The importance of sulfur-containing motifs in drug design and discovery

Sulfondiimines: synthesis, derivatisation and application

“…As already pointed out, sulfones and sulfonamides are widely present in pharmaceuticals and agrochemicals. 1 As a result, replacements of these moieties have become powerful tools for the fine-tuning of pharmacological profiles. 50 Consequently, this concept has also been applied for hexavalent sulfur compounds and was included in drug development programs in pharmaceutical industry.…”

“…A literature survey focusing on sulfur-containing drugs revealed that sulfones 1 and sulfonamides 2 cover more than 30% of all drugs approved by the Food and Drug Administration (FDA) in the United States. 1 In contrast, only a few attempts to apply their aza-analogues sulfoximines 3 , sulfonimidamides 4 , and sulfondiimines 5 have been reported, 2 with the latter being the least explored compound class (Fig. 1).…”

New Opportunities for the Utilization of the Sulfoximine Group in Medicinal Chemistry from the Drug Designer's Perspective**

“…Sulfur‐based functional groups offer drug designers an exceptional structural diversity [1] . While sulfonamides 5 in particular, and to a lesser extent sulfones 2 and sulfoxides 1 (Figure 1), are found in many approved drugs, [1,2] a large variety of sulfur‐based functional groups has historically been neglected in drug discovery [3] .…”

“…Sulfur‐based functional groups offer drug designers an exceptional structural diversity [1] . While sulfonamides 5 in particular, and to a lesser extent sulfones 2 and sulfoxides 1 (Figure 1), are found in many approved drugs, [1,2] a large variety of sulfur‐based functional groups has historically been neglected in drug discovery [3] . However, in recent years underexplored functional groups such as sulfoximines 3 , [3b,4] sulfondiimines 4 , [3b] sulfonimidamides 6 , [3b,5] sulfondiimidamides 7 [6] and sulfur fluorides like the pentafluorosulfanyl group (SF 5 ) 8 [7] have started to attract an increasing interest from drug designers.…”

Sulfoximines in Medicinal Chemistry: Emerging Trends and Opportunities from the Drug Designer’s Perspective

“…Sulfur-based functional groups offer drug designers an exceptional structural diversity. [1] While sulfonamides 5 in particular, and to a lesser extent sulfones 2 and sulfoxides 1 (Figure 1), are found in many approved drugs, [1,2] a large variety of sulfur-based functional groups has historically been neglected in drug discovery. However, in recent years underexplored functional groups such as sulfoximines 3, [3] sulfondiimines 4, [3b] sulfonimidamides 6, [3b,4] sulfondiimidamides 7 [5] and sulfur fluorides like the pentafluorosulfanyl group (SF5) 8 [6] have started to attract an increasing interest from drug designers.…”