50 value 22.00 ± 1.10 µM) respectively. …”
Get full text

Synthesis, biological evaluation and molecular docking study of pyrimidine based thiazolidinone derivatives as potential anti-urease and anti-cancer agents by Shoaib Khan, Hayat Ullah, Fazal Rahim, Rafaqat Hussain, Yousaf Khan, Muhammad Saleem Khan, Rashid Iqbal, Baber Ali, Mohammed Fahad Albeshr

“…Their inhibitory potentials were determined using the minimum inhibitory concentration (MIC) in the presence of their standard drugs, Thiourea (IC50 = 8.20 ± 0.20 µM) and Tetrandrineb (IC50 = 12.30 ± 0.10 µM) respectively. …”
Get full text