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261.
Shoaib Khan Shahid Iqbal Fazal Rahim Mazloom Shah Rafaqat Hussain Hamad Alrbyawi Wajid Rehman Ayed A. Dera Liaqat Rasheed H. H. Somaily Rami Adel Pashameah Eman Alzahrani Abd-ElAziem Farouk 《Molecules (Basel, Switzerland)》2022,27(19)
Amylase and glucosidase enzymes are the primary harmful source in the development of the chronic condition known as diabetes mellitus. The main function of these enzymes is to break the macromolecules into simple sugar units which are directly involved in the solubility of blood, hence increasing blood glucose levels. To overcome this effect, there is a need for a potent and effective inhibitor that inhibits the conversion of macromolecules of sugar into its smaller units. In this regard, we synthesized thiazolidinone-based indole derivatives (1–20). The synthesized derivatives were evaluated for α-amylase and α-glucosidase inhibitory activity. Different substituted derivatives were found with moderate to good potentials having IC50 values ranging, for α-amylase, from 1.50 ± 0.05 to 29.60 ± 0.40 μM and, for α-glucosidase, from IC50 = 2.40 ± 0.10 to 31.50 ± 0.50 μM. Among the varied substituted compounds, the most active analogs four (1.80 ± 0.70 and 2.70 ± 0.70), five (1.50 ± 0.05 and 2.40 ± 0.10, respectively) of the series showed few folds better inhibitory activity than standard drug acarbose (IC50 = 10.20 ± 0.10 and 11.70 ± 0.10 μM, respectively). Moreover, structure–activity relationship (SAR) was established and binding interactions were analyzed for ligands and proteins (α-amylase and α-glucosidase) through a molecular docking study. 相似文献
262.
263.
Faiz Ullah Sami Ullah Muhammad Farhan Ali Khan Muhammad Mustaqeem Rizwan Nasir Paracha Muhammad Fayyaz ur Rehman Fariha Kanwal Syed Shams ul Hassan Simona Bungau 《Molecules (Basel, Switzerland)》2022,27(19)
Fluorescent molecules absorb photons of specific wavelengths and emit a longer wavelength photon within nanoseconds. Recently, fluorescent materials have been widely used in the life and material sciences. Fluorescently labelled heterocyclic compounds are useful in bioanalytical applications, including in vivo imaging, high throughput screening, diagnostics, and light-emitting diodes. These compounds have various therapeutic properties, including antifungal, antitumor, antimalarial, anti-inflammatory, and analgesic activities. Different neutral fluorescent markers containing nitrogen heterocycles (quinolones, azafluoranthenes, pyrazoloquinolines, etc.) have several electrochemical, biological, and nonlinear optic applications. Photodynamic therapy (PDT), which destroys tumors and keeps normal tissues safe, works in the presence of molecular oxygen with light and a photosensitizing drugs (dye) to obtain a therapeutic effect. These compounds can potentially be effective templates for producing devices used in biological research. Blending crown compounds with fluorescent residues to create sensors has been frequently investigated. Florescent heterocyclic compounds (crown ether) increase metal solubility in non-aqueous fluids, broadening the application window. Fluorescent supramolecular polymers have widespread use in fluorescent materials, fluorescence probing, data storage, bio-imaging, drug administration, reproduction, biocatalysis, and cancer treatment. The employment of fluorophores, including organic chromophores and crown ethers, which have high selectivity, sensitivity, and stability constants, opens up new avenues for research. Fluorescent organic compounds are gaining importance in the biological world daily because of their diverse functionality with remarkable structural features and positive properties in the fields of medicine, photochemistry, and spectroscopy. 相似文献
264.
Amnah Yusaf Muhammad Usman Matloob Ahmad Muhammad Siddiq Asim Mansha Sami A. Al-Hussain Magdi E. A. Zaki Hafiza Fatima Rehman 《Molecules (Basel, Switzerland)》2022,27(23)
Micellar-enhanced ultrafiltration (MEUF), being a separation technique, was used to remove cobalt metal ion (Co2+) from their aqueous solutions in an application to reduce the toxicity level from industrial effluents using a micellar solution of anionic and cationic surfactants. The metal ions were first adsorbed by using anionic surfactants, i.e., sodium dodecyl sulfate (SDS) and sodium oleate (SO). The calculations for partition (Kx) and binding constants (Kb) and their respective free energy of partition and binding (ΔGp and ΔGb kJmol−1) helped significantly to find out the extent of binding or interaction of Co2+ with the surfactant and ΔGp and ΔGb were found to be −29.50 and −19.38 kJmol−1 for SDS and −23.95 and −12.67 kJmol−1 in the case of SO. MEUF work was also performed to find out the optimal conditions to remove metal pollutants from the aqueous system. For the said purpose, various factors and concentrations effect were studied, such as the concentration of the surfactant, concentration of the electrolyte (NaCl), transmembrane pressure, RPM, and pH. The efficiency of this process was checked by calculating various parameters, such as rejection percentage (R%) and permeate flux (J). A maximum rejection of 99.95% with SDS and 99.99% with SO was attained. 相似文献
265.
Abrar Ahmad Syed Niaz Ali Shah Mehwish Arshad Francine Blanger‐Gariepy Edward R.T. Tiekink Zia ur Rehman 《应用有机金属化学》2021,35(1)
Nitrophenols are among the widely used industrial chemicals worldwide; however, their hazardous effects on environment are a major concern nowadays. Therefore, the conversion of environmentally detrimental p‐nitrophenol (PNP) to industrially valuable p‐aminophenol (PAP), a prototype reaction, is an important organic transformation reaction. However, the traditional conversion of PNP to PAP is an expensive and environmentally unfriendly process. Here, we report a honeycomb‐like porous network with zeolite‐like channels formed by the self‐organization of copper, 1,10‐phenanthroline, 4,4′‐bipyridine, and water. This porous network effectively catalyzed the transformation of hazardous PNP to pharmaceutically valued PAP. In the presence of complex, PNP to PAP conversion occurred in a few minutes, which is otherwise a very sluggish process. To assess the kinetics, the catalytic conversion of PNP to PAP was studied at five different temperatures. The linearity of lnCt/Co versus temperature plot indicated pseudo‐first‐order kinetics. The copper complex with zeolite like channels may find applications as a reduction catalyst both on laboratory and industrial scales and in green chemistry for the remediation of pollutants. 相似文献
266.
Rehman Samiya Keefover-Ring Ken Haq Ihsan ul Dilshad Erum Khan Mohammad Imran Akhtar Nosheen Mirza Bushra 《Applied biochemistry and biotechnology》2019,188(2):460-480
Applied Biochemistry and Biotechnology - Prostate cancer is one of the major causes of cancer-related deaths in men and there is a growing interest in identifying natural compounds for its... 相似文献
267.
Sajid Muhammad Usman Ali Hafiz Muhammad Sufyan Abu Rashid Danial Zahid Saad Ullah Rehman Wajih Ur 《Journal of Thermal Analysis and Calorimetry》2019,137(4):1279-1294
Journal of Thermal Analysis and Calorimetry - The present study comprises experimental investigation on heat transfer and hydrodynamic characteristics of TiO2 nanofluid as coolant in wavy channel... 相似文献
268.
Basit Shafiq M. Allauddin Usman Qaisrani Mumtaz A. Rehman Tauseef-ur- Ahmed Naveed Usman Mushtaq M. Ali Hafiz Muhammad 《Journal of Thermal Analysis and Calorimetry》2022,147(21):12111-12126
Journal of Thermal Analysis and Calorimetry - Heat exchangers serve as pivotal components in industries. Enhancement in the performance of heat exchangers has been the focus of researchers in the... 相似文献
269.
Adinath D. Badar Shubham M. Sulakhe Mahesh B. Muluk Naziya N. M. A. Rehman Prashant P. Dixit Prafulla B. Choudhari Estharla Madhu Rekha Dharmarajan Sriram Kishan P. Haval 《Journal of heterocyclic chemistry》2020,57(10):3544-3557
In the present study, a series of new isoniazid-1,2,3-triazole conjugates ( 5a-k ) was synthesized via click chemistry approach. The newly synthesized compounds were assessed for their in vitro antitubercular and antimicrobial activities. The compound 5g has displayed potent antitubercular activity against Mycobacterium tuberculosis H37Rv (Mtb) with MIC value 1.56 μg/mL. The active compounds were screened for their cytotoxicity profile by MTT assay against RAW 264.7 cell line. The four compounds have shown good in vitro antimicrobial activities against both antibacterial and antifungal pathogens. A molecular docking study was accomplished to identify the probable mode of action of synthesized derivatives. These compounds have shown excellent binding affinity toward Enoyl-acp reductase (INHA) and DNA gyrase. 相似文献
270.
Aftab Alam Najeeb Ur Rehman Mohd Nazam Ansari Amber Hanif Palla 《Molecules (Basel, Switzerland)》2021,26(9)
The present study examined the chemical composition and antimicrobial and gastrointestinal activity of the essential oils of Elettaria cardamomum (L.) Maton harvested in India (EC-I) and Guatemala (EC-G). Monoterpenes were present in higher concentration in EC-I (83.24%) than in EC-G (73.03%), whereas sesquiterpenes were present in a higher concentration in EC-G (18.35%) than in EC-I (9.27%). Minimum inhibitory concentrations (MICs) of 0.5 and 0.25 mg/mL were demonstrated against Pseudomonas aeruginosa in EC-G and EC-I, respectively, whereas MICs of 1 and 0.5 mg/mL were demonstrated against Escherichia coli in EC-G and EC-I, respectively. The treatment with control had the highest kill-time potential, whereas the treatment with oils had shorter kill-time. EC-I was observed to be more potent in the castor oil-induced diarrhea model than EC-G. At 100 and 200 mg/kg, P.O., EC-I exhibited 40% and 80% protection, respectively, and EC-G exhibited 20% and 60% protection, respectively, in mice, whereas loperamide (10 mg/kg, i.p., positive control) exhibited 100% protection. In the in vitro experiments, EC-I inhibited both carbachol (CCh, 1 µM) and high K+ (80 mM)-induced contractions at significantly lower concentrations than EC-G. Thus, EC-I significantly inhibited P. aeruginosa and E. coli and exhibited more potent antidiarrheal and antispasmodic effects than EC-G. 相似文献