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1.
Clin Case Rep ; 12(2): e8514, 2024 Feb.
Article in English | MEDLINE | ID: mdl-38344363

ABSTRACT

Porcelain aorta, characterized by extensive calcification of the aortic wall is often associated with coronary calcification. It can pose an increased risk of thromboembolic complications during interventional and surgical procedures. We present a case of a 52-year-old female, a chronic smoker with dyslipidemia with complaints of exertional chest pain for past 6 months. She was diagnosed as a case of non-ST elevation myocardial infarction (NSTEMI) with multivessel CAD, with porcelain aorta and calcified coronaries based on abnormal ECG, elevated troponin and coronary angiography findings. Percutaneous transluminal coronary angioplasty (PTCA) was the treatment modality chosen considering the risk of thromboembolism with aortic manipulation during coronary artery bypass grafting (CABG). Repeat ECG after the procedure showed resolution of ST segment depression. Her hospital stay was uneventful. She was discharged on dual antiplatelet therapy, statin and metoprolol. One-week follow-up revealed normal ECG and blood reports, with further outpatient department visits scheduled every 3 months. Porcelain aorta and coronary calcification is a challenging case for cardiologists. PTCA if done meticulously could be preferable to coronary-artery by-pass grafting (CABG) in such patients. Despite the risks like aortic rupture and thromboembolic complications, PTCA in a case of multivessel CAD with porcelain aorta and calcified coronaries could be a life-saving procedure.

2.
Oman Med J ; 32(6): 507-509, 2017 Nov.
Article in English | MEDLINE | ID: mdl-29218128

ABSTRACT

A ten-year-old boy presented to the hospital with body ache and joint pains for two months and headache, vomiting, and skin rash for three days. He was drowsy and lethargic at admission. Physical examination revealed bilateral papilledema. There were no cranial nerve involvement, neuromotor deficit, or signs of meningeal irritation. Computed tomography and magnetic resonance imaging of the brain did not reveal any evidence of cerebral edema or space occupying lesion. In view of the high endemicity of brucellosis in the area, Brucella agglutination test (BAT) was done at the time of admission and was negative. However, on the eighth day of admission, blood culture showed growth of Brucella melitensis. A repeat BAT at this time was strongly positive with a titer of 1:1 280. The initial one was negative due to prozone phenomenon caused by very high antibody titers. A diagnosis of neurobrucellosis with pseudotumor cerebri was made. He was treated with gentamicin, rifampicin, and septrin along with acetazolamide for raised intracranial pressure. The boy responded well to therapy and made a complete clinical recovery with resolution of papilledema. In areas endemic for brucellosis, a high index of suspicion for neurobrucellosis should be entertained in any child presenting with diverse neurological signs.

3.
Bioorg Med Chem Lett ; 17(5): 1443-6, 2007 Mar 01.
Article in English | MEDLINE | ID: mdl-17169555

ABSTRACT

4-[6-(2-Tertiaryaminoethyl)naphthalen-2-yl]benzonitriles are conformationally constrained histamine H3 receptor antagonists with high potency and selectivity. The analogs were designed around a naphthalene core, with the goal of enhancing lipophilicity and CNS penetration, as compared to a previously reported benzofuran series. The SAR of the tertiary amine moiety is similar to that reported for the benzofuran series, with analogs bearing a 2-methylpyrrolidine substituent possessing the greatest rat and human H3 receptor binding affinities.


Subject(s)
Central Nervous System/metabolism , Histamine Antagonists/chemical synthesis , Nitriles/chemical synthesis , Receptors, Histamine H3/drug effects , Animals , Histamine Antagonists/pharmacokinetics , Humans , Hydrophobic and Hydrophilic Interactions , Naphthalenes , Nitriles/pharmacokinetics , Permeability , Protein Binding , Rats , Receptors, Histamine H3/metabolism , Structure-Activity Relationship
4.
J Org Chem ; 68(8): 3238-40, 2003 Apr 18.
Article in English | MEDLINE | ID: mdl-12688796

ABSTRACT

A practical and scaleable synthesis of a novel nonsteroidal ligand for the glucocorticoid receptor A-224817.0 1A is described. The synthesis proceeds in seven steps starting from 1,3-dimethoxybenzene. The biaryl intermediate 5 was prepared by an optimized high-yielding and high-throughput Negishi protocol. The quinoline core 8 was constructed by using a modified Skraup reaction. The final product was obtained by a direct allylation reaction of lactol 10 with allyltrimethylsilane. The process was accomplished efficiently to produce 1A in 25% overall yield and >99% purity with simple and practical isolation and purification procedures.


Subject(s)
Combinatorial Chemistry Techniques , Heterocyclic Compounds, 2-Ring/chemical synthesis , Quinolines/chemical synthesis , Receptors, Glucocorticoid/metabolism , Catalysis , Heterocyclic Compounds, 2-Ring/analysis , Indicators and Reagents , Ligands , Molecular Structure , Quinolines/analysis , Stereoisomerism
6.
J Am Chem Soc ; 124(16): 4282-6, 2002 Apr 24.
Article in English | MEDLINE | ID: mdl-11960457

ABSTRACT

A new approach for atropselective preparation of axially chiral biaryl was developed. This process proceeded through a chirality transfer from a stereogenic center of a secondary alcohol to the stereogenic axis via regioselective intramolecular silyl group migration. This methodology allowed for the preparation of a single atropisomer 2 in good yield (85%) with high diastereoselectivity (99:1), which subsequently led to the successful development of an efficient asymmetric synthesis of A-240610.0, 1.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Glucocorticoids/chemical synthesis , Heterocyclic Compounds, 4 or More Rings/chemical synthesis , Stereoisomerism
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