Phosphorus-substituted imidazole compounds with anti-HIV properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit reverse transcriptase activity and are useful therapeutically for the inhibition of such enzymes, as well as in assays for the detection of such enzymes.

Non nucleoside reverse transcriptase inhibitors

A series of new sulfone compounds containing the 1,3,4-oxadiazole moiety were designed and synthesized. Their structures were identified by 1H and 13C nuclear magnetic resonance and elemental analyses. Antibacterial bioassays indicated that most compounds exhibited promising in vitro antibacterial bioactivities against tobacco bacterial wilt at 200 μg/mL. The relationship between structure and antibacterial activity was also discussed. Among the title compounds, 5′c, 5′h, 5′i, and 5′j could inhibit mycelia growth of Ralstonia solanacearum in vitro by approximately 50% (EC50) at 39.8, 60.3, 47.9, and 32.1 μg/mL, respectively. Among them, compound 5′j was identified as the most promising candidate due to its stronger effect than that of Kocide 3000 [Cu(OH)2] within the same concentration range. Field trials demonstrated that the control effect of compound 5′j against tobacco bacterial wilt was better than that of the commercial bactericide Saisentong. For the first time, the present work demonstrated that s...

Inhibition of tobacco bacterial wilt with sulfone derivatives containing an 1,3,4-oxadiazole moiety.

Benzimidazole nucleus is a constituent of many bioactive heterocyclic compounds that are of wide interest because of their diverse biological and clinical applications. Moreover, benzimidazole derivatives are structural isosters of naturally occurring nucleotides, which allows them to interact easily with the biopolymers of the living system. This created interest in researchers who have synthesized variety of benzimidazole derivatives and screened them for their various biological activities, viz., anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimycobacterial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant as well antidiabetic activities.

Benzimidazole: a medicinally important heterocyclic moiety

Copper(I)-Catalyzed Sulfonylation of 8-Aminoquinoline Amides with Sulfonyl Chlorides in Air

A catalytic bicyclization reaction of 1,5-enynes anchored by α,β-conjugates with arylsulfonyl radicals generated in situ from sulfonyl hydrazides has been established using TBAI (20 mol%) and Cu(OAc)2 (5 mol%) as co-catalysts under convenient conditions. In addition, the use of benzoyl peroxide (BPO) as the oxidant and pivalic acid (PivOH) as an additive was proven to be necessary for this reaction. The reactions occurred through 5-exo-dig/6-endo-trig bicyclizations and homolytic aromatic substitution (HAS) cascade mechanisms to give benzo[b]fluorens regioselectively. A similar catalytic process was developed for the synthesis of γ-ketosulfones. These reactions feature readily accessible starting materials and simple one-pot operation.

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Catalytic arylsulfonyl radical-triggered 1,5-enyne-bicyclizations and hydrosulfonylation of α,β-conjugates

3-O-substituted benzyl pyridazinone derivatives as COX inhibitors.

New styryl sulfones as anticancer agents

Novel water soluble C-ring analogues of 20(S)-camptothecin having the general formula 1, All the compounds of the formula 1 are prepared from the compounds of the general formula 2 having 20(S)-chiral carbon where R1 to R5 have the meaning given above. The compounds of the formula 1 possess potent anti-cancer and anti-viral properties. The invention also provides an alternate process for the preparation of known C-5 substituted compounds of the formula 1,

Water soluble analogues of 20(S)-camptothecin

New 3-O-substituted benzyl pyridazinone compounds have been synthesised and evaluated for their cyclooxygenase inhibitory activity and COX-2 selectivity. Among the compounds synthesised, three compounds (11b–11d) have shown in vitro COX-2 selectivity. These compounds have been evaluated for their in vivo potential using carrageenan-induced rat paw edema assay. One compound (11b) showed 32% anti-inflammatory activity at 30 mg kg−1 dose.

3‐O‐Substituted Benzyl Pyridazinone Derivatives as COX Inhibitors.

Novel water-soluble C-ring analogues of 20(S)-camptothecin having formula (1). The compounds of formula (1) are prepared from the compounds of formula (12) having C-20(S) chiral-carbon. The compounds of formula (1) possess potent anti-cancer and anti-viral properties.

Vamsee Krishna Chintakunta

Papers

3-O-substituted benzyl pyridazinone derivatives as COX inhibitors.

New styryl sulfones as anticancer agents

Water soluble analogues of 20(S)-camptothecin

3‐O‐Substituted Benzyl Pyridazinone Derivatives as COX Inhibitors.

Novel water-soluble c-ring analogues of 20(s)-camptothecin