Sadia Naureen - Academia.edu (original) (raw)

Papers by Sadia Naureen

Research paper thumbnail of Four-Component, One-Pot Synthesis of Novel Conjugated Indole-Imidazole Derivatives

Iranian Journal of Chemistry & Chemical Engineering-international English Edition, Feb 1, 2019

A series of new tetrasubstituted imidazoles 2-phenyl-3-(1, 4, 5-triphenyl-1H-imidazol-2-yl)-1H-in... more A series of new tetrasubstituted imidazoles 2-phenyl-3-(1, 4, 5-triphenyl-1H-imidazol-2-yl)-1H-indole derivatives substituted with –F, Cl, Br, I,-OCH3 and -NHCOCH3 were synthesized using a multicomponent reaction. The compounds were obtained in good yields by easy workup and with high purity

Research paper thumbnail of CCDC 2017033: Experimental Crystal Structure Determination

Research paper thumbnail of CCDC 2017032: Experimental Crystal Structure Determination

Research paper thumbnail of Identification of Imidazolylpyrazole Ligands as Potent Urease Inhibitors: Synthesis, Antiurease Activity and In Silico Docking Studies

ChemistrySelect, 2020

Towards discovery of effective urease inhibitors; we disclose here a hybrid series of imidazole a... more Towards discovery of effective urease inhibitors; we disclose here a hybrid series of imidazole and pyrazole motifs as potent antiurease agents. A para-toluenesulfonic acid (TsOH) catalyzed, facile synthetic approach was employed for the preparation of targeted molecular designs in good yields upto 94 %. The novel scaffolds were characterized by different spectroscopic means (FTIR, NMR, and Mass spectrometry) and elemental analysis helped to identify the purity of these compounds. Afterwards, the derivatives was tested against Jack bean's urease enzyme to explore their inhibiting potencies. All analogues (4 a-4 l) were found active against the studied enzyme in comparison with the standard drug thiourea (IC 50 = 21.26 � 0.12 μM). However, following dibromo substituted derivatives: 4 f, 4 g, 4 h, 4 i, 4 j, 4 k, and 4 l were surfaced out as potent urease inhibitors among the series. The identified lead candidates were meta-nitro substituted 4 k with IC 50 = 0.7 � 0.002 μM and a para-nitro containing compound 4 l with IC 50 = 1.0 � 0.003 μM. As observed in docking calculations, ionic and hydrogen bonding, π-stacking, interaction with nickel ions and other hydrophobic interactions probably stabilized the ligand bindings at the active site of urease.

Research paper thumbnail of Synthesis and in vitro cholinesterase inhibitory potential of dihydropyridine derivatives

Pakistan journal of pharmaceutical sciences, 2019

Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vi... more Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vitro cholinesterases (AChE, BChE) inhibitory activity. All compounds showed potent activity with IC50 values between 0.21±0.003 to 147.14±0.12μM for AChE and among them five compounds showed potent activity with IC50 values 17.16±0.02 to 231.6±0.12μM for BChE when compared with standard Eserine (IC50 = 0.85±0.0001 μM (AChE) & 0.04±0.0001μM (BChE). The most potent compound 11 can be considered as potential lead compound showed an inhibition of 95.35±0.11 and IC50= 0.21±0.003 while compound 7 showed an inhibition of 83.45±0.13 and IC50= 17.16±0.02. It is concluded from structural activity relationship that the presence of nitro group at C-2 and C-4 position of dihydropyridine ring increase the acetyl cholinesterase and butyrylcholinesterase activities of these compounds while presence of -Br and -Cl also enhances the activities.

Research paper thumbnail of On Efficient Synthesis, X‐Ray Analysis and DPPH Radical Scavenging Activity of Pyrazolone‐Based trans ‐Chalcones

ChemistrySelect, 2019

The present work highlights the facile and substantially streamlined microwave assisted synthesis... more The present work highlights the facile and substantially streamlined microwave assisted synthesis of chalcones 3(a-m) from acetylpyrazolone 1 a and aldehyde 2(a-m) in piperidineethanolic medium. The organocatalytic action of piperidine has been proposed in a mechanism. Different physical and analytical methods have been used to characterize the synthesized chalcones. Single Crystal XRD analyses of compounds 3 e and 3 f also supported proposed interpretation of the structural arrangements of these molecules. Further the synthesized compounds were evaluated for DPPH activity and results were compared with standard quercetin. Following compounds; 3 h, 3 i, 3 j and 3 d articulated excellent antioxidant activity.

Research paper thumbnail of Evaluation of α-glucosidase inhibiting potentials with docking calculations of synthesized arylidene-pyrazolones

Bioorganic chemistry, Apr 10, 2018

Herein, condensation of aryl(hetaryl)pyrazole-4-carbaldehydes 1(a-c) with substituted pyrazolones... more Herein, condensation of aryl(hetaryl)pyrazole-4-carbaldehydes 1(a-c) with substituted pyrazolones 2(a-d) lead to the corresponding arylidene-pyrazolones 3(a-l) which were tested against α-glucosidase enzyme. The synthesized compounds displayed moderate to good activity. Among these, a coumarin derivative 3k exhibited excellent results (IC2.10 ± 0.004 µM) in comparison to clinical drug acarbose (IC37.38 ± 0.12 µM). The ligand-protein interactions were identified through docking and stabilizing energy calculations.

Research paper thumbnail of Synthesis of Tetrasubstitutd Imidazoles Containing Indole and Their Antiurease and Antioxidant Activities

Journal of the Chilean Chemical Society, 2017

Indole-based tetraarylimidazoles were prepared by multicomponent reaction of substituted 2-arylin... more Indole-based tetraarylimidazoles were prepared by multicomponent reaction of substituted 2-arylindole-3-carbaldehydes, benzil, substituted anilines and ammonium acetate in acetic acid. The new compounds were evaluated for their antiurease and antioxidant activity. The synthesized compounds exhibited potent antiurease activity.

Research paper thumbnail of In search of new α -glucosidase inhibitors: Imidazolylpyrazole derivatives

Bioorganic Chemistry, 2017

In search of new α-glucosidase inhibitors: Imidazolylpyrazole derivatives

Research paper thumbnail of Amino acid catalyzed reactions. A facile route to some heteroarylbispyrazoles

Synthetic Communications, 2017

ABSTRACT This newly designed route assembled a pyrazole ring with an aldehydic functionality over... more ABSTRACT This newly designed route assembled a pyrazole ring with an aldehydic functionality over another pyrazole moiety. Further, formyl group was exploited in different routes such as condensation reactions, imidazole and pyrimidone/thione synthesis. The present reactions were performed with glycine, a facile catalyst, and the results were compared well with those of conventional methods. GRAPHICAL ABSTRACT

Research paper thumbnail of Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity

European Journal of Medicinal Chemistry, 2015

A series of tetraarylimidazoles (5A-5O) were prepared by one pot four component condensation reac... more A series of tetraarylimidazoles (5A-5O) were prepared by one pot four component condensation reactions of 2-arylindole-3-carbaldehydes, substituted anilines, benzil and ammonium acetate in acetic acid. The synthesized compounds exhibited potent antiurease activity with IC 50 values ranging from 0.12±0.06 µM to 29.12±0.18 µM as compared with thiourea. However, low inhibition profiles were observed for lipoxygenase. The data show that tetraarylimidazoles containing a substituted 2-penylindole have emerged as a new class of potent inhibitors of urease enzyme.

Research paper thumbnail of Triarylimidazoles-synthesis of 3-(4,5-diaryl-1H-imidazol-2-yl)-2-phenyl-1H-indole derivatives as potent α-glucosidase inhibitors

Medicinal Chemistry Research, 2014

A series of new trisubstituted imidazoles-3-(4,5-diaryl-1H-imidazol-2-yl)-2-phenyl-1H-indole deri... more A series of new trisubstituted imidazoles-3-(4,5-diaryl-1H-imidazol-2-yl)-2-phenyl-1H-indole derivatives (2a-2u) were synthesized and evaluated for their aglucosidase inhibition. The new compounds showed significant a-glucosidase inhibitory activity as compared to the standard inhibitor acrabose. Structures of synthesized compounds were determined using FT-IR, Mass spectrometry, 1 H NMR, 13 C NMR, and elemental analyses.

Research paper thumbnail of Facile, eco-friendly, one-pot protocol for the synthesis of indole-imidazole derivatives catalyzed by amino acids

Synthetic Communications, 2017

An Efficient, convenient green approach for the synthesis of Indole-based2,4,5trisubstituted and ... more An Efficient, convenient green approach for the synthesis of Indole-based2,4,5trisubstituted and 1,2,4,5-tetra substituted imidazoles by multicomponent reaction of substituted 2-arylindole-3-carbaldehydes, benzil, substituted anilines and ammonium acetate using catalytic aminoacid (Glycine) in ethanol is described. Several amino acids have also been evaluated as organic catalysts for these reactions. The structures of the compounds have been established on the basis of infrared, mass and 1H NMR spectral data. The mild reaction conditions, inexpensive / economical reagents and good yield show the usefulness of this approach.

Research paper thumbnail of Biological evaluation of new imidazole derivatives tethered with indole moiety as potent α-glucosidase inhibitors

Bioorganic chemistry, Feb 1, 2018

A series of triarylimidazoles substituted with 2-arylindoles (4a-4j) were prepared and evaluated ... more A series of triarylimidazoles substituted with 2-arylindoles (4a-4j) were prepared and evaluated for their in vitro α-Glucosidase inhibition. α-Glucosidase inhibition assay displayed a new class of highly potent agents The new compounds showed significant α-glucosidase inhibitory activity as compared to the standard inhibitor acrabose. Structures of synthesized compounds were determined by using Mass spectrometry FT-IR,H NMR andC NMR.

Research paper thumbnail of Four-Component, One-Pot Synthesis of Novel Conjugated Indole-Imidazole Derivatives

Iranian Journal of Chemistry & Chemical Engineering-international English Edition, Feb 1, 2019

A series of new tetrasubstituted imidazoles 2-phenyl-3-(1, 4, 5-triphenyl-1H-imidazol-2-yl)-1H-in... more A series of new tetrasubstituted imidazoles 2-phenyl-3-(1, 4, 5-triphenyl-1H-imidazol-2-yl)-1H-indole derivatives substituted with –F, Cl, Br, I,-OCH3 and -NHCOCH3 were synthesized using a multicomponent reaction. The compounds were obtained in good yields by easy workup and with high purity

Research paper thumbnail of CCDC 2017033: Experimental Crystal Structure Determination

Research paper thumbnail of CCDC 2017032: Experimental Crystal Structure Determination

Research paper thumbnail of Identification of Imidazolylpyrazole Ligands as Potent Urease Inhibitors: Synthesis, Antiurease Activity and In Silico Docking Studies

ChemistrySelect, 2020

Towards discovery of effective urease inhibitors; we disclose here a hybrid series of imidazole a... more Towards discovery of effective urease inhibitors; we disclose here a hybrid series of imidazole and pyrazole motifs as potent antiurease agents. A para-toluenesulfonic acid (TsOH) catalyzed, facile synthetic approach was employed for the preparation of targeted molecular designs in good yields upto 94 %. The novel scaffolds were characterized by different spectroscopic means (FTIR, NMR, and Mass spectrometry) and elemental analysis helped to identify the purity of these compounds. Afterwards, the derivatives was tested against Jack bean's urease enzyme to explore their inhibiting potencies. All analogues (4 a-4 l) were found active against the studied enzyme in comparison with the standard drug thiourea (IC 50 = 21.26 � 0.12 μM). However, following dibromo substituted derivatives: 4 f, 4 g, 4 h, 4 i, 4 j, 4 k, and 4 l were surfaced out as potent urease inhibitors among the series. The identified lead candidates were meta-nitro substituted 4 k with IC 50 = 0.7 � 0.002 μM and a para-nitro containing compound 4 l with IC 50 = 1.0 � 0.003 μM. As observed in docking calculations, ionic and hydrogen bonding, π-stacking, interaction with nickel ions and other hydrophobic interactions probably stabilized the ligand bindings at the active site of urease.

Research paper thumbnail of Synthesis and in vitro cholinesterase inhibitory potential of dihydropyridine derivatives

Pakistan journal of pharmaceutical sciences, 2019

Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vi... more Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vitro cholinesterases (AChE, BChE) inhibitory activity. All compounds showed potent activity with IC50 values between 0.21±0.003 to 147.14±0.12μM for AChE and among them five compounds showed potent activity with IC50 values 17.16±0.02 to 231.6±0.12μM for BChE when compared with standard Eserine (IC50 = 0.85±0.0001 μM (AChE) & 0.04±0.0001μM (BChE). The most potent compound 11 can be considered as potential lead compound showed an inhibition of 95.35±0.11 and IC50= 0.21±0.003 while compound 7 showed an inhibition of 83.45±0.13 and IC50= 17.16±0.02. It is concluded from structural activity relationship that the presence of nitro group at C-2 and C-4 position of dihydropyridine ring increase the acetyl cholinesterase and butyrylcholinesterase activities of these compounds while presence of -Br and -Cl also enhances the activities.

Research paper thumbnail of On Efficient Synthesis, X‐Ray Analysis and DPPH Radical Scavenging Activity of Pyrazolone‐Based trans ‐Chalcones

ChemistrySelect, 2019

The present work highlights the facile and substantially streamlined microwave assisted synthesis... more The present work highlights the facile and substantially streamlined microwave assisted synthesis of chalcones 3(a-m) from acetylpyrazolone 1 a and aldehyde 2(a-m) in piperidineethanolic medium. The organocatalytic action of piperidine has been proposed in a mechanism. Different physical and analytical methods have been used to characterize the synthesized chalcones. Single Crystal XRD analyses of compounds 3 e and 3 f also supported proposed interpretation of the structural arrangements of these molecules. Further the synthesized compounds were evaluated for DPPH activity and results were compared with standard quercetin. Following compounds; 3 h, 3 i, 3 j and 3 d articulated excellent antioxidant activity.

Research paper thumbnail of Evaluation of α-glucosidase inhibiting potentials with docking calculations of synthesized arylidene-pyrazolones

Bioorganic chemistry, Apr 10, 2018

Herein, condensation of aryl(hetaryl)pyrazole-4-carbaldehydes 1(a-c) with substituted pyrazolones... more Herein, condensation of aryl(hetaryl)pyrazole-4-carbaldehydes 1(a-c) with substituted pyrazolones 2(a-d) lead to the corresponding arylidene-pyrazolones 3(a-l) which were tested against α-glucosidase enzyme. The synthesized compounds displayed moderate to good activity. Among these, a coumarin derivative 3k exhibited excellent results (IC2.10 ± 0.004 µM) in comparison to clinical drug acarbose (IC37.38 ± 0.12 µM). The ligand-protein interactions were identified through docking and stabilizing energy calculations.

Research paper thumbnail of Synthesis of Tetrasubstitutd Imidazoles Containing Indole and Their Antiurease and Antioxidant Activities

Journal of the Chilean Chemical Society, 2017

Indole-based tetraarylimidazoles were prepared by multicomponent reaction of substituted 2-arylin... more Indole-based tetraarylimidazoles were prepared by multicomponent reaction of substituted 2-arylindole-3-carbaldehydes, benzil, substituted anilines and ammonium acetate in acetic acid. The new compounds were evaluated for their antiurease and antioxidant activity. The synthesized compounds exhibited potent antiurease activity.

Research paper thumbnail of In search of new α -glucosidase inhibitors: Imidazolylpyrazole derivatives

Bioorganic Chemistry, 2017

In search of new α-glucosidase inhibitors: Imidazolylpyrazole derivatives

Research paper thumbnail of Amino acid catalyzed reactions. A facile route to some heteroarylbispyrazoles

Synthetic Communications, 2017

ABSTRACT This newly designed route assembled a pyrazole ring with an aldehydic functionality over... more ABSTRACT This newly designed route assembled a pyrazole ring with an aldehydic functionality over another pyrazole moiety. Further, formyl group was exploited in different routes such as condensation reactions, imidazole and pyrimidone/thione synthesis. The present reactions were performed with glycine, a facile catalyst, and the results were compared well with those of conventional methods. GRAPHICAL ABSTRACT

Research paper thumbnail of Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity

European Journal of Medicinal Chemistry, 2015

A series of tetraarylimidazoles (5A-5O) were prepared by one pot four component condensation reac... more A series of tetraarylimidazoles (5A-5O) were prepared by one pot four component condensation reactions of 2-arylindole-3-carbaldehydes, substituted anilines, benzil and ammonium acetate in acetic acid. The synthesized compounds exhibited potent antiurease activity with IC 50 values ranging from 0.12±0.06 µM to 29.12±0.18 µM as compared with thiourea. However, low inhibition profiles were observed for lipoxygenase. The data show that tetraarylimidazoles containing a substituted 2-penylindole have emerged as a new class of potent inhibitors of urease enzyme.

Research paper thumbnail of Triarylimidazoles-synthesis of 3-(4,5-diaryl-1H-imidazol-2-yl)-2-phenyl-1H-indole derivatives as potent α-glucosidase inhibitors

Medicinal Chemistry Research, 2014

A series of new trisubstituted imidazoles-3-(4,5-diaryl-1H-imidazol-2-yl)-2-phenyl-1H-indole deri... more A series of new trisubstituted imidazoles-3-(4,5-diaryl-1H-imidazol-2-yl)-2-phenyl-1H-indole derivatives (2a-2u) were synthesized and evaluated for their aglucosidase inhibition. The new compounds showed significant a-glucosidase inhibitory activity as compared to the standard inhibitor acrabose. Structures of synthesized compounds were determined using FT-IR, Mass spectrometry, 1 H NMR, 13 C NMR, and elemental analyses.

Research paper thumbnail of Facile, eco-friendly, one-pot protocol for the synthesis of indole-imidazole derivatives catalyzed by amino acids

Synthetic Communications, 2017

An Efficient, convenient green approach for the synthesis of Indole-based2,4,5trisubstituted and ... more An Efficient, convenient green approach for the synthesis of Indole-based2,4,5trisubstituted and 1,2,4,5-tetra substituted imidazoles by multicomponent reaction of substituted 2-arylindole-3-carbaldehydes, benzil, substituted anilines and ammonium acetate using catalytic aminoacid (Glycine) in ethanol is described. Several amino acids have also been evaluated as organic catalysts for these reactions. The structures of the compounds have been established on the basis of infrared, mass and 1H NMR spectral data. The mild reaction conditions, inexpensive / economical reagents and good yield show the usefulness of this approach.

Research paper thumbnail of Biological evaluation of new imidazole derivatives tethered with indole moiety as potent α-glucosidase inhibitors

Bioorganic chemistry, Feb 1, 2018

A series of triarylimidazoles substituted with 2-arylindoles (4a-4j) were prepared and evaluated ... more A series of triarylimidazoles substituted with 2-arylindoles (4a-4j) were prepared and evaluated for their in vitro α-Glucosidase inhibition. α-Glucosidase inhibition assay displayed a new class of highly potent agents The new compounds showed significant α-glucosidase inhibitory activity as compared to the standard inhibitor acrabose. Structures of synthesized compounds were determined by using Mass spectrometry FT-IR,H NMR andC NMR.