《Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors》 was written by Patel, Manoj; Naidu, B. Narasimhulu; Dicker, Ira; Higley, Helen; Lin, Zeyu; Terry, Brian; Protack, Tricia; Krystal, Mark; Jenkins, Susan; Parker, Dawn; Panja, Chiradeep; Rampulla, Richard; Mathur, Arvind; Meanwell, Nicholas A.; Walker, Michael A.. Formula: C4H5ClO3This research focused ontricyclic pyrimidinone carboxamide preparation antiviral activity; Bridged tricyclic pyrimidinone; HIV; HIV Integrase; Integrase inhibitor; Strand transfer inhibitor. The article conveys some information:
The design, synthesis and structure-activity relationships associated with a series of bridged tricyclic pyrimidinone carboxamides I (R = (dimethylcarbamoyl)carbonyl, (dimethylcarbamoyl)methyl, [cyclopropyl(methyl)carbamoyl]carbonyl, etc.; R1 = H, 2-F, 3-CF3, 2-C(O)NHCH3, etc.) as potent inhibitors of HIV-1 integrase strand transfer are described. Structural modifications to these mols. were made in order to examine the effect on potency towards wild-type and clin.-relevant resistant viruses. The [3.2.2]-bridged tricyclic system I was identified as an advantageous chemotype, with representatives exhibiting excellent antiviral activity against both wild-type viruses and the G140S/Q148H resistant virus that arises in response to therapy with raltegravir and elvitegravir. After reading the article, we found that the author used Ethyl oxalyl monochloride(cas: 4755-77-5Formula: C4H5ClO3)
Ethyl oxalyl monochloride(cas: 4755-77-5) belongs to acyl chlorides. Lacking the ability to form hydrogen bonds, acyl chlorides have lower boiling and melting points than similar carboxylic acids. For example, acetic acid boils at 118 °C, whereas acetyl chloride boils at 51 °C. Like most carbonyl compounds, infrared spectroscopy reveals a band near 1750 cm−1.Formula: C4H5ClO3
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