Hit to lead (H2L) - wiki

Hit to lead (H2L) also known as lead generation is a stage in early drug discovery where small molecule hits from a high throughput screen (HTS) are evaluated and undergo limited optimization to identify promising lead compounds.^[1][2] These lead compounds undergo more extensive optimization in a subsequent step of drug discovery called lead optimization (LO).^[3][4] The drug discovery process generally follows the following path that includes a hit to lead stage:

• target validation (TV) → assay development → high-throughput screening → hit to lead (H2L) → lead optimization (LO) → preclinical drug development → clinical drug development

Further reading:

Hit and lead generation: beyond high-throughput screening

KH Bleicher, HJ Böhm, K Müller, AI Alanine - Nature reviews Drug discovery, 2003

Cited by 887

[HTML] nature.com

[HTML] Hit discovery and hit-to-lead approaches

GM Keserű, GM Makara - Drug discovery today, 2006

Cited by 189

[HTML] sciencedirect.com

[HTML] Hit-to-lead studies: the discovery of potent adamantane amide P2X 7 receptor antagonists

A Baxter, J Bent, K Bowers, M Braddock, S Brough… - Bioorganic & medicinal …, 2003

Cited by 109

[HTML] sciencedirect.com

Abamectin - wiki

Abamectin is a widely used insecticide and anthelmintic.

Abamectin is a mixture of avermectins containing more than 80% avermectin B1a and less than 20% avermectin B1b. These two components, B1a and B1b have very similar biological and toxicological properties. The avermectins are insecticidal and antihelmintic compounds derived from various laboratory broths fermented by the soil bacterium Streptomyces avermitilis. Abamectin is a natural fermentation product of this bacterium.

Abamectin

[B] Ivermectin and abamectin

WC Campbell - 2012

Cited by 417

[HTML] A review of regional and temporal use of avermectins in cattle and horses worldwide

AB Forbes - Veterinary parasitology, 1993

Cited by 48

[HTML] sciencedirect.com

Evolution of a specific fluorogenic derivatization of ivermectin for bioanalytical applications. A review

DW Fink, JSK Shim - Analyst, 1996

Cited by 13

The Morita-Baylis-Hilman reaction - wiki

The Baylis–Hillman reaction is a carbon-carbon bond forming reaction between the α-position of an activated alkene and an aldehyde, or generally a carbon electrophile. Employing a nucleophilic catalyst, such as tertiary amine and phosphine, this reaction provides a densely functionalized product (e.g. functionalized allyl alcohol in the case of aldehyde as the electrophile). This reaction is also known as the Morita–Baylis–Hillman reaction or MBH reaction. It is named for the Japanese chemist Ken-ichi Morita, the British chemist Anthony B. Baylis and the German chemist Melville E. D. Hillman.

Links:

http://www.organic-chemistry.org/namedreactions/baylis-hillman-reaction.shtm
http://www.name-reaction.com/baylis-hillman-reaction

Further reading:

The Catalyzed α‐Hydroxyalkylation and α‐Aminoalkylation of Activated Olefins (The Morita—Baylis—Hillman Reaction)

E Ciganek - Organic Reactions, 1997

Cited by 776

In a patent application published in 1972, Baylis and Hillman reported the reaction of acetaldehyde with ethyl acrylate and acrylonitrile in the presence of catalytic amounts of 1,4-diazabicyclo[2.2.2]octane to give the α-hydroxyethylated products in good yields. No structure proof was given. 

The enantioselective Morita–Baylis–Hillman reaction and its aza counterpart

G Masson, C Housseman, J Zhu - Angewandte Chemie International Edition, 2007

Cited by 413

Asymmetric Morita− Baylis− Hillman Reactions Catalyzed by Chiral Brønsted Acids

NT McDougal, SE Schaus - Journal of the American Chemical Society, 2003

Cited by 311