Syntheses of new difluoromethylene benzoxazole and 1,2,4-oxadiazole derivatives, as potent non-nucleoside HIV-1 reverse transcriptase inhibitors

Oxadiazoles

“…13.3.6 1,2,4-Oxadiazoles in Medicine 1,2,4-Oxadiazole ring occurs widely in biologically active synthetic compounds, and is often used in drug discovery as a hydrolysis-resisting bioisosteric replacement for amide or ester functionalities [283] because of its electronic properties. Its derivatives can be found in a vast number of compounds exerting biological activity, such as ligands of benzodiazepine receptors [284,285], anti-inflammatory agents [131,199,234], antiviral agents [283], inhibitors of protein tyrosine phosphatases [286], agonists of muscarinic receptors [287], inhibitors of Src SH2 [183], antagonists of histamine H 3 -receptors [288], integrin receptor antagonists [200], angiotensin II receptor antagonists [289], and HIV-1 reverse transcriptase inhibitors [290]. 1,2,4-Oxadiazole moieties have been used in the design of dipeptidomimetics as peptide building blocks [184a,b].…”

Synthesis of new fluorine-containing pyrazolo[3,4-b]pyridinones as promising drug precursors

“…The bond lengths in sulf oxide 10a are close to those in structure 10b. The C (15) and C(16) atoms (1 -x, 1 -у, -z) are linked by a short ened intermolecular π-π contact. The molecules form helical chains along the axis b, which are held together by intermolecular hydrogen bonds, thereby producing the mo lecular packing (see Table 6).…”

“…10 In particular, this frag ment is thought to be an isopolar and isosteric substitute for oxygen. 11 Some CF 2 containing compounds exhibit high physiological activity, 12 including antitumor 13 and antifungal effects 14 and inhibition of HIV 1 reverse tran scriptase 15 and various protein kinases. 16 Thus, develop ment of synthetic routes to compounds with functional ized fragments CF 2 is an important step in searching for novel biologically active molecules.…”

Conjugates with an Antimicrobial Effect Based on New Derivatives of Mercaptobenzoxazole Esterified onto Poly(maleic anhydride‐alt‐vinyl acetate)

“…Also, it is used in treating cognitive dysfunctions, disorders of the central nervous system , Alzheimer's , schizophrenia (derivatives of benzoxazolyl‐2[benzyl‐1‐carboxylated piperazine] ), HIV , and inflammatory and neurodegenerative diseases (derivatives of N ‐aryl and N ‐alkyl‐2‐aminobenzoxazole , 2‐(1,2‐difluoro‐2‐metoxy‐2‐phenyl‐ethyl) benzoxazole , and 2‐(benzoxazole‐2‐yl)‐2,2 difluoro‐1‐ pyridine‐3‐ylethyl‐3‐(trifluoromethyl)benzoate and derivatives of 6,8‐dichloro[1,2,4]triazolo[3,4‐b][1,3]benzoxazol‐3(2H)‐thione that also have antioxidative and anthelmintic activity, respectively) .…”