Synthesis, Structure and in Vitro Anti-Human Immunodeficiency virus Activity of Novel 3-Methyl-1H,3H-Thiazolo[3,4-a]Benzimidazoles

Chimirri, Alba; Grasso, Silvana; Monforte, Anna Maria; Monforte, P; Rao, Angela; Zappalà, Maria; Bruno, G.; Nicolò, Francesco; Pannecouque, Christophe; Witvrouw, Myriam; Clercq, Erik De

doi:10.1177/095632029800900507

Cited by 28 publications

(8 citation statements)

References 14 publications

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“…2). It was also evidenced by the extensive structural modifications on TBZ derivatives [15][16][17][18][19][20][21][22][23] (Fig. 3) that specific requirements existed in respect of the determining factors for an optimal anti-HIV potency.…”

Section: The Discovery Of the 23-diaryl-13-thia-zolidin-4-ones As Hmentioning

confidence: 98%

Recent Advances in the Research of 2,3-Diaryl-1,3-thiazolidin-4-one Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

Tian

Zhan²,

Rai³

et al. 2012

CMC

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Derived from the structure of 1H,3H-thiazolo[3,4-a]benzimidazoles (TBZs), 2,3-diaryl-1,3-thiazolidin-4-one derivatives became a novel class of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Under the guidance of continuous structure-activity relationship (SAR) analysis and molecular modeling, various structural modifications were carried out on nearly all the positions of the thiazolidin-4-one nucleus. Some of the derivatives proved to be highly effective against HIV-1 replication at 10-40 nanomolar concentration ranges with minimal cytotoxicities. In this article, the whole development of 2,3-diaryl-1,3-thiazolidin-4-one series from the discoveries to recent advances, their panoramic SAR studies and binding modes based on molecular modeling were reviewed, and also some enlightenments for further investigation were presented.

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Section: The Discovery Of the 23-diaryl-13-thia-zolidin-4-ones As Hmentioning

confidence: 98%

Recent Advances in the Research of 2,3-Diaryl-1,3-thiazolidin-4-one Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

Tian

Zhan²,

Rai³

et al. 2012

CMC

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“…1-aryl-1H,3H-thiazolo[3,4-a]benzimidazoles (TBZs) have shown high activity as HIV-1 NNRTIs [85][86][87]. Structureactivity studies on these compounds suggested that the substitution on the C-1 atom of the thiazolo[3,4-a]benzimidazole moiety played a crucial role in the interaction of TBZs with the HIV-1 RT, especially when a 2,6-dihalo-substituted phenyl ring was present.…”

Section: Reverse Transcriptionmentioning

confidence: 99%

Recent Advances in Combinatorial Chemistry Applied to Development of Anti-HIV Drugs

Pettersson¹,

Clotet‐Codina

Ballana

et al. 2006

MRMC

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“…Novel 1-aryl-3-methyl-1H,3H-thiazolo[3,4-a]benzimidazoles (TBZ's) were prepared and found to possess activity as HIV-1 NNRTI agents [99]. The most potent compound was trans-1-(2,6-difluorophenyl) -3-methyl-1H,3H-thiazolo [3,4-a]benzimidazole (20).…”

Section: Cells Than Against Hiv Lai In Cem-ss Cells the [Azt]-[tsao-mentioning

confidence: 99%

A Review of Recent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor Research Activity

Corbett¹

2002

CMCAIA

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This non-nucleoside reverse transcriptase inhibitor review covers the patent and published literature from January, 1998-August, 2001. Major advances have been made in the past decade in discovering non-nucleoside reverse transcriptase inhibitors that are effective in inhibiting replication of wild-type virus. Attention is now focused upon the discovery of agents that are effective in inhibiting replication of virus' with singly and doubly mutated HIV-1 reverse transcriptase. Notable advances in the discovery of such broad spectrum therapeutics are SG-153 and the quinazolines DPC961 and DPC083. Attempts at discovering other broad spectrum anti-viral agents are presented herein.

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Synthesis, Structure and in Vitro Anti-Human Immunodeficiency virus Activity of Novel 3-Methyl-1H,3H-Thiazolo[3,4-a]Benzimidazoles

Cited by 28 publications

References 14 publications

Recent Advances in the Research of 2,3-Diaryl-1,3-thiazolidin-4-one Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

Recent Advances in the Research of 2,3-Diaryl-1,3-thiazolidin-4-one Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

Recent Advances in Combinatorial Chemistry Applied to Development of Anti-HIV Drugs

A Review of Recent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor Research Activity

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