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1.
Pharmaceuticals (Basel) ; 17(2)2024 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-38399403

RESUMO

This work describes the design and synthesis of three series of hybrids of thienopyrimidines and sulfonamides. Dihydrofolate reductase enzyme was selected as a target for the in-silico screening of the synthesized thienopyrimidine-sulfonamide hybrid as an antibacterial, while squalene epoxidase was selected as an antifungal target protein. All screened compounds showed promising binding affinity ranges, with perfect fitting not exceeding 1.9 Å. The synthesized compounds were tested for their antimicrobial activity using agar well diffusion and minimum inhibitory concentration tests against six bacterial strains in addition to two Candida strains. Compounds 8iii and 12ii showed varying degrees of inhibition against Staphylococcus aureus and Escherichia coli bacterial strains, whereas the best antifungal activity against Candida was displayed by compound 8iii. Compound 12ii, the cyclohexathienopyrimidine coupled with sulfadiazine at position 3, has the best antibacterial activity, which is consistent with molecular docking results at the active site of the oxidoreductase protein. Interestingly, compound 12ii also has the highest docking binding energy at the antifungal squalene epoxidase active site. Investigating the physicochemical properties of the synthesized hybrids revealed their high tolerability with cell membranes, and moderate to poor oral bioavailability, and that all are drug-like candidates, among which 4i, the cyclohexathieno[2,3-d] pyrimidine core with sulphaguanidine incorporated at position 4, recorded the best score (1.58).

2.
Cureus ; 15(11): e49219, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-38143616

RESUMO

Infective endocarditis (IE) refers to an infection of the endocardium that can be caused by bacteria, viruses, or fungi. It can manifest either acutely or sub-acutely. Which can be complicated to stroke and congestive heart failure. We report a case of IE caused by Streptococcus (S.) pluranimalium. It is a rare organism that was discovered in 1999 in infections affecting domestic animals. It can cause serious complications, such as brain abscesses, and IE in both humans and animals. Our patient was diagnosed with IE caused by S. pluranimalium based on modified Duke's criteria. After the diagnosis was made, the patient started on intravenous antibiotics according to the blood cultures. Then, the patient significantly improved. We are reporting this case because only a few cases were documented for infective endocarditis caused by S. pluranimalium.

3.
Cureus ; 15(12): e50489, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38226084

RESUMO

Rheumatoid arthritis (RA) is a systemic autoimmune disease that mainly affects the joints, which can lead to joint deformity. Since the disease is systemic, it affects many organs, including the heart, which can lead to pericarditis, coronary artery disease, and heart failure. We are reporting on a male patient, 34 years of age and Sudanese, who complained of shortness of breath and chest pain that started weeks before he came to the hospital, with no other associated symptoms. The patient was admitted to the hospital, and extensive work was done for the patient, which revealed that he had pericardial effusion secondary to RA, which is the first presentation of the disease. RA rarely presents as a first presentation with pericarditis and pericardial effusion. The patient was managed medically, and he showed significant improvement.

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