Azole Amide Analogues as Antibacterial Agents Against Methicillin‐Resistant <i>Staphylococcus aureus</i> and Its Structure‐Activity Relationship Studies

Methicillin-resistant Staphylococcus aureus (MRSA) is a well-known cause of serious skin and soft tissue infections, representing a significant global public health threat. The rapid development of MRSA resistance to all known antibiotics is the biggest concern. Therefore generating new anti-MRSA agents is the need of the present hour. Azoles combined with amides are well-known structures for developing compounds that exhibit antimicrobial effects against MRSA. Molecular hybridization, which involves combining various heterocyclic pharmacophores into a single molecular hybrid, offers a promising way for creating new antibacterial agents. In view of this, numerous attempts were made to incorporate various heterocyclic systems into azole nucleus bearing amide groups, which were then tested for antibacterial activity. This review outlines the advancements made over the past ten years regarding azole amide derivatives that exhibit extensive antibacterial properties against various MRSA strains. Specifically, we focused on the antibacterial property of structurally diverse azole analogues, such as thiazole, imidazole, oxadiazole, triazole, and pyrazole amides against MRSA and examined structure-activity relationship (SAR) studies.

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Journal
Drug Development Research
Published
2026-02-09
DOI
https://doi.org/10.1002/ddr.70242
Primary Topic
Synthesis and biological activity
Type
article
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article

Azole Amide Analogues as Antibacterial Agents Against Methicillin‐Resistant Staphylococcus aureus and Its Structure‐Activity Relationship Studies

K.P. Rakesh, Saraswati Sharma, Man Vir Singh, Rameshwari Verma et al.
Drug Development Research
Synthesis and biological activity
article

Azole Amide Analogues as Antibacterial Agents Against Methicillin‐Resistant Staphylococcus aureus and Its Structure‐Activity Relationship Studies

K.P. Rakesh, Saraswati Sharma, Man Vir Singh, Rameshwari Verma, Santosh Kumar Verma, Kothanahally S Sharath Kumar, Divakara S, Piyush Kumar Thakur
article en

Abstract

Methicillin-resistant Staphylococcus aureus (MRSA) is a well-known cause of serious skin and soft tissue infections, representing a significant global public health threat. The rapid development of MRSA resistance to all known antibiotics is the biggest concern. Therefore generating new anti-MRSA agents is the need of the present hour. Azoles combined with amides are well-known structures for developing compounds that exhibit antimicrobial effects against MRSA. Molecular hybridization, which involves combining various heterocyclic pharmacophores into a single molecular hybrid, offers a promising way for creating new antibacterial agents. In view of this, numerous attempts were made to incorporate various heterocyclic systems into azole nucleus bearing amide groups, which were then tested for antibacterial activity. This review outlines the advancements made over the past ten years regarding azole amide derivatives that exhibit extensive antibacterial properties against various MRSA strains. Specifically, we focused on the antibacterial property of structurally diverse azole analogues, such as thiazole, imidazole, oxadiazole, triazole, and pyrazole amides against MRSA and examined structure-activity relationship (SAR) studies.

Drug Development ResearchVol. 87(2)
University of North Carolina at Chapel Hill (US), University of Mysore (IN), Uttaranchal University (IN), Chhattisgarh Council of Science and Technology (IN), Yulin University (CN), Visvesvaraya Technological University (IN), Institute of Chartered Financial Analysts of India (IN)
Partnerships for the goals
Openalex Percentile: Top 61%
Synthesis and biological activity
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Azole Amide Analogues as Antibacterial Agents Against Methicillin‐Resistant <i>Staphylococcus aureus</i> and Its Structure‐Activity Relationship Studies — K.P. Rakesh, Saraswati Sharma, et al. · Drug Development Research (2026) | TGRS Research Map | TGRS