Muhammad Taha

• Ph.D
• Professor (Associate ) at Imam Abdulrahman Bin Faisal University

Alzheimer's is a long‐term neurodegenerative illness that causes brain cells to deteriorate and has an especially negative impact on a person's capacity for independent functioning. Despite ongoing research, there is no effective cure for the disease, although early intervention can reduce its long‐lasting effects. In search for the more effective...

This study presents the single-step synthesis of a variety of 3-phenylimidazo[1,2-a]pyridine derivatives 1–24 by reacting different phenacyl bromides with 2-aminopyridine in the presence of DABCO (1,4-diazabicyclo[2.2.2]octane) as a base. Compounds were characterized by spectroscopic techniques to confirm their structures. All synthetic derivatives...

Aim: Quinoline scaffolds are serving as the core structure for numerous antifungal, analgesic, antipyretic, anti-inflammatory drugs as well as have also been investigated for their potential antidiabetic properties. Though further exploration is required in this area as the current antidiabetic agents, such as acarbose, miglitol and voglibose, are...

A series of benzothiazine derivatives (1–17) were synthesized via an intermolecular cyclocondensation reaction involving 2‐aminothiophenol (i) and substituted phenacyl bromide (ii). Structural elucidation of these synthetic derivatives utilized EI–MS, HR‐EIMS, ¹H NMR, and ¹³C NMR spectroscopic techniques. The synthesized analogs were evaluated agai...

Aim: Current study aims exploration of bis-benzoxazole bearing bis-Schiff base scaffolds (1-16) as anti-Alzheimer's agents.Materials & methods: 2-aminophenol is used as starting materials which react with different reagents in different step to give us bis-benzoxazole bearing bis-Schiff base analogs. NMR and HREI-MS techniques were used for charact...

A series of new benzohydrazide based thiourea derivatives were synthesized, characterized through different spectroscopic techniques like 1 HNMR, 13 CNMR and HREI-MS and screened against Bacillus pasteurii (B.P) and Jack bean (J.B) ureases enzymes. All derivatives showed good inhibitory potential ranging from 20.05 ± 0.03 to 39.34 ± 1.05 (against J...

The current study was aimed to synthesize piperazine‐based bis‐Schiff base derivatives (1–15) and were also screened in vitro for their inhibition against urease enzyme under the positive control of thiourea drug (IC50 value of 36.40±2.35 μM). Among the tested analogs, the maximum potency was shown by analog 2 with the lowest IC50 value of 2.10±1.1...

The current study involves the synthesis of Schiff bases based on 1,2,4-triazoles skeleton and assessing their α-amylase and α-glucosidase profile. Furthermore, the precise structures of the synthesized derivatives were elucidated using various spectroscopic methods such as ¹ H-NMR, ¹³ C-NMR and HREI-MS. Using glimepiride as the reference standard,...

A library of imidazole‐thiadiazole compounds ( 1–24 ) was synthesized to explore their therapeutic applications. The compounds were subjected to meticulous in vitro evaluation against α ‐glucosidase, α ‐amylase, acetylcholinesterase (AChE), and butylcholinesterase (BChE) enzymes. Compounds were also investigated for antioxidant activities using cup...

The current research deals with the microwave-assisted green synthesis of two acridine-based libraries and in vitro urease inhibitory activities. The first library is based on 9-phenyl acridine 1–13 derivatives, while the second is based on 10H-acridin-9-one 14–33 derivatives. All compounds were characterized using FTIR, EI-MS, 1H-NMR, and CHNX tec...

A series of 3-substituted and 3,5-disubstituted rhodanine-based derivatives were synthesized from 3-aminorhodanine and examined for α-amylase inhibitory, DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging activities in vitro. These derivatives displayed significant α-amylase inhi...

Background: Unsymmetrical thioureas 1–20 were synthesized and then characterized by various spectroscopy techniques such as UV, IR, fast atom bombardment (FAB)-MS, high-resolution FAB-MS, ¹ H-NMR and ¹³ C-NMR. Methods: Synthetic compounds 1–20 were tested for their ability for antioxidant, lipoxygenase and xanthine oxidase activities. Results: Comp...

In an effort to develop novel enzyme inhibitors with potent activity and high selectivity, a series of nicotinonitrile derivatives was synthesized. Cyano pyridone intermediates undergo nucleophilic substitution reactions with variously substituted phenacyl halides to yield the nicotinonitriles 1–20. All nicotinonitriles exhibited moderateto excelle...

We have synthesized indole-based sulfonamides derivatives (1-10), characterized through NMR and HR-EIMS, and screened against α-glucosidase and α-amylase enzymes. All the synthesized analogues showed various degrees of inhibitory potential ranging between 1.10 ± 0.10 to 10.90 ± 0.20 µM (against α-glucosidase) and 0.70 ± 0.10 to 11.30 ± 0.20 µM (aga...

Diabetes II is the most occurring disease which involves the blood sugar to rise and cause diabetes with many complications including weight loss, kidney failure, heart disease etc. The current drugs available for managing diabetes II have side effects and cause problems. We design the new thiazole compounds to inhibits the enzymes that involves in...

A rare but lethal central nervous system disease known as granulomatous amoebic encephalitis (GAE) and potentially blinding Acanthamoeba keratitis are diseases caused by free-living Acanthamoeba. Currently, no therapeutic agent can completely eradicate or prevent GAE. Synthetic compounds are a likely source of bioactive compounds for developing new...

Background: Diabetes mellitus is a significant health disorder; therefore, researchers should focus on discovering new drug candidates. Methods: A series of indole–pyridine carbonitrile derivatives, 1–34, was synthesized through a one-pot multicomponent reaction and evaluated for antidiabetic and antioxidant potential. Results: In this library, 12...

Background: Quinoline and acyl thiourea scaffolds have major chemical significance in medicinal chemistry. Quinoline-based acyl thiourea derivatives may potentially target the urease enzyme. Materials & methods: Quinoline-based acyl thiourea derivatives 1–26 were synthesized and tested for urease inhibitory activity. Results: 19 derivatives (1–19)...

A library of 22 derivatives of 1,3,4‐oxadiazole‐2‐thiol was synthesized, structurally characterized, and assessed for its potential to inhibit α‐amylase, α‐glucosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and antioxidant activities. Most of the tested compounds demonstrated good to moderate inhibition potential; however, thei...

Background: Diabetes mellitus (DM) is a chronic disorder considered a major global health challenge in the 21st century. α-Glucosidase enzyme is a well-known drug target to treat type II DM. Methods: A new library of biphenyl-substituted triazines was synthesized and confirmed by various spectroscopic techniques. Results: All compounds showed poten...

Background: Researchers seeking new drug candidates to treat diabetes mellitus have been exploring bioactive molecules found in nature, particularly tetrahydropyridines (THPs). Methods: A library of THPs 1-31 was synthesized via a one-pot multicomponent reaction and investigated for their inhibition potential against α-glucosidase and α-amylase enz...

Diabetes mellitus is a syndrome that is caused due to the imbalance of insulin production in the body. In the present study we have synthesized a class of fifteen compounds (1–15) based on thiadiazole-bearing thiourea that were assessed for in vitro alpha-amylase and alpha-glucosidase inhibitory potentials against standard drug acarbose. In this se...

Helicobacter pylori causes severe stomach disorders and the use of enzyme inhibitors for treatment is one of the possible therapies. The great biological potential of imine analogs as urease inhibitors has been the focus of researchers in past years. In this regard, we have synthesized twenty-one derivatives of dichlorophenyl hydrazide. These compo...

The clinical significance of benzimidazole-containing drugs has increased in the current study, making them more effective scaffolds. These moieties have attracted strong research interest due to their diverse biological features. To examine their various biological significances, several research synthetic methodologies have recently been establis...

Diabetes is also known as a critical and noisy disease. Hyperglycemia, that is, increased blood glucose level is a common effect of uncontrolled diabetes, and over a period of time can cause serious effects on health such as blood vessel damage and nervous system damage. However, many attempts have been made to find suitable and beneficial solution...

Aim: To synthesize pyrrolopyridine-based thiazolotriazoles as a novel class of α-amylase and α-glucosidase inhibitors and to determine their enzymatic kinetics. Methodology: Pyrrolopyridine-based thiazolotriazole analogs (1-24) were synthesized and characterized through proton nuclear magnetic resonance, carbon-13 nuclear magnetic resonance and hig...

We have synthesized twelve thiazole-thiourea hybrid derivatives (1-12) and evaluated against acetylcholinesterase and butyrylcholinesterase enzymes. All analogues showed outstanding activities having IC50 values ranged from 0.30 ± 0.05 to 15.40 ± 0.30 µM (AChE) and 0.40 ± 0.05 to 22.70 ± 0.40 µM (BuChE) as compared to standard drug Donepezil (IC50...

Here, we discuss the synthesis of thiosemicarbazide derivatives based on benzoxazole. These compounds were obtained via sequence of reactions. The targeted products were confirmed using a number of spectroscopic methods, including NMR (1H and 13C) and EI-MS. After spectral confirmation all the synthesized compounds were evaluated for urease and β-G...

A library of 2-oxopyridine carbonitriles 1-34 was synthesized by regioselective nucleophilic substitution reactions. In the first step, a one-pot multicomponent reaction yield pyridone intermediates. The resulting pyridone intermediates were then reacted with phenacyl halides in DMF and stirred at 100 °C for an hour to afford the desired compounds...

The current study has afforded twelve analogs (4a-l) of pyridine-derived bis-oxadiazole containing bis-schiff base and subsequently evaluated for their potential to inhibit thymidine phosphorylase(in vitro). All the synthesized analogs were structurally elucidated using various spectroscopic tools including NMR and HREIMS. All synthesized scaffolds...

Twenty-one analogs were synthesized based on benzimidazole, incorporating a substituted benzaldehyde moiety (1–21). These were then screened for their acetylcholinesterase and butyrylcholinesterase inhibition profiles. All the derivatives except 13, 14, and 20 showed various inhibitory potentials, ranging from IC50 values of 0.050 ± 0.001 µM to 25....

This work reports the convenient approach for the synthesis of thiazole based thiourea derivatives (1-21) from 2-bromo-1-(4-fluorophenyl)thiazole-1-one and phenyl isothiocyanates. The scope and diversity were achieved from readily available phenyl isothiocyanates. This protocol involves an oxidative C-S bond formation. Moreover, hybrid thiazole bas...

Background: Diabetes mellitus is a serious global health concern, and this is expected to impact more than 300 million people by 2025. The current study focuses on identifying substituted indolin-2-one-based inhibitors for two indispensable drug targets, α-amylase and α-glucosidase. Methods: The structures of synthetic compounds were confirmed by s...

Alzheimer's disease is a major public brain condition that has resulted in many deaths, as revealed by the World Health Organization (WHO). Conventional Alzheimer's treatments such as chemotherapy, surgery, and radiotherapy are not very effective and are usually associated with several adverse effects. Therefore, it is necessary to find a new thera...

A range of substituted arylidene chromane-2,4-dione derivatives 1–30 were synthesized by the condensation reaction between 6-chloro-4-hydroxycoumarin and different benzaldehydes in ethanol. All synthesized derivatives are structurally new and fully characterized by various spectroscopic approaches. Compounds were tested for α-amylase inhibitory and...

This study was carried out to synthesize benzotriazole-based bis-Schiff base scaffolds (1–20) and assess them in vitro for α-glucosidase inhibitory potentials. All the synthetics analogs based on benzotriazole-based bis-Schiff base scaffolds were found to display an outstanding inhibition profile on screening against the α-glucosidase enzyme. The s...

In search of potent inhibitors of cholinesterase enzymes and antioxidant agents, synthetic derivatives dihydroquinazolin-4(1H)-one 1-38 were evaluated as potential anti-Alzheimer agents through in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitions and radical (DPPH and ABTS) scavenging activities. The (SAR) was mainly ba...

Triazole-based thiosemicarbazone derivatives (6a-u) were synthesized then characterized by spectroscopic techniques, such as 1HNMR and 13CNMR and HRMS (ESI). Newly synthesized derivatives were screened in vitro for inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. All derivatives (except 6c and 6d, w...

The current study reports synthesis, structure establishment, anti-glycation, and anti-oxidant activities of ligand 4-[(2-hydroxynaphthalene-1-ylmethylene)-amino]-benzenesulfonamide (L) and its coordination compounds with Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) metal ions. The analytical techniques used (UV-Vis, FT-IR, CHN/S) confirmed the biden...

Acetylcholinesterase prevails in the healthy brain, with butyrylcholinesterase reflected to play a minor role in regulating brain acetylcholine (ACh) levels. However, BuChE activity gradually increases in patients with (AD), while AChE activity remains unaffected or decays. Both enzymes therefore represent legitimate therapeutic targets for amelior...

A series of thiazole-based thiazolidinone derivatives (1-20) have been synthesized and evaluated against α-glucosidase and α-amylase enzymes. All derivatives showed good α-glucosidase activity having IC50 values ranging from 2.40 ± 0.10 to 31.40 ± 0.90 μM and for α-amylase having IC50 values ranging from 1.80 ± 0.05 to 27.60 ± 0.80 μM as compared t...

The current study was conducted to obtain hybrid analogues of indole-based thiadiazole derivatives (1–16) in which a number of reaction steps were involved. To examine their biological activity in the presence of the reference drug Donepezil (0.21 ± 0.12 and 0.30 ± 0.32 M, respectively), the inhibitory potentials of AChE and BuChE were determined f...

Herein, a library of novel pyridone derivatives 1-34 was designed, synthesized, and evaluated for α-amylase and α-glucosidase inhibitory as well as antioxidant activities. Pyridone derivatives 1-34 were synthesized via a one-pot multi-component reaction of variously substituted aromatic aldehydes, acetophenone, ethyl cyanoacetate, and ammonium acet...

Background: To discover novel lead molecules against diabetes, Alzheimer's disease and oxidative stress, a library of arylated pyrazole-fused pyran derivatives, 1-20, were synthesized in a one-pot reaction. Materials & methods: 1 H-NMR spectroscopic and electron ionization mass spectrometry techniques were used to characterize the synthetic hybrid...

The development of drugs resistance in diabetes mellitus is a growing clinical problem, creates many challenges for patient. To overcome these problems, there is a serious deficiency of antidiabetic agents, may be synthesized that inhibit alpha amylase and alpha glucosidase activity. Here, we have design and synthesized benzoxazole based sulphonami...

There is an excellent approach to design antidiabetic drugs based on inhibitors of α-glucosidase. These inhibitors control the sugar level in blood of diabetic patients to avoid complications on patient health. In current study we designed a new series of oxadiazole based derivatives (1–20). All synthesized analogues were characterized through ¹H-N...

Thiadiazole is a potential class of α-glucosidase, β-glucuronidase, and anti-leishmanial inhibitors. Our aim was to develop thiadiazole based dual inhibitors for urease glycation inhibition and (DDPH) scavenging activity. Pyridine-based-thiadiazole analogs (1-18) were synthesized and characterized through ¹H-NMR, ¹³C-NMR, EI-HRMS. All synthesized c...

Twenty-four analogues of benzimidazole-based thiazoles (1-24) were synthesized and assessed for their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory potential. All analogues were found to exhibit good inhibitory potential against cholinesterase enzymes, having IC50 values in the ranges of 0.10 ± 0.05 to 11.10 ± 0....

Several S-substituted-2-mercaptobenzimidazole derivatives 1–34 were synthesized by reacting 2-mercaptobenzimidazole with a variety of substituted benzyl bromide and characterized with the help of various spectroscopic techniques. All synthetic compounds were evaluated for urease inhibitory and DPPH radical scavenging activities. Compounds showed si...

A library of hydrazinyl thiazole-linked indenoquinoxaline hybrids 1–36 were synthesized via a multistep reaction scheme. All synthesized compounds were characterized by various spectroscopic techniques including EI-MS (electron ionization mass spectrometry) and ¹H NMR (nuclear magnetic resonance spectroscopy). Compounds 1–36 were evaluated for thei...

A widespread increase in people affected by diabetes mellitus (DM) has led to the development of new strategies to combat this disease. Targeting the activity of the α-amylase enzyme and preventing oxidative stress involved in the onset and progression of type 2 DM is considered to represent the most effective therapeutic strategy for treating meta...

A series of twenty bis ‐thiazolidinone based chalcone scaffolds (1‐20) were synthesized and characterized by using various spectroscopic tools such as HR‐EI‐MS, 1 HNMR, 13 CNMR and were screened in vitro for their AChE and BuChE inhibition profile. It was noteworthy, that all the synthetic analogues (except analogues 10, 12 and 1 4 , which are foun...

6‐Ethoxy‐2‐mercapto benzothiazole derivatives 1–26 were synthesized by following two different reaction schemes. Products 1–18 were synthesized by treating 6‐ethoxy‐2‐mercaptobenzothiazole with different phenacyl bromides whereas compounds 19–26 were prepared by the reaction of 6‐ethoxy‐2‐mercaptobenzothiazole with benzyl bromide derivatives under...

ZnCo2O4/Ag3PO4 heterostructure nanoparticles were prepared via a facile ultrasonic method and characterized using various techniques. The photocatalytic activity of ZnCo2O4/Ag3PO4 nanoparticles was investigated for the degradation of organic pollutants (methyl orange and bisphenol A) under visible-light irradiation. An enhanced photocatalytic effic...

Background: To find alternative molecules against Klebsiella pneumonia, Proteus mirabilis and methicillin-resistant Staphylococcus aureus, new enoxacin derivatives were synthesized and screened. Methods: All derivatives exhibited promising antibacterial activities as compared to standard enoxacin (2 μg/ml) and standard cefixime (82 μg/ml). Compound...

A two-step reaction method was used to synthesize a series of rhodanine-based Schiff bases (2–33) that were characterized using spectroscopic techniques. All compounds were assessed for α-amylase inhibitory and radical scavenging (DPPH and ABTS) activities. In comparison to the standard acarbose (IC50 = 9.08 ± 0.07 µM), all compounds demonstrated g...

This work has described the synthesis of novel class (1-25) of benzofuran based hydrazone. The hybrid scaffolds (1-25) of benzofuran based hydrazone were evaluated in vitro, for their urease inhibition. All the newly synthesized analogues (1-25) were found to illustrate moderate to good urease inhibitory profile ranging from 0.20 ± 0.01 to 36.20 ±...

Inhibition of α-glucosidase and α-amylase enzymes is one of the significant approaches in designing anti-diabetic drugs because of its role in decreasing the carbohydrate digestion. In the present study we designed a new series of benzofuran Schiff base and evaluated them for their inhibitory potentials against α-amylase and α-glucosidase enzymes....

This study presents applications of various Equation of State (EOS) models (including specifically, Peng-Robinson, Soave Redlich-Kwong, and Peng-Robinson-Stryjek-Vera), in the simulation of the process of removing nitrogen (N2) from the natural gas (pre-treated) on Aspen HYSYS v11 using the cryogenic distillation method. Different equations of stat...

In the present study, Indole-based-oxadiazole (1A-17A) compounds were successfully synthesized. The structures of all synthesized compounds were fully characterized by different sophisticated spectroscopic techniques such 1H NMR, 13C NMR, EI-MS and HREI-MS. Further, the synthesized compounds were explored to investigate their broad-spectrum antibac...

Background Anthranilic acid is an active compound with diverse biological activities such as anti-inflammatory, antineoplastic, anti-malarial and α-glucosidase inhibitory properties. It can also chelate transition metals to form complexes with applications as antipathogens, photoluminescent materials, corrosion inhibitors, and catalysts. Results A...

Diabetes mellitus is one of the most prevalent diseases nowadays. Several marketed drugs are available for the cure and treatment of diabetes, but there is still a dire need of introducing compatible drug molecules with lesser side effects. The current study is based on the synthesis of isatin thiazole derivatives 4–30 via the Hantzsch reaction. Th...

In the present study, twenty (20) structural variants of nitrofurazone were synthesized based on BIODS (Biology-oriented drug synthesis) approach. The structure elucidation of the synthetic molecules (1-20) was carried out using different spectroscopic techniques, and their α-glucosidase inhibitory activity was also determined. The synthetic molecu...

Oxadiazole-based-thiourea analogs (1–18) were synthesized and evaluated for their β-glucuronidase inhibitory activity. All analogs showed extensive β-glucuronidase inhibitory potential ranging between (IC50 = 2.20 ± 0.01 µM) to (IC50 = 52.25 ± 1.20 µM) by comparing with the standard D-Saccharic acid 1,4-lactone (IC50 = 48.30 ± 1.25 µM). Among the s...

We have synthesized benzo[d]oxazole derivatives (1–21) through a multistep reaction. Alteration in the structure of derivatives was brought in the last step via using various substituted aromatic aldehydes. In search of an anti-Alzheimer agent, all derivatives were evaluated against acetylcholinesterase and butyrylcholinesterase enzyme under positi...

New benzimidazole analogues (1–18) were synthesized and characterized through different spectroscopic techniques such as ¹H NMR, ¹³C NMR and HREI-MS. All analogues were screened for β-glucuronidase inhibitory potential. All analogues showed varied degree of inhibitory potentials with IC50 values ranging between 1.10 ± 0.10 to 39.60 ± 0.70 μM when c...

[This corrects the article DOI: 10.1021/acsomega.0c05581.].

Background & Introduction Antioxidants are known to prevent oxidative stress-induced damage to the biomolecules and thus, delay the onset of cancers and many age-related diseases. Therefore, the development of novel and potent antioxidants is justified. Method During this study, we synthesized symmetrical bis-Schiff bases of carbohydrazide 1-27, a...