Search engine for discovering works of Art, research articles, and books related to Art and Culture
Javascript must be enabled to continue!
Synthesis, Characterization, Molecular Docking Studies and Biological Evaluation of Some Conjugated Quinazoline‐Sulfonamide Scaffold
View through CrossRef
Abstract
A series of sulfonamides containing 4‐aminoquinazoline scaffolds
7 a‐7 l
was synthesized, characterized and evaluated for their in vitro antitubercular, antimicrobial and anticancer activity. The compounds with 4‐nitrophenyl (
7 c
), 3‐trifluoromethylphenyl (
7 f
) and 5‐chloro‐pyridin‐2‐yl (
7 h
) derivatives have shown potent antitubercular activity against
Mycobacterium tuberculosi
s
H37Rv
strain and the activity was two‐fold higher than the standard drug Ciprofloxacin. The compounds with 4‐chlorophenyl (
7 a
), pyridin‐2‐yl (
7 g
), 5‐chloro‐pyridin‐2‐yl (
7 h
) and pyrimidin‐2‐yl (
7 i
,
7 j
and
7 k
) derivatives were observed as excellent antimicrobial agents. The preliminary toxicity of selected potent compounds was also tested on Red Blood Cells by hemolytic assay and found to be non‐toxic even at higher concentrations. Compounds with 4‐nitrophenyl (
7 c)
and 4‐fluorophenyl (
7 e)
substitutions emerged as potent molecules against MDA‐MB‐231 cell line. ADME (A
bsorption, Distribution, Metabolism and Excretion
) screening study revealed that the compounds are strong candidates for antitubercular activity with good ADME parameters. In addition, the structure and antitubercular activity relationship were further supported by molecular docking studies of the active compounds against the DNA topoisomerase II (5BTC) enzyme of
M. tuberculosis
.
Title: Synthesis, Characterization, Molecular Docking Studies and Biological Evaluation of Some Conjugated Quinazoline‐Sulfonamide Scaffold
Description:
Abstract
A series of sulfonamides containing 4‐aminoquinazoline scaffolds
7 a‐7 l
was synthesized, characterized and evaluated for their in vitro antitubercular, antimicrobial and anticancer activity.
The compounds with 4‐nitrophenyl (
7 c
), 3‐trifluoromethylphenyl (
7 f
) and 5‐chloro‐pyridin‐2‐yl (
7 h
) derivatives have shown potent antitubercular activity against
Mycobacterium tuberculosi
s
H37Rv
strain and the activity was two‐fold higher than the standard drug Ciprofloxacin.
The compounds with 4‐chlorophenyl (
7 a
), pyridin‐2‐yl (
7 g
), 5‐chloro‐pyridin‐2‐yl (
7 h
) and pyrimidin‐2‐yl (
7 i
,
7 j
and
7 k
) derivatives were observed as excellent antimicrobial agents.
The preliminary toxicity of selected potent compounds was also tested on Red Blood Cells by hemolytic assay and found to be non‐toxic even at higher concentrations.
Compounds with 4‐nitrophenyl (
7 c)
and 4‐fluorophenyl (
7 e)
substitutions emerged as potent molecules against MDA‐MB‐231 cell line.
ADME (A
bsorption, Distribution, Metabolism and Excretion
) screening study revealed that the compounds are strong candidates for antitubercular activity with good ADME parameters.
In addition, the structure and antitubercular activity relationship were further supported by molecular docking studies of the active compounds against the DNA topoisomerase II (5BTC) enzyme of
M.
tuberculosis
.
Related Results
Sulfonamide Allergies
Sulfonamide Allergies
As one of the earliest developed antimicrobial classes, sulfonamides remain important therapeutic options for the empiric and definitive treatment of various infectious diseases. I...
Triazoloquinazoline: Synthetic Strategies and Medicinal Importance
Triazoloquinazoline: Synthetic Strategies and Medicinal Importance
Triazoloquinazoline is a fused heterocyclic nucleus, formed by the fusion of two fundamental heterocyclic moieties; triazole and quinazoline. This class of compound is known for it...
Synthesis and Investigation into Apatite-forming Ability of Hydroxyapatite/Chitosan-based Scaffold
Synthesis and Investigation into Apatite-forming Ability of Hydroxyapatite/Chitosan-based Scaffold
In this study, porous scaffolds were fabricated using inorganic material-hydroxyapatite and chitosan for bone-tissue engineering. The combination of hydroxyapatite and chitosan may...
DTMol: Pocket-based Molecular Docking using Diffusion Transformers
DTMol: Pocket-based Molecular Docking using Diffusion Transformers
Abstract
In computational chemistry, molecular docking—predicting the binding structure of a small molecule ligand to a protein—is vital for understanding interacti...
Biomimetic gradient scaffold of collagen–hydroxyapatite for osteochondral regeneration
Biomimetic gradient scaffold of collagen–hydroxyapatite for osteochondral regeneration
Osteochondral defects remain a major clinical challenge mainly due to the combined damage to the articular cartilage and the underlying bone, and the interface between the two tiss...
Development of a polymer/ceramic composite scaffold for bone tissue engineering
Development of a polymer/ceramic composite scaffold for bone tissue engineering
The current gold standard for traumatic bone injury is autograft. Harvesting this graft material requires additional surgery, leading to potential complications and added pain and ...
Sulfonamides in Drug Discovery: A Review of Synthetic Approaches and
Biological Activities
Sulfonamides in Drug Discovery: A Review of Synthetic Approaches and
Biological Activities
Sulfonamides represent one of the most versatile scaffolds in medicinal chemistry. Since
their introduction as the first synthetic antibacterial agents in the 1930s, the sulfonamid...
Recent Advances in Biological Active Sulfonamide based Hybrid
Compounds Part C: Multicomponent Sulfonamide Hybrids
Recent Advances in Biological Active Sulfonamide based Hybrid
Compounds Part C: Multicomponent Sulfonamide Hybrids
Abstract:
Sulfonamides, with the general formula R-SO2NR1R2, have attracted great attention
since the early discovery of sulfonamide-containing antibacterial drugs. The combination...