Analysis of 1-Aroyl-3-[3-chloro-2-methylphenyl] Thiourea Hybrids as Potent Urease Inhibitors: Synthesis, Biochemical Evaluation and Computational Approach by Samina Rasheed, Mubashir Aziz, Aamer Saeed, Syeda Abida Ejaz, Pervaiz Ali Channar, Seema Zargar, Qamar Abbas, Humidah Alanazi, Mumtaz Hussain, Mona Alharbi, Song Ja Kim, Tanveer A. Wani, Hussain Raza

Subjects: “…thiourea hybrids…”
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Three New Acrylic Acid Derivatives from <i>Achillea mellifolium</i> as Potential Inhibitors of Urease from Jack Bean and <i>α</i>-Glucosidase from <i>Saccharomyces cerevisiae</i> by Umar Farooq, Sara Khan, Sadia Naz, Tanveer A. Wani, Syed Majid Bukhari, Abullahi Tunde Aborode, Sohail Anjum Shahzad, Seema Zargar

“…In-vitro studies showed that compound <b>3</b> has the highest inhibition against urease enzyme (IC₅₀ =10.46 ± 0.03 μΜ), followed by compound <b>1</b> and compound <b>2</b> with percent inhibition and IC₅₀ value of 16.87 ± 0.02 c and 13.71 ± 0.07 μΜ, respectively, compared to the standard (thiourea-IC₅₀ = 21.5 ± 0.01 μΜ). The investigated IC₅₀ value of compound 3 against the urease enzyme is two times lower compared to thiourea, suggesting that this compound is twice as active compared to the standard drug. …”
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N-Adamantanyl-2-(2-(phenyl)hydrazone)-3-oxobutanamides endowed with dual inhibitors of urease and α-glucosidase: Design, synthesis, and computational studies by Abdul Manan, Hafiza Zara Tariq, Syeda Abida Ejaz, Aamer Saeed, Aftab Ahmed, Atteeque Ahmed, Tanveer A. Wani, Muhammad Saleem, Jabir Hussain, Ghulam Shabir, Hesham El-Seedi

“…The compound 6c exhibited strong inhibition of urease enzyme, with IC50 value of 13.10 ± 0.55 µM, in comparison to the IC50 value of the standard inhibitor thiourea i.e., 16.4 ± 1.02 µM. In addition to this, compounds 6d and 6e demonstrated a significant α-glucosidase inhibition with IC50 values of 17.16 ± 0.91 µM but found less potent as compared to the standard inhibitor Acarbose, i.e. 9.80 ± 0.20 μM. …”
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Design, Synthesis, Kinetic Analysis and Pharmacophore-Directed Discovery of 3-Ethylaniline Hybrid Imino-Thiazolidinone as Potential Inhibitor of Carbonic Anhydrase II: An Emerging... by Atteeque Ahmed, Mubashir Aziz, Syeda Abida Ejaz, Pervaiz Ali Channar, Aamer Saeed, Seema Zargar, Tanveer A. Wani, Asad Hamad, Qamar Abbas, Hussain Raza, Song Ja Kim

“…Synthesis was carried out by diethyl but-2-ynedioate cyclization and different acyl thiourea substitutions of 3-ethyl amine. The CA (II) enzyme inhibition profile for all synthesized derivatives was determined. …”
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Novel Coumarin Derivatives as Potential Urease Inhibitors for Kidney Stone Prevention and Antiulcer Therapy: From Synthesis to In Vivo Evaluation by Kiran Shahzadi, Syed Majid Bukhari, Asma Zaidi, Tanveer A. Wani, Muhammad Saeed Jan, Seema Zargar, Umer Rashid, Umar Farooq, Aneela Khushal, Sara Khan

“…The in silico analyses were augmented by an enzymatic assay, which revealed that compounds <b>3a</b> and <b>5a</b> had strong inhibitory action, with IC₅₀ of 0.412 µM (64.0% inhibition) and 0.322 µM (77.7% inhibition), respectively, compared to standard (Thiourea) with 82% inhibition at 0.14 µM. Moreover, the most active compound, <b>5a</b>, was further tested in vivo for antiulcer activity by different types of induced ulcers, including pyloric ligation-, ethanol-, aspirin-, and histamine-induced ulcers. …”
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