DESIGN AND SYNTHESIS OF NOVEL TERREMIDE AND SULFONAIDES DERIVATIVES FOR PHARMACOLOGICAL EVALUATION | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Article 7, Volume 66, Issue 2, September and October 2022, Pages 126-137 PDF (361.38 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ajps.2022.269244 | ||
| Authors | ||
| Ahmed Helal* ; Abdelrahman Hussien; Mohamed Elsebaei; Abdelrahman Mayhoub | ||
| Department of Pharmaceutical Organic Chemistry, College of Pharmacy(boys), Al-Azhar University, Cairo 11884, Egypt | ||
| Abstract | ||
| Bacterial infections were first recorded back at 3000 B.C.E. Since then, there have been an enormous number of pandemics that hit the world. Countless doctors and researchers have been working on a definitive solution to exterminate all bacterial infections of all kinds. Marine microorganisms have been widely used as a valid source for pharmacologically active components, and recently the amount of metabolites produced by marine-derived fungi have been increased magnificently, which provided not only wide spectrum of highly active compounds but also gave an enormous number of opportunities for chemists to modify theses incredible entities into more effective and less harmful compounds that can be used as cytotoxic, antiviral, antibacterial and antifungal agents.(He et al., 2013) Quinazolines have been spotted as a new group of agents of decent promising and potential chemotherapeutic and antimicrobial activities.(Raghavendra, Gurubasavarajaswamy, Nagaranavile, & Parameshwaran, 2009) The structure activity relationship of quinazolines has shown it has a very weak antimicrobial activity,(Alafeefy, 2009) Close inspection of the structure-activity-relationships (SAR) of quinazolines revealed important structural features necessary for their antimicrobial activity: a nitrogenous ring and a side chain. Quinazoline heterocyclic compounds have been used to synthesize compounds like terremide B to enhance the activity. Currently, advantageous moieties have been combined to generate new hybrid scaffolds of quinazoline with the objective of synthesizing new moieties enhancing the biological activity and drug-like properties. | ||
| Keywords | ||
| quinazoline; terremide B; MRSA; antimicrobial resistance; antitumor | ||
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